612500-40-0Relevant articles and documents
Design and synthesis of some substituted 1H-pyrazolyl-oxazolidines or 1H-pyrazolyl-thiazolidines as anti-inflammatory-antimicrobial agents
Bekhit, Adnan A.,Fahmy, Hesham T.Y.
, p. 111 - 118 (2003)
Four series of 1H-pyrazole derivatives have been synthesized. The first series was synthesized starting with the reaction of 3-(5-bromo-2-thienyl)-1 -phenyl-1H-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, or reacted with 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 5 b, (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.
