408538-63-6Relevant academic research and scientific papers
Design, synthesis and screening of some novel benzoxazole based 1,3,4-oxadiazoles as potential antimicrobial agents
Vodela, Sunil,Mekala, Raghu Vardhan Reddy,Danda, Ravinder Reddy,Kodhati, Venkateshwarlu
, p. 625 - 628 (2013/07/27)
A series of novel 2-(5-substituted-[1,3,4]oxadiazol-2-yl)-benzoxazoles (7a-h) were synthesized in good yields in two different directions by involving benzoxazole-2-carboxylic acid (1) as raw material and benzoxazole-2-carbonyl chloride (2), benzoxazole-2-carboxylic acid methyl ester (3), benzoxazole-2-carboxylic acid hydrazide (4), benzoxazole-2-carboxylic acid N′-acetyl hydrazide (5a-d) and benzoxazole-2-carboxylic acid-ethylidene-hydrazides (6a-d) as reactive intermediates. The chemical structures of all the synthesized compounds were elucidated by their IR, 1H NMR and 13C NMR and mass spectral data. Further, the target compounds were screened for their antimicrobial activity against various Gram-positive and Gram-negative bacteria.
Synthesis and screening of some novel 2-[5-(Substituted phenyl)-[1,3,4]oxadiazol-2-yl]-benzoxazoles as potential antimicrobial agents
Gadegoni, Hemalatha,Manda, Sarangapani,Rangu, Shivaprasad
, p. 221 - 226 (2013/07/26)
A series of some novel 2-[5-(substituted phenyl)-[1,3,4]oxadiazol-2-yl]- benzoxazoles were synthesized by using benzoxazole-2-carboxylic acid on reaction with thionyl chloride in presence of ethanol solvent at room temperature gave benzoxazole-2-carbonyl chloride, which is turned into benzoxazole-2-carboxylic acid hydrazide on reaction with hydrazine hydrate in ethanol solvent under reflux. The subsequent treatment of benzoxazole-2-carboxylic acid hydrazide with an appropriate aromatic carboxylic acid in presence of polyphosparic acid under reflux afforded the title compounds. The chemical structures of the newly synthesized compounds were elucidated by their IR, 1H NMR and Mass spectral data analysis. Further the compounds are used to find out their ability towards anti microbial and nematicidal activity.
Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors
Romero,Morge,Biles,Berrios-Pena,May,Palmer,Johnson,Smith,Busso,Tan,Voorman,Reusser,Althaus,Downey,So,Resnick,Tarpley,Aristoff
, p. 999 - 1014 (2007/10/02)
A variety of analogues of 1-[4-methoxy-3,5-dimethylbenzyl]-4-[3- (ethylamino)-2-pyridyl]piperazine hydrochloride (U-80493E) were synthesized and evaluated for their inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis(heteroaryl)piperazines (BHAPs) that were 10-100-fold more potent than U-80493E. The pyridyl portion of the lead molecule was found to be very sensitive to modifications. Extensive preclinical evaluations of several of these compounds led to the selection of 1-[(5-methoxyindol-2-yl)carbonyl]-4-[3-(ethylamino)-2- pyridyl]piperazine methanesulfonate (U-87201E, atevirdine mesylate) for clinical evaluation.
