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- W2078449360 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)(2)O to provide compounds 2. The latter compounds could be N-deprotected by 4N HCl/dioxane to afford the second series 3 or reacted with NH(4)OH 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 margin and no ulcerogenic effect." @default.
- W2078449360 created "2016-06-24" @default.
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- W2078449360 date "2003-04-01" @default.
- W2078449360 modified "2023-10-16" @default.
- W2078449360 title "Design and Synthesis of Some Substituted 1H-Pyrazolyl-oxazolidines or 1H-Pyrazolyl-thiazolidines as Anti-inflammatory-Antimicrobial Agents" @default.
- W2078449360 doi "https://doi.org/10.1002/ardp.200390007" @default.
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