Design, synthesis, and pharmacological evaluation of novel oxadiazole and oxadiazoline analogs as anti-inflammatory agents.
Two novel series of oxadiazole and oxadiazoline analogs possessing an indole nucleus were synthesized for their potential anti-inflammatory activity. The structures of the compounds were elucidated by elemental and spectral (IR, (1)H-NMR, (13)C-NMR, and MS) analysis. Most of the test compounds demonstrated appreciable anti-inflammatory activities. The anti-inflammatory activity of oxadiazoles at doses of 100 mg/kg was shown by their ability to provide 27-66%, 14-32%, and 20-51%. protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. On the other hand, the anti-inflammatory properties of oxadiazolines at doses of 100 mg/kg were reflected by their ability to provide 20-56%, 11-26%, and 25-47% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. The ulcerogenic potential of the compounds was determined. Structure-activity relationships among synthesized compounds were also established.
Medicinal Chemistry Division, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur, India. harishdops@yahoo.co.in
Harish
H
Rajak
Ravichandran
R
Veerasamy
Murlidhar
M
Kharya
Pradeep
P
Mishra
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy / Q000517:prevention & control; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D014456:Ulcer / Q000139:chemically induced
D000893:Anti-Inflammatory Agents; D010069:Oxadiazoles