Synthesis and testing of 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazole derivatives for antifungal activity against selected Candida Species

Abstract

Uma série de 21 derivados, 1,3,4-oxadiazolinas, foi sintetizada pela ciclização de N-acilhidrazonas com anidrido acético e avaliada in vitro quanto à sua atividade antifúngica contra seis espécies de Candida: Candida albicans (ATCC 90028 e LM V-42), Candida krusei (ATCC 6258 e LM 12 C) e Candida tropicalis (ATCC 13803 e LM 14). As espécies de Candida foram consideradas sensíveis a uma série dos compostos, os quais inibiram o crescimento de 50 a 90%, com um intervalo de concentração inibitória mínima (MIC) de 64 a 512 µg mL -1 . As estruturas dos compostos foram totalmente confirmadas e caracterizadas pelas técnicas de infravermelho com transformada de Fourier (FTIR), ressonância magnética nuclear (NMR) de 1 H e 13 C, e espectrometria de massa (MS).A series of 21 1,3,4-oxadiazoline derivatives was synthesized by cyclization of N-acylhydrazones with acetic anhydride and evaluated for their in vitro antifungal activity against six Candida strains: Candida albicans (ATCC 90028 and LM V-42), C. krusei (ATCC 6258 and LM 12 C) and C. tropicalis (ATCC 13803 and LM 14). The Candida strains were found to be sensitive to some of the compounds, which inhibited the growth by 50-90%, with minimum inhibitory concentration (MIC) in the range of 64-512 µg mL -1 . The compounds' structures were fully confirmed and characterized by Fourier transform infrared spectroscopy (FTIR), 1 H and 13 C nuclear magnetic resonance (NMR) and mass spectrometry (MS).

Synthesis of some new 1-(5-((1H-pyrazol-1-yl)methyl)-2-aryl-1,3,4-oxadiazol-3(2H)-yl) ethanone derivatives and study their antimicrobial activity

“…A mixture of compound 2 (0.1 mol) and appropriate aromatic aldehyde (0.1 mol) in (50 ml) of absolute ethanol, the mixture was re ex for 4 hrs and concentrated and cooled the reaction mixture [26]. The crude product was obtained, separated by ltration, and recrystallized from ethanol.…”

Synthesis and in vivo Anti-inflammatory and Analgesic activities of Oxadiazoles clubbed with Benzothiazole nucleus

“…Both the nucleuses are well acknowledged to possess a wide range of pharmaceutical, agrochemical, and biological applications. Substituted-oxadiazoles show wide variety of biological activities; anti-inflammatory (Ali et al, 2014) and (Husain and Ajmal, 2009) analgesic (Ali et al, 2010) and (Badiadka et al, 2005) antibacterial (Shridhar et al, Desai et al, 2014, Sahin et al, 2002 antifungal (Oliveira et al, 2013) and anticancer activities (Abu-Zaied et al, 2012 andValente et al, 2014). Benzothiazole derivatives have also reported to show antiinflammatory (Abbas et al, 2013 andPatil et al, 2015) analgesic Sharma et al, 2013a) antifungal (Liu et al, 2013) anticancer (Gurdal et al, 2015) and antimicrobial (Sigmundova et al, 2007and.…”

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“…Anticonvulsant 5 , Anti-diabetic 6 , Antimicrobia l7 , Antifungal [8][9] , CNS depressant 10 , Antimalarial 11 , Anthelmintic 12 , Anticancer 13 Antiurease 14 , Hypoglycemic agent 15 , Anti-oxidant 16 , Antihelmenthic 17 , Anti-histaminic 18 , Insecticidal 19, Anti-HIV 20 , Antiprotozoal 21 , Antitubercular 22 .…”