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To implement and evaluate a simultaneous multi-slice balanced SSFP (SMS-bSSFP) perfusion sequence and compressed sensing reconstruction for cardiac MR perfusion imaging with full left ventricular (LV) coverage (nine slices/heartbeat) and high spatial resolution (1.4 × 1.4 mmA preliminary study was performed to evaluate the performance of blipped controlled aliasing in parallel imaging (CAIPI) and RF-CAIPI with gradient-controlled local Larmor adjustment (GC-LOLA) in the presence of fat. A nine-slice SMS-bSSFP sequence using RF-CAIPI with GC-LOLA with high spatial resolution (1.4 × 1.4 mmFat signal leakage was significantly higher for blipped CAIPI than for RF-CAIPI with GC-LOLA (7.9% vs. 1.2%, p = 0.010). All 10 SMS-bSSFP perfusion datasets resulted in 16/16 diagnostic myocardial segments. There were no significant differences between the SMS and conventional acquisitions in terms of image quality (2.6 ± 0.6 vs. 2.7 ± 0.2, p = 0.8) or perceived SNR (2.8 ± 0.3 vs. 2.7 ± 0.3, p = 0.3). Inter-reader variability was good for both image quality (ICC = 0.84) and perceived SNR (ICC = 0.70). Myocardial sharpness was improved using the SMS sequence compared to the conventional sequence (0.37 ± 0.08 vs 0.32 ± 0.05, p 0.001). There was no significant difference between measurements of upslope index for the SMS and conventional sequences (0.11 ± 0.04 vs. 0.11 ± 0.03, p = 0.84).SMS-bSSFP with multiband factor 3 and compressed sensing reconstruction enables cardiac MR perfusion imaging with three-fold increased spatial coverage and improved myocardial sharpness compared to a conventional sequence, without compromising perceived SNR, image quality, upslope index or number of diagnostic segments.

PURPOSE To enable free-breathing whole-heart 3D T2 mapping with high isotropic resolution in a clinically feasible and predictable scan time. This 3D motion-corrected undersampled signal matched (MUST) T2 map is achieved by combining an undersampled motion-compensated T2 -prepared Cartesian acquisition with a high-order patch-based reconstruction. METHODS The 3D MUST-T2 mapping acquisition consists of an electrocardiogram-triggered, T2 -prepared, balanced SSFP sequence with nonselective saturation pulses. Three undersampled T2 -weighted volumes are acquired using a 3D Cartesian variable-density sampling with increasing T2 preparation times. A 2D image-based navigator is used to correct for respiratory motion of the heart and allow 100% scan efficiency. Multicontrast high-dimensionality undersampled patch-based reconstruction is used in concert with dictionary matching to generate 3D T2 maps. The proposed framework was evaluated in simulations, phantom experiments, and in vivo (10 healthy subjects, 2 patients) with 1.5-mm3 isotropic resolution. Three-dimensional MUST-T2 was compared against standard multi-echo spin-echo sequence (phantom) and conventional breath-held single-shot 2D SSFP T2 mapping (in vivo). RESULTS Three-dimensional MUST-T2 showed high accuracy in phantom experiments (R2 > 0.99). The precision of T2 values was similar for 3D MUST-T2 and 2D balanced SSFP T2 mapping in vivo (5 ± 1 ms versus 4 ± 2 ms, P = .52). Slightly longer T2 values were observed with 3D MUST-T2 in comparison to 2D balanced SSFP T2 mapping (50.7 ± 2 ms versus 48.2 ± 1 ms, P < .05). Preliminary results in patients demonstrated T2 values in agreement with literature values. CONCLUSION The proposed approach enables free-breathing whole-heart 3D T2 mapping with high isotropic resolution in about 8 minutes, achieving accurate and precise T2 quantification of myocardial tissue in a clinically feasible scan time.

