Synthesis and Anti‐inflammatory Activities of New Cyanopyrane Derivatives Fused with Steroidal Nuclei

Abstract

Thirteen new heterocyclic derivatives containing a cyanopyrane ring fused to a steroidal moiety were conveniently synthesized and screened for their anti-inflammatory potencies comparable to that of the glucocorticoid prednisolone. Four compounds 5a, 5b, 6b, and 8 exhibited superior anti-inflammatory indices (in rats, protection against carrageenan induced edema and inhibition of plasma PGE). All the candidates were less toxic than the reference drug concerning LD(50) values. Synthetic steroidal structures fused to a substituted cyanopyrane ring seem to be a promising approach in search for novel leads for potent anti-inflammatory agents.