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-H₂SO4⁽⁺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 <i>Mycobacterium tuberculosis</i> H37Rv (Resistant strain)) and anti-inflammatory activity (in-vivo assay using Wistar rat). The result showed that derivatives <b>4c</b>, <b>4h</b>, and <b>4m</b> have significant potency against tested <i>M. tuberculosis</i>. However, derivatives <b>4i</b> and <b>4j</b> found significantly active against inflammation. <i>In vitro</i> COX inhibition assay also supported the result in favor of selectivity and efficacy of derivatives.