Purpose: To enable whole-heart 3D coronary magnetic resonance angiography (CMRA) with isotropic sub-millimeter resolution in a clinically feasible scan time by combining respiratory motion correction with highly accelerated variable density sampling in concert with a novel 3D patch-based undersampled reconstruction (3D-PROST). Methods: An undersampled variable density spiral-like Cartesian trajectory was combined with 2D image-based navigators to achieve 100% respiratory efficiency and predictable scan time. 3D-PROST reconstruction integrates structural information from 3D patch neighborhoods through sparse representation, thereby exploiting the redundancy of the 3D anatomy of the coronary arteries in an efficient low-rank formulation. The proposed framework was evaluated in a static resolution phantom and in 10 healthy subjects with isotropic resolutions of 1.2mm3 and 0.9mm3 and undersampling factors of ×5 and ×9. 3D-PROST was compared against fully sampled (1.2mm3 only), conventional parallel imaging, and compressed sensing reconstructions. Results: Phantom and in vivo (1.2mm3) reconstructions were in excellent agreement with the reference fully sampled image. In vivo average acquisition times (min:s) were 7:57±1:18 (×5) and 4:35±0:44 (×9) for 0.9mm3 resolution. Sub-millimeter 3D-PROST resulted in excellent depiction of the left and right coronary arteries including small branch vessels, leading to further improvements in vessel sharpness and visible vessel length in comparison with conventional reconstruction techniques. Image quality rated by 2 experts demonstrated that 3D-PROST provides good image quality and is robust even at high acceleration factors. Conclusion: The proposed approach enables free-breathing whole-heart 3D CMRA with isotropic sub-millimeter resolution in

Autosomal recessive primary microcephaly (MCPH) is an abnormal proliferation of neurons during brain development that leads to a small brain size but architecturally normal in most instances. Mutations in the ASPM gene have been identified to be the most prevalent. Thirty-seven patients from 30 unrelated families with a clinical diagnosis of MCPH were enrolled in this study. Screening of ASPM gene mutations was performed by targeted linkage analysis followed by direct sequencing. Thirteen protein truncating mutations of the ASPM were identified in 15 families (50%), eight of which were novel mutations. The mutations detected were eight nonsense, four frameshift, and one splice site. Two of these mutations (p.R1327* and p.R3181*) were recurrent and shared similar haplotypes suggesting founder effect. Patients with ASPM mutations had mild to severe intellectual disability and variable degrees of simplified gyral pattern and small frontal lobe. In addition, hypoplasia of corpus callosum (18 patients), mildly small cerebellar vermis (10 patients), and relatively small pons (13 patients) were found in 85.7%, 47.6%, and 61.9%, respectively. Furthermore, one patient had porencephaly and another had a small midline cyst. Epilepsy was documented in two patients (9.5%). Non-neurologic abnormalities consisted of growth retardation (four patients), and co-incidental association of oculo-cutaneous albinism (one patient). Our study expands the mutation spectrum of ASPM. Moreover, the simplified gyral pattern and small frontal lobe together with hypoplastic corpus callosum, small cerebellum and pons enable ASPM mutated patients to be distinguished. © 2016 Wiley Periodicals, Inc.

New 4-arylazo-3,5-diamino-1H-pyrazole derivatives substituted in the 4-aryl ring with the acetyl moiety were designed and synthesized. The antiproliferative activity of the novel arylazopyrazoles was examined against the MCF-7 cell line. Among all target compounds, 8b (IC50 3.0 µM) and 8f (IC50 4.0 µM) displayed higher cytotoxicity as compared with the reference standard imatinib (IC50 7.0 µM). Further studies to explore the mechanism of action were performed on the most active hit of our library, 8b, via anti-CDK2 kinase activity. It demonstrated good inhibitory effects for CDK2 (IC50 0.24 µM) with 62.5% inhibition, compared with imatinib. The cell cycle analysis in the MCF-7 cell line revealed apoptosis induction by 8b and cell cycle arrest at the S phase. Docking in the CDK2 active site and pharmacophore modeling confirmed the affinity of 8b to the CDK2 active site. Absorption, distribution, metabolism, and excretion studies revealed that our target compounds are orally bioavailable, with no permeation through the blood-brain barrier.

Design and synthesis of some novel pyrazoline and pyranopyrazole derivatives as potential anti-inflammatory agents are described. Most of the compounds were tested for their anti-inflammatory (in vitro and in vivo) and ulcerogenic activities. In all tested compounds, it was found that pyrazolines, 2a, and pyrazolopyrano[2,3-d]pyrimidine 9 are the potent anti-inflammatory and selective cyclooxygenase-2 (COX-2) inhibitor. All compounds are mainly in the safe level. Docking study of 2a and 9 revealed higher affinity for binding with the active site of COX-2 enzyme like SC-558, a selective COX-2 inhibitor.

