No abstract

Triphenylpnictogens were oxidazed to access diphenylpnictiogenic acids Ph2XOOH (X = P, As, Sb, Bi). It was shown that oxidation with chloramine-T does not lead to the cleavage of a C–pnictogen...

Selective heterocyclization leading to 1,2,3,4-tetrahydrobenzo[h]quinazolines from ortho-ketimines of 1,8-bis(dimethylamino)naphthalene (DmanIms) under acid catalysis has been revealed. In contrast to rather unreactive N,N-dimethylaniline ortho-ketimine, DmanIms readily undergo this transformation without additional...

This study of the interaction system of binucleophilic 3-substituted 4-amino-4H-1,2,4-triazole-5-thiols and 3-phenyl-2-propynal made it possible to develop a new approach to synthesis of such isomeric classes as 7-benzylidene-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine and 8-phenyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazepine. Among the 20 compounds studied in vitro against influenza A/Puerto Rico/8/34 (H1N1) virus, half of them demonstrated selectivity index (SI) of 10 or higher and one of them (4-((3-phenylprop-2-yn-1-yl)amino)-4H-1,2,4-triazole-3-thiol) possessed the highest (SI > 300). Docking results and values showed that the preferred interactant for our ligands was M2 proton channel of the influenza A virus. Protein-ligand interactions modeling showed that the aliphatic moiety of ligands could negatively regulate target activity level.

The synthesis of 5-aryl-and 4-aryl/hetaryl/cyclopropyl/ alkynyl-5-aryl-1H-pyrrole-2,3-diones by formal isomerization of isoxazole-5-carbaldehydes mediated Mo(CO) 6 in wet MeCN has been developed. The resulting 1H-pyrrole-2,3-diones are good precursors for substituted 1H-pyrrolo[2,3-b]quinoxalines.