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Design, synthesis and biological evaluation of benzoxazolinone-containing 1,3,4-thiadiazoles as TNF-? inhibitors.

ABSTRACT: A library of nineteen benzoxazolinone-based 1,3,4-thiadiazoles has been synthesized and screened for their anti-inflammatory activity. The compound 1f exhibited a potent anti-inflammatory activity with an inhibition of 65.83% and 32.50% after 3 h and 5 h respectively. It also exhibited a significant in vitro (p < 0.01), TNF- ? inhibitory activity with 51.44 % inhibition. The compound 1f showed hydrogen bonding with GLN 61 and interactions with TYR 119, TYR 151 and GLY 121. The histopathology report showed that none of the compounds caused gastric ulceration. The results from the in vivo & in vitro antiinflammatory activity along with In Silico studies exhibit that benzoxazolinone-based 1,3,4-thiadiazoles may be used in the future development of anti-inflammatory drugs.

SUBMITTER: Haider S 

PROVIDER: S-EPMC6479203 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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Design, synthesis and biological evaluation of benzoxazolinone-containing 1,3,4-thiadiazoles as TNF-α inhibitors.

Haider Saqlain S   Alam Mohammad Sarwar MS   Hamid Hinna H   Dhulap Abhijeet A   Kumar Deepak D  

Heliyon 20190422 4

A library of nineteen benzoxazolinone-based 1,3,4-thiadiazoles has been synthesized and screened for their anti-inflammatory activity. The compound <b>1f</b> exhibited a potent anti-inflammatory activity with an inhibition of 65.83% and 32.50% after 3 h and 5 h respectively. It also exhibited a significant <i>in vitro</i> (p < 0.01), TNF- α inhibitory activity with 51.44 % inhibition. The compound <b>1f</b> showed hydrogen bonding with GLN 61 and interactions with TYR 119, TYR 151 and GLY 121. T  ...[more]

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