Aims Echocardiographic studies have shown that left atrial volume (LAV) predicts adverse outcome in small heart failure (HF) cohorts of mixed aetiology. However, the prognostic value of LAV in non-ischaemic dilated cardiomyopathy (DCM) is unknown. Cardiovascular magnetic resonance (CMR) allows accurate and reproducible measurement of LAV. We sought to determine the long-term prognostic significance of LAV assessed by CMR in DCM. Methods and results We measured LAV indexed to body surface area (LAVi) in 483 consecutive DCM patients referred for CMR. Patients were prospectively followed up for a primary endpoint of all-cause mortality or cardiac transplantation. During a median follow-up of 5.3 years, 75 patients died and 9 underwent cardiac transplantation. After adjustment for established risk factors, LAVi was an independent predictor of the primary endpoint [hazard ratio (HR) per 10 mL/m2 1.08; 95% confidence interval (CI) 1.01–1.15; P = 0.022]. LAVi was also independently associated with the secondary composite endpoints of cardiovascular mortality or cardiac transplantation (HR per 10 mL/m2 1.11; 95% CI 1.04–1.19; P = 0.003), and HF death, HF hospitalization, or cardiac transplantation (HR per 10 mL/m2 1.11; 95% CI 1.04–1.18; P = 0.001). The optimal LAVi cut-off value for predicting the primary endpoint was 72 mL/m2. Patients with LAVi >72 mL/m2 had a three-fold elevated risk of death or transplantation (HR 3.00; 95% CI 1.92–4.70; P < 0.001). LAVi provided incremental prognostic value for the prediction of transplant-free survival (net reclassification improvement 0.17; 95% CI 0.05–0.29; P = 0.002). Conclusions LAVi is a powerful independent predictor of transplant-free survival and HF outcomes in DCM. Assessment of LAV improves risk stratification in DCM and should be incorporated into routine CMR examination.

Apoptosis is the primary mechanism through which most chemotherapeutic agents induce tumor cell death. The purpose of this study was to monitor the expression of pro- and anti-apoptotic proteins CD(95) , Bcl-2, as well as copper and zinc levels in the peripheral blood of children with acute lymphocytic leukemia (ALL) prior to and 6 months after the beginning of chemotherapy. Blood parameters and bone marrow blast count were also assessed. Twenty of 26 patients who received treatment showed amelioration in apoptotic response, which is reflected in the elevation of CD(95) , whereas Bcl-2 protein was significantly lowered. In these patients, the elevated serum copper level was not significantly affected whereas the low serum zinc level was significantly raised. Improvement in blood parameters and bone marrow blast count were also achieved. Taken together, the data suggested that assessment of apoptosis signaling molecules might have a predictive impact on treatment outcome.

Please cite this paper as: Guerrero K, Emery S, Wareham K, Ismail S, Watkins A, Lucas M. A randomised controlled trial comparing TVTTM, PelvicolTM and autologous fascial slings for the treatment of stress urinary incontinence in women. BJOG 2010;117:1493–1503. Objective To compare TVTTM, PelvicolTM and autologous fascial slings (AFSs). Design A multicentre randomised control trial. Setting Four units in the UK. Population Women requiring primary surgery for stress urinary incontinence (SUI). Methods A total of 201 women with urodynamically proven stress incontinence were randomised into three groups and assessed at baseline, 6 weeks, 6 months and 1 year. Main outcome measure The primary outcome was patient-reported improvement rates. Secondary outcomes included operative complications/time, intermittent self-catheterisation (ISC) and re-operation rates. The quality-of-life tools used were the Bristol Female Lower Urinary Tract Symptoms (BFLUTS) and EuroQoL. Results Fifty women had a PelvicolTM sling, 79 had AFSs and 72 had TVTTM. At 6 months the PelvicolTM arm had poorer improvement rates (73%) than TVTTM (92%)/AFS (95%); P = 0.003. At 1 year only 61% of the PelvicolTM slings remained as improved, versus 93% of TVTs and 90% of AFSs (P

