Silica catalyzed one pot synthesis of hybrid thiazolidin-4-one derivatives as anti-tubercular and anti-inflammatory agent by attenuating COX-2 pathway

A novel series of a hybrid class of hybrid thiazolidin-4-one derivatives were designed and synthesized through one-pot catalytic synthesis. The reaction was catalyzed in the presence of silica-H 2 SO4 (+6) . The derivatives computational ADMET profile was calculated. The study shows that most active derivatives have optimal logP, higher anti-inflammatory activity score, and poor metabolism at the sight of P450-3A4 and 2D6. The entire series of derivatives were further evaluated for anti-tubercular (against Mycobacterium tuberculosis H37Rv (Resistant strain)) and anti-inflammatory activity (in-vivo assay using Wistar rat). The result showed that derivatives 4c , 4h , and 4m have significant potency against tested M. tuberculosis . However, derivatives 4i and 4j found significantly active against inflammation. In vitro COX inhibition assay also supported the result in favor of selectivity and efficacy of derivatives.