A. Bekhit, H. Fahmy
Apr 1, 2003
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0
Influential Citations
61
Citations
Journal
Archiv der Pharmazie
Abstract
Four series of 1 H‐pyrazole derivatives have been synthesized. The first series was synthesized starting with the reaction of 3‐(5‐bromo‐2‐thienyl)‐1‐phenyl‐1 H‐pyrazole‐4‐carboxaldehyde 1 with L‐serine, L‐cysteine, or L‐penicillamine, followed by N‐protection using (Boc)2O to provide compounds 2. The latter compounds could be N‐deprotected by 4N HCl/dioxane to afford the second series 3 orreactedwith NH4OH in the presence of DCC/HOBt to give the corresponding amides 4 followed by N‐deprotection giving rise to compounds 5. The newly synthesized compounds were evaluated for their anti‐inflammatory‐antimicrobial activities. In addition, the ulcerogenic and acute toxicity profiles were determined. Compound 5b (2RS, 4R)‐2‐[3‐(5‐bromo‐2‐thienyl)‐1‐phenyl‐1H‐pyrazol‐4‐yl]‐5‐methylthiazolidine‐4‐carboxamide, proved to be the most active anti‐inflammatory‐antimicrobial agent in the present study with a good safety margine and no ulcerogenic effect.