Objective Levator ani avulsion injury is associated with pelvic organ prolapse. Although it can be detected by magnetic resonance imaging or translabial ultrasonography, both require substantial training. This retrospective study provides baseline measurements of the unilateral coronal or transverse diameter of the levator hiatus and assesses its use in the prediction of levator ani avulsion injury, as a step towards automated detection. Methods Datasets of 787 patients seen in a tertiary urogynecological unit were assessed, including history, examination and three/four-dimensional pelvic floor ultrasound. Unilateral coronal diameters were measured off-line in stored volume datasets, with the operator blinded to clinical data. Volumes obtained during maximum pelvic floor muscle contraction were used, resorting to volumes obtained at rest for patients unable to contract their pelvic floor muscles. Results Ultrasound images were available for 761 patients, including 16 (2.1%) who could not contract their pelvic floor muscles, generating 1522 unilateral measurements (both sides for 761 patients). Levator ani avulsion injury was associated with significant increase in the unilateral coronal diameter (2.57 ± 0.5 vs. 2.1 ± 0.3 cm, P < 0.0001). Receiver–operating characteristics curve analysis showed an area under the curve of 0.801 (95% CI, 0.765–0.837). A cut-off of 2.3 cm had a sensitivity of 71% and a specificity of 79% for the diagnosis of levator ani avulsion injury. Conclusions Levator ani avulsion injury is associated with a significant increase in unilateral coronal diameter, a cut-off point of 2.3 cm being most appropriate for alerting clinicians to a high likelihood of this diagnosis. It is hoped that this information will help to automate the detection of levator ani avulsion injury. Copyright © 2010 ISUOG. Published by John Wiley & Sons, Ltd.

A prospective randomized study was carried out to evaluate the efficacy of physical therapy in addition to splint therapy on treatment outcome in patients with temporomandibular disorders (TMD) with respect to objective and subjective parameters. Twenty-six patients suffering from an arthrogenic TMD and exhibiting a painfully restricted jaw opening were randomized in two groups. Thirteen patients were treated solely with Michigan splint (group I), 13 patients received supplementary physical therapy (group II). Before treatment a clinical examination and electronic recording of jaw movements were performed and subjective pain level was evaluated by visual analogue scales. After 3 months of therapy maintenance of improvement was evaluated. Within treatment groups comparison of data before and after treatment was analysed using Wilcoxon test. Groups were compared by Mann-Withney-U test. A P-value < 0.05 was considered significant. Compared with the baseline, in both groups mandibular movement capacity increased significantly after treatment, whereas subjective pain decreased significantly (P < 0.05). Active jaw opening increased from 28.6 +/- 5.8 to 35.9 +/- 4.8 mm in group I and from 30.1 +/- 5.4 to 40.8 +/- 4.1 mm in group II. After therapy the difference of active jaw opening between groups was significant (P < 0.05). Physical therapy also gave a supplementary improvement of protrusive mandibular movement capacity during electronic registration and subjective pain level. For none of these parameters this difference between groups was significant. Physical therapy seems to have a positive effect on treatment outcome of patients with TMD.

The aim of the present study was to investigate the effects of hot summer climatic conditions (compared to winter) on the libido, semen quality traits, level of serum testosterone hormone and some physiological and body measurements of Egyptian Suffolk rams. A parameter for the tolerance of the rams to adverse hot climatic conditions, designated as the tunica dartos index (TDI), was estimated as the multiplication of the percentage change in scrotal length and that of the percentage difference between rectal temperature and scrotal skin temperature. The relationships between the TDI and semen characteristics were also estimated. The results showed that in summer, the reaction time, pH, percentage dead and abnormal spermatozoa, acrosomal damage and temperatures of rectum, body skin and scrotal skin and scrotal length were significantly higher, while sperm motility, sperm concentration, scrotal circumference and testis length were significantly lower than in winter. The correlation coefficient (r) values estimated between the TDI and each of the semen pH, ejaculate volume, sperm motility and sperm cell concentration were positive, and those estimated between the TDI and each of the reaction time, dead and abnormal spermatozoa and acrosomal damage were negative. The best values of libido (low reaction time), semen pH, semen motility percentage, sperm cell concentration and testosterone level were recorded with a high TDI level (7.5 and more), while those of percentage of dead spermatozoa, sperm abnormalities and acrosomal damage were recorded with a low TDI level (less than 4.5). It can be concluded that the TDI correlates well with the reproductive ability of the ram and can be a reliable parameter to indicate the tolerance of rams to hot subtropical conditions in Egypt.

