Anti-inflammatory profile of some synthesized heterocyclic pyridone and pyridine derivatives fused with steroidal structure.
We herein report the anti-inflammatory activity of some newly synthesized heterocyclic pyridone and pyridine derivatives fused with steroidal structure. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All compounds, except 3b, 22, and 23, were interestingly less toxic than the reference drug (Prednisolone). Regarding the protection against Carrageenan-induced edema, eight compounds were found to be more potent than Prednisolone. On the other hand, in searching for COX-2 inhibitor, the inhibition of plasma PGE2 for the compounds was determined and four compounds were found to be more potent than the reference drug. The structure assignment of the new compounds was based on chemical and spectroscopic evidence.
Amr
Abdel-Galil E
AG
Applied Organic Chemistry Department, National Research Center, Cairo, Dokki, Egypt. aamr1963@yahoo.com
Abdulla
Mohamed M
MM
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002351:Carrageenan / Q000633:toxicity; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007928:Lethal Dose 50; D008297:Male; D011725:Pyridines / Q000737:chemistry*; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry*; D051381:Rats; D011919:Rats, Inbred Strains; D013256:Steroids / Q000737:chemistry*; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D052246:Cyclooxygenase 2 Inhibitors; D006571:Heterocyclic Compounds; D011725:Pyridines; D011728:Pyridones; D013256:Steroids; D002351:Carrageenan; C023666:pyridine