Synthesis and anti-inflammatory activities of new cyanopyrane derivatives fused with steroidal nuclei.
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.
Amr
Abdel-Galil E
AG
Organic Chemistry Department, National Research Center, Cairo, Egypt. aamr1963@yahoo.com
Abdulla
Mohamed M
MM
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D011714:Pyrans / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013256:Steroids / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000893:Anti-Inflammatory Agents; D011714:Pyrans; D013256:Steroids