Novel 2,5-disubstituted thiadiazoles bearing different substituents are obtained by cyclization of thiosemicarbazide (IV) followed by reaction with electrophilic reagents, such as aromatic aldehydes, isatin, phenyl isothiocyanate, and carbon disulfide.

A series of novel quinoxaline 1,4-di-N-oxides is prepared and evaluated for antitumor and hypoxia-selective cytotoxic activities.

Background Pelvic organ prolapse is common and can be detected in up to 50% of parous women although many are asymptomatic. Oestrogen preparations are used to improve vaginal thinning (atrophy). It is possible that oestrogens, alone or in conjunction with other interventions, might prevent or assist in the management of pelvic organ prolapse, for example by improving the strength of weakened supporting structures. Objectives To determine the effects of oestrogens or drugs with oestrogenic effects alone, or in conjunction with other treatments, both for prevention and treatment of pelvic organ prolapse. Search methods We searched the Cochrane Incontinence Group Specialised Register of trials (searched 6 May 2010), MEDLINE (January 1950 to April 2010) as well as reference lists of relevant articles. Selection criteria Randomised or quasi-randomised controlled trials that included the use of any oestrogens or drugs with oestrogenic (or anti-oestrogenic) actions for pelvic organ prolapse. Data collection and analysis Trials were assessed and data extracted independently by two review authors. Main results Three trials and one meta-analysis of adverse effects of a further three trials were identified. One trial did not provide useable data. Two trials included 148 women with prolapse, one included 58 postmenopausal women and the meta-analysis reported a mixed population (women with and without prolapse) of postmenopausal women (N=6984). The meta analysis and one other small trial investigated the effect of selective oestrogen receptor modulators (SERMs) for treatment or prevention of osteoporosis but also collected data of the effects on prolapse. Interventions included oestradiol, conjugated equine oestrogen and two (SERMs), raloxifene and tamoxifen. Only one small trial addressed the primary outcome (prolapse symptoms). One small treatment trial of oestradiol for three weeks before prolapse surgery found a reduced incidence of cystitis in the first four weeks after surgery but this unexpected finding needs to be confirmed in a larger trial. A meta-analysis of adverse effects of a SERM, raloxifene (used for treatment or prevention of osteoporosis in postmenopausal women) found a statistically significant reduction in the need for prolapse surgery at three year follow up (OR 0.50, 95% CI 0.31 to 0.81), but this was statistically significant only in women older than 60 years (OR 0.68, 95% CI 0.22 to 2.08) and the total number of women having prolapse surgery was small. A further small trial comparing conjugated equine oestrogen, raloxifene, tamoxifen and placebo in postmenopausal women having pelvic floor muscle training was too small to detect effects on prolapse outcomes. Authors' conclusions There was limited evidence from randomised controlled trials regarding the use of oestrogens for the prevention and management of pelvic organ prolapse. The use of local oestrogen in conjunction with pelvic floor muscle training before surgery may reduce the incidence of post-operative cystitis within four weeks after surgery. Oral raloxifene may reduce the need for pelvic organ prolapse surgery in women older than 60 years although this cannot be taken as an indication for practice. There is a need for rigorous randomised controlled trials with long term follow up to assess oestrogen preparations for prevention and management of pelvic organ prolapse, particularly as an adjunctive treatment for women using pessaries and also before and after prolapse surgery.

