Bekhit Adnan A, Abdel-Rahman Hamdy M, Guemei Aida A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.
Arch Pharm (Weinheim). 2006 Feb;339(2):81-7. doi: 10.1002/ardp.200500197.
Some hydroxypyrazole derivatives 2-7 were synthesized by cyclocondensation of the keto-ester 1 with hydrazines hydrate or substituted hydrazines followed by reduction and acylation with acetic anhydride or trifluoroacetic anhydride. The newly synthesized compounds were evaluated for their anti-inflammatory, antimicrobial activities. In addition, the ulcerogenic and acute toxicity profiles were determined. Compounds N-(4-(5-hydroxy-1-trifluoroacetyl-1H-pyrazol-3-yl)phenyl) trifluoroacetamide 4b, 3-(4-nitrophenyl)-1-(4-methoxyphenyl)-1H-pyrazol-5-ol 5b, and N-(4-(5-hydroxy-1-methyl-1H-pyrazol-3-yl)phenyl)trifluoroacetamide 7b were proved to be the most active anti-inflammatory, antimicrobial agents in the present study with a good safety margin and minimal or no ulcerogenic effect.
通过酮酯1与水合肼或取代肼进行环缩合反应，随后用乙酸酐或三氟乙酸酐进行还原和酰化反应，合成了一些羟基吡唑衍生物2 - 7。对新合成的化合物进行了抗炎、抗菌活性评估。此外，还测定了它们的致溃疡和急性毒性情况。在本研究中，化合物N-(4-(5-羟基-1-三氟乙酰基-1H-吡唑-3-基)苯基)三氟乙酰胺4b、3-(4-硝基苯基)-1-(4-甲氧基苯基)-1H-吡唑-5-醇5b和N-(4-(5-羟基-1-甲基-1H-吡唑-3-基)苯基)三氟乙酰胺7b被证明是活性最强的抗炎、抗菌剂，具有良好的安全范围且致溃疡作用极小或无致溃疡作用。
