Design, Synthesis, Anti-Inflammatory And Analgesic Studies Of Novel 1,3,4- Oxadiazole-Thione Derivatives

Abstract

A set of novel 1,3,4-oxadiazole based derivatives (5a-n) were synthesized through a series of reactions including cyclization of hydrazides. The structure of new compounds was supported by 1H NMR, 13C NMR and MS data. The analgesic and anti-inflammatory activities of the synthesized compounds were evaluated using writhing assays and carrageenan-induced rat paw edema respectively. Majority of the tested compounds exhibited both analgesic and anti-inflammatory activities, particularly compounds 5d and 5m showed a comparable effect to a well-known analgesic and anti-inflammatory drug Ibuprofen. Compound 5j showed best anti-inflammatory activity.

1,3,4-Oxadiazole Contained Sesquiterpene Derivatives: Synthesis and Microbiocidal Activity for Plant Disease

“…Among them, 1,3,4-oxadiazole is a kind of heterocyclic compound with a variety of biological activities, and its derivatives show antiviral ( Gan et al, 2017 ; He et al, 2021 ), antibacterial ( Vasantha et al, 2019 ; Yu et al, 2021 ; Wang S. et al, 2021 ), antifungal ( Wen et al, 2019 ; Wang X. et al, 2021 ) and insecticidal activity ( Yang et al, 2020 ) in agricultural applications. Some also proved to be attractive anti-cancer ( Kumar et al, 2009 ), anti-depressant ( Ergun et al, 2010 ), anti-HIV ( Parizadeh et al, 2018 ), and anti-inflammatory ( Naseer et al, 2019 ) medicines. Additionally, the presence of alkyl groups on the oxadiazole nucleus increases their ability to penetrate active sites and enhance their biological activity ( Vasantha et al, 2019 ).…”