Synthesis and antimicrobial screening of some novel substituted aryloxy acids and their 1,3,4-oxadiazole derivatives

Shubhalaxmi, . and Pathak, Lokesh and Ananda, K and Bhat, Subrahmanya K (2015) Synthesis and antimicrobial screening of some novel substituted aryloxy acids and their 1,3,4-oxadiazole derivatives. In: 10th Mid Year CRSI Symposium in Chemistry, Jul 23-25 2015, NIT, Trichy.

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Abstract

The development of new and multidrug resistant microorganisms against present antibiotics warrant urgent need of broad spectrum and highly effective antimicrobial agents with novel structural characteristics [1]. Synthesis of novel molecules based on hybrid pharmacophores are expected to achieve pluripotent pharmacological activities. Oxadiazole is an important chemical moiety which is widely synthesized and studied for its various biological activities. Some of the noted applications include anti-microbial, anti-inflammatory and analgesics, anti- convulsant, anticancer agents [2]. Ayloxyacetic acid scaffolds are extensively studied for diuretic action as one of the important and widely used diuretic drug ethacrynic acid. Moreover, aryloxyacetic acids could be seen as bioisosteric analog of phenylpropionic acid or dihydrocinnamic acids, and were shown to have potent antimicrobial activities [3]. In this context it would be interesting to see antimicrobial potential of much overlooked and untapped potential of aryloxyacetic acid derivatives as antimicrobial agents, with chalcone side chain which can potentially enhance their biological properties [4]. In view of this, some oxadiazolo-propenone (1) derivatives were synthesized to investigate their potential antimicrobial activities, after in-silico screening by docking. The chemical structures of the compounds were elucidated by IR, 1H NMR and FAB-MS spectral data and elemental analyses. Antibacterial and antifungal activities of the compounds were determined using zone of inhibition and MIC studies. The QSAR was performed for the molecules for similar activities based on MIC results. Compounds in the series exhibited different levels of antimicrobial activities when compared to the reference drug ciprofloxacin, and fluconazole.

Item Type: Conference or Workshop Item (Paper)
Subjects: Engineering > MIT Manipal > Chemistry
Depositing User: MIT Library
Date Deposited: 27 Jul 2015 11:42
Last Modified: 27 Jul 2015 11:42
URI: http://eprints.manipal.edu/id/eprint/143598

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