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This study examines the relationship between; erythrocyte membrane bound Na+K+- ATPase activity, HbA1c level, Hb-AGE (hemoglobin advanced glycation end product) level and lipid profile in Indian diabetic population. The aim was to look at the dependence of this parameter on glycemic and lipid indices in general. Control subjects were volunteers with no diabetic history but were either normolipidemic or dyslipidemic. The diabetic patients were categorized on the basis of glycemic control (HbA1c values) and further into normolipidemic or dyslipidemic groups. HbA1c was analyzed by affinity chromatography while all other parameters including hemoglobin, plasma glucose and lipid profile was estimated using kits on automated analyzer. Hb-AGE was measured in terms of fluorescence intensity and RBC-ATPase activity was measured using an assay kit. Among the diabetic groups, patients in the uncontrolled category (Group 3) were maximally dyslipidemic with high total cholesterol (TC) and triglyceride levels (TG). Observations indicate that even though HbA1c is not significantly different between dyslipidemic and normolipidemic patients in each group, levels of fasting blood sugar, TG and LDL cholesterol were significantly higher in the former. Na+-K+ATPase activity was found to decrease as a function of HbA1c in an inverse manner but did not show any significant correlation with TC levels. Our data indicates that erythrocyte membrane Na+-K+ATPase activity is significantly related to glycemic status rather than to the lipidemic status of individuals in the Asian Indian population. Glycation of the membrane proteins rather than increase in membrane cholesterol content alters the enzyme function.

[3H]SCH 211803, at a specific activity of 1.56 Ci/mmol, was prepared by direct exchange with tritiated water and platinum metal. [2H4]SCH 211803 was prepared from [2H]formaldehyde in a seven step synthesis in 10% yield. [14C]SCH 211803 was prepared from N‐benzyl‐4‐hydroxy[2‐14C]piperidine in a four‐step synthesis in 35% radiochemical yield. Additionally a high specific activity batch of [3H]SCH 211803 was prepared by Ru(Ph3P)3Cl2 catalysed exchange with 90 at% tritiated water to a specific activity of 35 Ci/mmol. Copyright © 2007 John Wiley & Sons, Ltd.

[3H]Sch 66336 was prepared at a specific activity of 1.35 Ci/mmol by Ru(Ph3P)3Cl2 catalysed exchange with tritiated water. [13C215N]Sch 66336 was synthesized from potassium [13C]cyanide and [13C15N2]urea in 29% overall yield from potassium [13C]cyanide. [14C]Sch 66336 was synthesized from potassium [14C]cyanide in 31% yield. A second synthesis, from N‐Boc‐4‐hydroxy[14C]piperidine, gave [14C]Sch 66336 labelled in a different site in 19% overall yield. Copyright © 2004 John Wiley & Sons, Ltd.

A series of polyhalogenated imidazole nucleosides were designed and synthesized as ring-contracted analogues of 2,5,6-trichloro-1-(β-d-ribofuranosyl)benzimidazole (TCRB) and its 2-bromo analogue (BDCRB) in an effort to explore the spatial limitation of the active pocket(s) in the target protein(s). 2,4,5-Trichloro-, 2-bromo-4,5-dichloro-, and 2,4,5-tribromoimidazole nucleosides were prepared by a condensation of the preformed heterocycles with the appropriate sugar precursors. The ribofuranosyl and xylofuranosyl analogues were prepared by a direct glycosylation using the Vorbruggen's silylation method and provided exclusively the β-anomers. The arabinofuranosyl analogues were prepared by the sodium salt method to give both the α- and β-anomers. The absolute configurations were established by ¹H NMR spectroscopy. Alkylation of the polyhalogenated imidazoles with the appropriate bromomethyl ethers gave the acyclic acyclovir and ganciclovir analogues. In general, the parent polyhalogenated imidazoles showed some activity against human cytomegalovirus (HCMV) (IC50 ~ 35 μM). However, with the exception of two tribromo analogues (7c, 13c-β), most of their nucleoside derivatives were inactive against both HCMV and herpes simplex virus type-1 (HSV-1) and were not cytotoxic. The results suggest that the ring-contracted nucleoside analogues of TCRB and BDCRB interacted weakly or not at all with viral and cellular targets.

³H-Sch 58235 was prepared at a specific activity of 29.1 Ci/mmol by Ir(COD)(Cy3P)PyPF6 catalysed exchange with tritium gas. ¹⁴C-Sch 58235 was prepared in three steps from p-hydroxy[ring-U-¹⁴C]benzaldehyde with an overall radiochemical yield of 21%. ¹³C6-Sch 58235 was similarly prepared in three steps from p-hydroxy[ring-U-¹³C6]benzaldehyde in an overall yield of 41%. Copyright © 2002 John Wiley & Sons, Ltd.