6,7-Dimethylquinoxaline-2,3-dicarboxylic acid anhydride I on treatment with binucleophiles 2 in ethanol at re flux condition affords 2-carboxamidoquinoxaline-3-carboxylic acid derivatives 3a-e. The biscarboxamido derivatives 4a,b are obtained upon treatment of 3a,b with the anhydride derivative I which are converted into the corresponding bispyrrolo derivatives 5a,b. Acetylation of 3a,b with acetic anhydride at room temperature yields the acetamido derivatives 6a,b. While, 3a,b on refluxing with acetic anhydride, afford the pyrrolo[3,4-d]quinoxaline derivatives 7a,b. The pyrrole ring in compounds 7a,b is opened via th e ir reaction with the aromatic amines under fusion condition. Condensation of compound 3a with aromatic aldehydes in DMF furni shes the Schiffs bases 9a,b. While, on repeating the reacti on under fu sion conditi on caused decarboxylation to give th e corresponding Schiffs bases IOa,b. Some of the prepared compounds are tested in vitro for their antimicrobial activities. Quinoxaline derivatives have attracted considerable attention since these compounds showed antimicro­ bial l , antifungal 2 , tuberculostatic 3 , antiviral 4 and anti­ cancers activities. As an extension of our studies on quinoxaline derivatives 6 . lo , it was interesting to syn­ thesize some 6,7-dimethylquinoxaline derivatives with a view to investigating their antimicrobial po­ tency. The effect of side chain variation as acetamido and Schiffs bases upon the antimicrobial activity has been discussed. Also, the chemical behaviour of 6,7dimethylquinoxaline-2,3-dicarboxylic acid anhydride

The reactivity of quinoxaline-2,3-dicarboxylic anhydride 1 towards some heterocyclic amines as nitrogen nucleophiles has been investigated. Cyclic anhydride 1 on treatment with 2-aminobenzo[b]thiophenes 2a-c in refluxing ethanol, gives novel substituted quinoxalines 3a-c. On the other hand, fusion of compound 1 and 2b,c furnishes the corresponding quinoxalines 4a,b. Double cyclization occurs when compound 3b is refluxed with hydrazine hydrate to furnish polyheterocyclic system 6. Pyrroloquinoxalines 7a,b are obtained by refluxing compounds 3a,b in acetic anhydride. Dicarboxamides 8a-c are produced by fusion of 7b with aromatic amines. Thieno[2,3-d]pyrimidine 9 is obtained by refluxing thecompound 4a or 4b with hydrazine hydrate. Condensation of compound 9 with aromatic aldehydes furnishes the corresponding Schiff bases 10a-c. Finally, refluxing of compound 9 with acetic anhydride yields the acetamido derivative 11.

Although cyclosporin A (CsA) and cortisone acetate (CRT) adversely affect bone, their combined effect on bone is unknown. Sprague Dawley rats were therefore administered either vehicle or CsA (7.5 mg/kg/day) by gavage and saline or CRT (2 mg/100 mg/day) by s.c. injection for 28 days. Group A received vehicle plus saline, group B CsA plus saline, group C vehicle plus CRT, and group D CsA/CRT. Serial bloods were sampled over a 28-day period for ionized calcium (Ca), PTH, 1,25 dihydroxyvitamin D (1,25(OH)2D), and bone gla protein (BGP osteocalcin) and tibia were examined on day 28 for histomorphometry. Results were compared with group A. Ca and PTH levels in groups B, C, and D were similar to those in group A during the study period. Group B had lower body weights, elevated levels of BGP, and an increase in 1,25(OH)2D. Group C developed weight loss and a decrease in BGP and 1,25(OH)2D. Group D had weight loss, BGP levels between those of group A and group C, and 1,25(OH)2D values similar to group A. Bone histomorphometry revealed high turnover osteopenia in group B and hyperostosis in group C with a decrease in bone formation and osteoclastlike cells. Combination therapy returned these to control values. In conclusion, the adverse effects of either CsA or CRT on bone in rats are minimized by combined therapy.

A novel series of pyrrolo[2,3-d] pyrimidines bearing sulfonamide moieties have been synthesized and tested for their antitumor activity. Among them, compounds 4, 8b, 8d, 8g and 14 showed promising antitumor activity. Moreover, compound 8d exhibited radioprotective activity. The structures of the newly synthesized compounds were established by their elemental analyses and spectral data.

