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Introduction A necrotic lung ball is a rare radiological feature that is sometimes seen in cases of pulmonary aspergillosis. This paper reports a rare occurrence of a necrotic lung ball in a young male caused by Candida and Streptococcus pneumoniae. Case report A 28-year-old male with pulmonary candidiasis was found to have a lung ball on computed tomography (CT) of the chest. The patient was treated with β-lactams and itraconazole and then fluconazole, which improved his condition (as found on a following chest CT scan) and serum β-D-glucan level. The necrotic lung ball was suspected to have been caused by coinfection with Candida and S. pneumoniae. Conclusion A necrotic lung ball can result from infection by Candida and/or S. pneumoniae, indicating that physicians should be aware that patients may still have a fungal infection of the lungs that could result in a lung ball, even when they do not have either Aspergillus antibodies or antigens.

A series of (nitrooxy)alkyl apovincaminates has been synthesized and evaluated for their effects on vertebral and femoral blood flow. These derivatives were prepared from apovincaminic acid (4). In cerebral circulation, compound 5 (0.03-1.0 mg/kg iv) caused a dose-dependent increase in cerebral blood flow (CerBF) without affecting the blood pressure. It was more potent than vinpocetine (2). The structures of 2 and 5, determined by X-ray crystallography, showed differences in the electrostatic potential image and in the conformation of the ethyl group at the 16-position.

Two new platelet aggregation inhibitors, PI-200 and PI-201 were isolated from the fermentation broth of Streptomyces sp. A7498. PI-200 and PI-201 inhibited ADP-induced aggregation of rabbit platelets with an IC50 of 3.8 x 10(-4) M and 7.1 x 10(-4) M, respectively.

Two new cembrane-type diterpenoids, sarcodiol (1) and 3,4-epoxysarcophytonin (4), were isolated from Okinawan soft coral of the genus, Sarcophyton. Their structures were determined from spectroscopic measurements, X-ray analysis and chemical reaction.

The conformations of tricyclic ketolide TE-802 (1) and its analogue were determined by crystallographic analysis and NMR spectroscopy. The 3-carbonyl function of 1 took an 'exo' orientation against the lactone ring, and the orientation of the amino sugar at the 5-position differed from that in clarithromycin (CAM:2). On the other hand, di- and tricyclic ketolides and a tricyclic macrolide were found to exist in 'semi-fold-out (4H-downward)' conformation in deuteriochloroform. The conformation of 1 in deuteriochloroform was closely similar to that in D,O. The newly formed tetrahydrodiazepine ring existed in chair form or boat form, governed by the presence of substituent and its position.

A new method has been developed for the synthesis of chiral β-amido cyanides by means of the regioselective cleavage of β-lactams in the presence of a TMSOTf catalyst and RCN

Hantzsch cyclization of cyanoethyl 3-aminocrotonate and (E,Z)-4,4-dialkoxy-2-benzylideneacetoacetates 12a–h afforded the corresponding 3,4-trans-2-hydroxy-1,2,3,4-tetrahydropyridines 14a–h with high stereoselectivity. 1H NMR and X-ray analyses of compound 14a established the configuration of 3-H and 4-H as trans and that of 3-H and 2-OH as trans also.

Enantiomeric (+)- and (–)-methy3-nitrooxypropyl 1,4-dihydro-2,6-dimethyl-4-(3- nitrophenyl) pyridine-3,5-dicarboxylate 1 were synthesized by esterification of the optically active monocarboxylic acids (+)-6 and (–)-6, which are available from racemate (±)-6 by optical resolution using cinchonidine and cinchonine. The absolute configuration of the key intermediates (S)-(+)-6 and (R)-(–)-6, was also unambiguously determined by the comparison with optical active (+)- and (–)-1 derived from (R)-(–)- and (S)-(+)-7 and (+)- and (–)-6, and X-ray crystallographic analysis of bromoethyl ester (R)-(–)-8 prepared from the acid (S)-(+)-7.

