A catalytic route for enantioselective total synthesis of cell adhesion inhibitor BIRT-377 is described. The quaternary stereocenter was constructed through l-proline-derived, tetrazole-catalyzed direct asymmetric alpha-amination of 3-(4-bromophenyl)-2-methylpropanal with dibenzyl azodicarboxylate. In the course of these studies, a one-pot trifluoro acetylation/selective benzyloxycarbonyl depro...

A novel (3,4)-connected 3D self-penetrating metal-organic framework with a nanometre-scale cavity constructed from metallacalix[4]arene building blocks and Keggin-type polyanions has been obtained by using a 1,3-bis(1-methyl-5-mercapto-1,2,3,4-tetrazole)propane ligand.

Some pentafluoropyridine derivatives have been synthesized by the reaction of pentafluoropyridine with appropriate C, S and N-nucleophile such as malononitrile, 1-methyl-tetrazole-5-thiol and piperazine. These reactions provided 4-substituted 2,3,5,6-tetrafluoropyridine derivatives in good yields. All the compounds were characterized using (1)H, (13)C and (19)F-NMR spectroscopy and X-ray crysta...

BACKGROUND Obstructive sleep apnea syndrome (OSAS) is a highly prevelant disorder and found in approximately 2-4% of middle-aged adults. OBJECTIVES To assess the efficacy of Watch-PAT-200 in the diagnosis of obstructive sleep apnea syndrome (OSAS). PATIENTS AND METHODS Patients suspected of having OSAS underwent overnight Level I polisomnography and simultaneously wore Watch-PAT-200 in the ...

A new series of 1-(4-{5-Amino-6-fluoro-1-[2'-(2H-tetrazole-5-yl)-biphenyl-4-ylmethyl]-1Hbenzoimidazol-2-yl}-phenyl)-3-chloro-4-(Substituted -phenyl)-azetidin-2-one derivatives MCS 06[1-15] has been synthesized and subjected to evaluate their antihypertensive activity. All the synthesized compounds of the series elicit remarkable activity in comparison to standard drug (Losartan). Structures of ...

A tetrazole ring is often used in drug discovery as a replacement for the carboxylic acid group. Previous work indicates that compounds containing a tetrazole moiety show asymmetric permeability in Caco-2 cells characteristic of an efflux transporter substrate. The aim of this study is to determine which transporters are responsible for polarization of transport of tetrazole-containing compound...

A series of methyl 6-Chloro-2-Substitued-1-[2-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]1H-benzoimidazol-5-ylamine were successfully synthesized. Benzimidazoles were prepared by condensation of 4-chloro-o-phenylenediamine with substituted aryl, aldehyde condensation with biphenyl tetrazole group and reduction stannous chloride dihydrate. An insertion-cyclization strategy was involved during synthe...

The monoclonal IgM antibody PAT-SM6 derived from human tumours induces apoptosis in tumour cells and is considered a potential anti-cancer agent. A primary target for PAT-SM6 is the unfolded protein response regulator GRP78, over-expressed externally on the cell surface of tumour cells. Small angle X-ray scattering (SAXS) studies of human GRP78 showed a two-domain dumbbell-shaped monomer, while...

INTRODUCTION We report the synthesis of novel 1,4-dihydropyridine derivatives containing biphenyl-2'-tetrazole moieties. We hypothesized that merging the key structural elements present in an AT1 receptor antagonist with key structural elements in 1,4-dihydropyridine calcium channel blockers would yield novel analogs with potential dual activity for both receptors. This strategy led to the desi...

The inhibition of insulin-regulated aminopeptidase (IRAP, EC 3.4.11.3) by angiotenesin IV is known to improve memory and learning in rats. Screening 10 500 low-molecular-weight compounds in an enzyme inhibition assay with IRAP from Chinese Hamster Ovary (CHO) cells provided an arylsulfonamide (N-(3-(1H-tetrazol-5-yl)phenyl)-4-bromo-5-chlorothiophene-2-sulfonamide), comprising a tetrazole in the...