The sodium salt of 2,5,6-trichlorobenzimidazole (8a) was condensed with [2-(benzyloxy)ethoxy]methyl chloride (9) and [1,3-bis(benzyloxy)-2-propoxy]methyl chloride (18) to provide the corresponding protected acyclic nucleosides 10a and 19a, which on debenzylation afforded 2,5,6-trichloro-1-[(2-hydroxyethoxy)methyl]benzimidazole (11a) and 2,5,6-trichloro-1-[(1,3-dihydroxy-2-propoxy)methyl]benzimidazole (20a), respectively. A similar condensation of 2,4,6-trichlorobenzimidazole (2a) and 2,4,5-trichlorobenzimidazole (7a) followed by debenzylation yielded 11b, 20b, 11c, and 20c, respectively. A nucleophilic displacement of the 2-chloro group of 11a−c and 20a−c with liquid ammonia, methylamine, dimethylamine, and thiourea furnished several interesting 2-substituted compounds in good yields, e.g., 12−14(a−e), 21−23(a−e), 15−17, and 24−26. Alkylation of the 2-thio analogs 15−17 and 24−26 with benzyl chloride furnished the 2-alkylthio acyclic nucleosides 12d−14d and 21d−23d. Desulfurization of 15 and 24 with Raney Ni furnished 5,6-dichloro-1-[(2-hydroxyethoxy)methyl]benzimidazole (12e) and 5,6-dichloro-1-[(1,3-dihydroxy-2-propoxy)methyl]benzimidazole (21e), respectively (acyclic analog of 5,6-dichloro-1-β-d-ribofuranosylbenzimidazole). Similarly the dihalo compounds 13e, 14e, and 23e were prepared in moderate yields from the 2-thio analogs 16, 17, and 26. Treatment of 2-bromo-5,6-dichlorobenzimidazole (8b) with 27 and 30 gave the protected acyclic compounds 28a and 31a, which on deacetylation with sodium carbonate and potassium cyanide yielded 2-bromo-5,6-dichloro-1-[(2-hydroxyethoxy)methyl]benzimidazole (29a) and 2-bromo-5,6-dichloro-1-[(1,3-dihydroxy-2-propoxy)methyl]benzimidazole (32a), respectively, in moderate yields. The 2-bromo-4,6-dichlorobenzimidazole and 2-bromo-4,5-dichlorbenzimidazole analogs 29b,c and 32b,c were prepared in a similar manner. Compounds were tested for activity against human cytomegalovirus (HCMV) and herpes simplex virus type 1 (HSV-1) and for cytotoxicity. In marked contrast to the ribosylbenzimidazoles, none of the acyclic analogs were specific and potent inhibitors of HCMV. Only the 2-thiobenzyl analogs 12d, 13d, 14d, and 23d and the 2-Br analogs 32a,b were active, but activity was not well separated from cytotoxicity. The lack of specific and potent antiviral activity strongly suggests that these acyclic nucleoside analogs are not phosphorylated by HCMV or HSV-1 gene products and that the ribosylbenzimidazoles do not require phosphorylation for antiviral activity.

We give a logic-based framework for defining counting problems and show that it exactly captures the problems in Valiant′s counting class #P. We study the expressive power of the framework under natural syntactic restrictions and show that some of the subclasses obtained in this way contain problems in #P with interesting computational properties. In particular, using syntactic conditions, we isolate a class of polynomial time computable #P problems and, also, a class in which every problem is approximable by a polynomial time randomized algorithm. These results set the foundation for further study of the descriptive complexity of the class #P. In contrast, we show, under reasonable complexity theoretic assumptions, that it is an undecidable problem to tell if a counting problem expressed in our framework is polynomial time computable or if it is approximable by a randomized polynomial time algorithm. Finally, we discuss some open problems which arise naturally from this work.

³H-SCH 51048 and ¹⁴C-SCH 56592 have been synthesized. ³H-SCH 51048 was prepared in two steps by acid catalyzed tritium exchange while ¹⁴C-SCH 56592 was prepared in three steps from ¹⁴C-formamidine acetate in an overall 21% radiochemical yield. © 1998 John Wiley & Sons, Ltd.

3H‐SCH 51048and 14C‐SCH 56592have been synthesized. 3H‐SCH 51048 was prepared in two steps by acid catalyzed tritium exchange while 14C‐SCH 56592 was prepared in three steps from 14C‐formamidine acetate in an overall 21% radiochemical yield. © 1998 John Wiley & Sons, Ltd.

14C‐Felbamate, 2‐[ring‐U‐14C]phenyl‐1,3‐propanediol‐dicarbamate, (1), was synthesized. The carbon label was introduced into Felbamate using uniformly labelled diethyl 2‐phenylmalonate as the starting material. © 1997 John Wiley & Sons, Ltd.

Abstract: Treatment of small postoperative interloop abscesses (ILA) can be challenging. In children, these collections have usually been drained surgically at a second operation. This article describes three children with small postoperative ILAs who were treated by percutaneous needle aspiration and parenteral antibiotics, with good outcomes. The advantages of this technique and its utilization in the management of children with ILAs are discussed.

A 50-year-old non-diabetic male subject was admitted for right sided hydropneumothorax. 4 days prior to this admission the patient had developed a high grade fever with shaking chills, a cough with scanty expectoration that later turned purulent and a discomfort in the right side of the chest. He denied any history of seizures, trauma to chest and contact with domestic animals. He was a smoker and had consumed alcohol socially. He had no past history of significant respiratory illness.

The synthesis of the acyclic spongosine analogues (V) and (VII) is carried out starting from the reaction of 2,6‐dichloropurine (I) with the chloro compounds (II) or (VI).