The three-dimensional structure of the E-64-c-papain complex has been determined by X-ray crystal analysis at 2.5 Å resolution (conventional R = 26.9%). The structure determined indicates that: (i) the C2 atom of the oxirane ring of E-64-c is covalently bound by the Sγ atom of Cys-25 of papain; (ii) this covalent bond formation results in a configurational conversion of the oxirane C2 atom from the S- to the R-form; and (iii) extensive hydrogen bonding and hydrophobic interactions are responsible for the specific interaction of the E-64-c molecule with papain.

In order to elucidate the conformational characteristics of cysteine protease inhibitors contributing to their inhibitory activities, the conformation of E-64 (N-[N-(L-3-trans-carboxyoxiran-2-carbonyl)-L-leucyl]-agmatine), a potent inhibitor of papain, was determined by X-ray crystal structure analysis. The molecules were packed in the crystal through electrostatic forces and hydrogen bonding between the oppositely charged terminal groups and between the amide groups. Two crystallographically independent E-64 molecules both took a flattened and slightly curved structure, which is similar to that of loxistatin, a related cysteine protease inhibitor. Based on the present results, a possible inhibitory mechanism of E-64 is proposed, with reference to the binding mode observed in the crystal structure of papain-substrate analogue complex.

Background A sudden onset of chest pain, which often reflects a life-threatening disease, requires prompt diagnosis in the emergency department. Findings A 12-year-old boy presented with sustained chest pain and dyspnea after diving into a swimming pool and was transferred to our emergency department. A chest examination noted a crunching and rasping sound at the precordium, synchronous with the heartbeat. Chest radiography showed lucent streaks and the mediastinal pleura at the left cardiac outline. Additionally, computed tomography showed massive pneumomediastinum surrounding the heart. Thus, he was diagnosed with spontaneous pneumomediastinum. Conclusions Spontaneous pneumomediastinum should be considered in the differential diagnosis of chest pain. In addition to medical history-taking, careful physical examination, which can identify the characteristic finding of a friction sound synchronous with the heartbeat (Hamman’s sound), will help in the immediate diagnosis of spontaneous pneumomediastinum.

The first highly asymmetric Pummerer-type cyclization of chiral, non-racemic β-amido sulfoxides to enantiomerically enriched β-lactams (80-85% ee) is described. S- and R-Sulfoxides (S-2a-d and R-2a-c) were treated with O-methyl-O-tert-butyldimethylsilyl ketene acetal 1 in the presence of a catalytic amount of zinc chloride in methylene dichloride to give predominantly the corresponding 4R- and 4S-β-lactams (R-3a-d and S-3a-c) in more than 80% ee. These results show that the stereoinduction is governed by the absolute configuration of the sulfoxides. Optically pure R- and S-3c were readily obtained by simple recrystallization in about 60% yield. The usefulness of the chiral, non-racemic 4-tolylsulfanyl-β-lactams 3a-d has been shown by their conversion into the key intermediate 11 for the optically pure carbapenem antibiotic, (+)-PS-5.

Background Carcinoma and adenoma of the duodenum, including the papilla of Vater, are problematic diseases in patients with familial adenomatous polyposis (FAP). Case presentation A 36-year-old man underwent a periodic medical examination for early colon cancer originating from FAP for which laparoscopic-assisted subtotal colectomy with a J-shaped ileal pouch-rectal anastomosis was performed 3 years earlier. A tumor was detected at the papilla of Vater along with elevation of total bilirubin and hepatobiliary enzymes. Although cytology did not determine the tumor to be an adenocarcinoma, we suspected adenocarcinoma due to its hypervascularity shown by contrast-enhanced computed tomography. Pylorus-preserving pancreaticoduodenectomy with modified Imanaga reconstruction and regional lymph node dissection (D2) was performed. The pathological study showed that the tumor was a papillary and moderately differentiated tubular adenocarcinoma. The patient is currently in good health without recurrence, weight loss, or severe diarrhea at 12 months after surgery. Conclusions Awareness of biliary-pancreatic symptoms and periodic gastroduodenoscopy might contribute both to the early detection of duodenal or periampullary polyps and cancer and to the radical treatment of FAP. Modified Imanaga reconstruction has the potential to become one of the more effective procedures for providing good quality of life to FAP patients with duodenal or periampullary cancer.