compound 10b (pyrrolo[3,4-d]pyridazinone derivative)

Compound 10b is a novel synthetic small molecule hybrid consisting of a pyrrolo[3,4-d]pyridazinone scaffold and a 1,3,4-oxadiazole-2-thione ring. Developed by researchers at Wroclaw Medical University in Poland, it acts as a dual inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), enzymes also known as prostaglandin G/H synthase 1 and 2. The 1,3,4-oxadiazole-2-thione moiety serves as a bioisostere for the carboxylic acid group typically found in traditional nonsteroidal anti-inflammatory drugs (NSAIDs). In preclinical rodent models, compound 10b has demonstrated significant antinociceptive and anti-inflammatory effects, reducing levels of inflammatory mediators such as prostaglandin E2 (PGE2) and TNF-α. Notably, it exhibits a favorable safety profile, appearing to lack the gastrointestinal toxicity commonly associated with traditional NSAIDs, and has shown efficacy in models of pain, paw edema, and TNBS-induced colitis.

Other names

6-butyl-3,5,7-trimethyl-1-[[4-[[4-(4-nitrophenyl)piperazin-1-yl]methyl]-5-thioxo-1,3,4-oxadiazol-2-yl]methoxy]pyrrolo[3,4-d]pyridazin-4-onepyrrolo[3,4-d]pyridazinone-1,3,4-oxadiazole hybrid 10b