A novel coordination nanocage was obtained with in situ-generated tetrazole ligands from the cobalt-thiacalix[4]arene system. Four in situ-generated 1,3-bis(2H-tetrazol-5-yl)benzene ligands bolster eight Co4-calix shuttle-cock-like secondary building units (SBUs) into a hollow tetragonal prism with a high surface area. The unprecedented {Co32} nanocage presents the highest nuclearity example.

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...

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...

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...

Protein arginine deiminases (PADs) catalyze the post-translational hydrolysis of arginine residues to form citrulline. This once obscure modification is now known to play a key role in the etiology of multiple autoimmune diseases (e.g., rheumatoid arthritis, multiple sclerosis, lupus, and ulcerative colitis) and in some forms of cancer. Among the five human PADs (PAD1, -2, -3, -4, and -6), it i...