Naphtho[2,1- b ]pyranone ( 3 ) was allowed to react with arylmethylenemalononitriles to yield 4-amino-5-oxo-2-aryl-5 H -dibenzo[ c , f ]chromene-3-carbonitriles ( 4a , b ); with ethyl 3,4-dichlorobenzylidene cyanoacetate to furnish dibenzo[ c , f ]chromene ( 5 ) and with elemental sulfur in dioxane containing piperidine to give thieno[3,4- d ]naphtho[2,1- b ]pyranone ( 6 ). Similarly, naphtho[1,2- b ]pyranone ( 7 ) was reacted with arylmethylenemalononitriles and elemental sulfur to furnish dibenzo[ c , h ]chromenes ( 8 ) and thieno[3,4- d ]naphtho[1,2- b ]pyranone ( 10 ), respectively. Compound 10 underwent cycloaddition with N -arylmaleimides to yield benzo[7,8]chromeno[3,4- f ]isoindoles ( 11a – c ). Some of these compounds were screened in vitro for their antimicrobial activities.

Malabsorption studies were performed on five Iranian patients with primary small intestinal lymphoma. The effect of oral tetracycline (1.0 g daily) was also studied in three of the above subjects. The results of breath tests (utilizing glycine-1-14C-cholic acid) were abnormal in all five subjects before the antibiotic treatment. Oral tetracycline had a striking effect towards normalizing the results of breath tests. Schilling tests (with intrinsic factor) improve in two patients and steatorrhea improved in all and there was significant weight gain. The antibiotic had no apparent effect on D-xylose or folate absorption tests. It is concluded that bacterial overgrowth in the small intestinal lumen is an important contributory factor to the malabsorption syndrome of this disease.

Sinapine, choline chloride, and sinapic acid were evaluated for bitterness and astringency, at suprathreshold concentrations in water, by a trained sensory panel using magnitude estimation. Power functions (S = kCn) were established for the bitterness of each of the three chemicals and the reference caffeine; none of the exponents for bitterness was significantly different from caffeine (n = 0.98) suggesting that, for any of these taste precursors, a doubling of concentration would double the bitterness perceived. Equimolar solutions of caffeine and sinapine were considered similar in intensity and significantly more bitter than choline chloride; sinapic acid was intermediate in bitterness. The sum of the bitterness values calculated from the power functions for choline chloride and sinapic acid accounted for approximately 80% of the bitterness of sinapine, at equimolar concentrations. Fifty to 94% of the bitterness perceived from tasting water slurries of rapeseed flour and protein concentrate was explained by the bitterness expected from their content of sinapine and free choline. Reliable power functions could not be established for the astringency of sinapine, choline chloride, and sinapic acid at the concentrations used. However, a clear psychophysical function was established for the astringency of the reference alum.

Reaktion von Grignardverbindungen mit gemischten Diimiden N-Phthalimidosukzinimid 1 und N-Phthalimidomaleinsaureimid 2 entstehen aus N-Aminophthalimid und Succzinsaure- bzw. Maleinsaureanhydrid. 1 reagiert mit Grignardverbindungen zu den 3, 3-disubstituierten Phthaliden 3 und N-Aminosucczinimid. 2 reagiert mit Grignardverbindungen ebenfalls zu den Phthaliden 3 und einem schwer zu reinigenden Verbindungsgemisch. N-Phthalimidomaleinsaureimid 2 reagiert leicht mit Diazoalkanen und Stickstoffwasserstoffsaure.

Arylmagnesium bromides react with N-arylcitraconimides at room temperature, to give 5-aryl-5-hydroxy-3-methyl-N-aryl-2-pyrrolinones 1, which can be considered as the cyclic form of cis-β-aroyl-α-methyl-N-arylacrylamides, as the sole product. The structure assignments are based on infrared and electronic spectra and also on the synthesis of these compounds by the isomerisation of the corresponding trans-isomers 3 which are synthesised by the reaction between trans-β-aroyl acryloyl chlorides and amines. Arylmagnesium halides react with 1 to give β-aroyl-β-aryl-α-methyl-N-arylpropionamides 5 as the sole product in most cases. However, in few cases a poor yield of an isomeric substance 5′ is obtained in addition to the predominating isomers. 5a, c, e and j are also obtained by the action of 3 moles of the suitable Grignard reagent on one mole of N-arylcitra-conimide. Structural assignments are based on infrared, electronic and nuclear magnetic resonance spectra.