Synthesis and biological evaluation of some hydroxypyrazole derivatives as anti-inflammatory-antimicrobial agents

被引：34
作者：
Bekhit, AA [1 ]
Abdel-Rahman, HM
Guemei, AA
机构：
[1] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21521, Egypt
[2] Assiut Univ, Fac Pharm, Pharmaceut Med Chem Dept, Assiut 71516, Egypt
[3] Univ Alexandria, Fac Med, Dept Pharmacol, Alexandria, Egypt
来源：
ARCHIV DER PHARMAZIE | 2006年 / 339卷 / 02期
关键词：
hydroxypyrazole; anti-inflammatory; antimicrobial; ulcerogenic effect; acute toxicity;
D O I：
10.1002/ardp.200500197
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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-l-trifluoroacetyl-1H-pyrazol-3yl)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.
引用
收藏
页码：81 / 87
页数：7
相关论文
共 24 条
[1]  
ABOUZEITHAR MS, 1982, PHARMAZIE, V37, P593
[2]   N-(5-substituted) thiophene-2-alkylsulfonamides as potent inhibitors of 5-lipoxygenase [J].
Beers, SA ;
Malloy, EA ;
Wu, W ;
Wachter, M ;
Ansell, J ;
Singer, M ;
Steber, M ;
Barbone, A ;
Kirchner, T ;
Ritchie, D ;
Argentieri, D .
BIOORGANIC & MEDICINAL CHEMISTRY, 1997, 5 (04) :779-786
[3]   Novel pyrazole derivatives as potential promising anti-inflammatory antimicrobial agents [J].
Bekhit, AA ;
Ashour, HMA ;
Guemei, AA .
ARCHIV DER PHARMAZIE, 2005, 338 (04) :167-174
[4]   Design, synthesis and biological evaluation of some pyrazole derivatives as anti-inflammatory-antimicrobial agents [J].
Bekhit, AA ;
Abdel-Aziem, T .
BIOORGANIC & MEDICINAL CHEMISTRY, 2004, 12 (08) :1935-1945
[5]   Design and synthesis of some substituted 1H-pyrazolyl-thiazolo[4,5-d]pyrimidines as anti-inflammatory-antimicrobial agents [J].
Bekhit, AA ;
Fahmy, HTY ;
Rostom, SAF ;
Baraka, AM .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2003, 38 (01) :27-36
[6]   Design and synthesis of some substituted 1H-pyrazolyl-oxazolidines or 1H-pyrazolyl-thiazolidines as anti-inflammatory-antimicrobial agents [J].
Bekhit, AA ;
Fahmy, HTY .
ARCHIV DER PHARMAZIE, 2003, 336 (02) :111-118
[7]  
BEKHIT AA, 2004, WORLD C DOS ANT NURN
[8]  
BEKHIT AA, 2003, 2 INT C NEW BIOM MAT
[9]  
BEKHIT AA, 2003, Patent No. 1117
[10]  
BEKHIT AA, 2001, 2 INT C PHARM BIOL S, P34
123