4-dialkylamino-1-(5-substituted or unsubstituted 1-phenyl-1H-pyrazol-4-yl)butan-1-ols:: synthesis and evaluation of analgesic, anti-inflammatory and platelet anti-aggregating activities

被引:7
作者
Menozzi, G
Mosti, L
Merello, L
Piana, A
Armani, U
Ghia, M
Angiola, M
Mattioli, F
机构
[1] Univ Genoa, Dipartimento Sci Farmaceut, I-16132 Genoa, Italy
[2] Univ Genoa, Ctr Ric Trombosi, Dipartimento Med Interna, I-16132 Genoa, Italy
[3] Univ Genoa, Sez Farmacol, Dipartimento Med Interna, I-16132 Genoa, Italy
[4] Univ Genoa, Tossicol Clin, I-16132 Genoa, Italy
来源
FARMACO | 2000年 / 55卷 / 03期
关键词
pyrazole derivatives; anti-inflammatory agents; analgesic agents; platelet anti-aggregating agents;
D O I
10.1016/S0014-827X(00)00007-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A number of 4-dialkylamino-1-(5-substituted or unsubstituted 1-phenyl-1H-pyrazol-4-yl)butan-1-ols 2a-n were synthesized and tested in vivo for anti-inflammatory and analgesic activities and in vitro for platelet anti-aggregating activity. Dimethyl-aminoderivatives 2b, e, g showed good analgesic activity; almost all of them had strong platelet anti-aggregating properties at a final concentration of 1 x 10(-3) M; pyrazoles 2c, d, f-h showed weak anti-inflammatory activity. (C) 2000 Elsevier Science S.A. All rights reserved.
引用
收藏
页码:219 / 226
页数:8
相关论文
共 15 条
[1]  
ARYA VP, 1973, Patent No. 3778443
[2]   AGGREGATION OF BLOOD PLATELETS BY ADENOSINE DIPHOSPHATE AND ITS REVERSAL [J].
BORN, GVR .
NATURE, 1962, 194 (4832) :927-&
[3]  
EDDY NB, 1950, J PHARMACOL EXP THER, V98, P121
[4]   THE PREPARATION AND PROPERTIES OF SOME DERIVATIVES OF 1-PHENYLPYRAZOLE [J].
FINAR, IL ;
GODFREY, KE .
JOURNAL OF THE CHEMICAL SOCIETY, 1954, (JUL) :2293-2298
[5]  
FINAR IL, 1957, J CHEM SOC, P3314
[6]  
KOSTER R, 1959, FED PROC, V18, P412
[7]   Cyclooxygenase 2 inhibitors: discovery, selectivity and the future [J].
Marnett, LJ ;
Kalgutkar, AS .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1999, 20 (11) :465-469
[8]   SYNTHESIS OF 5-SUBSTITUTED 1-ARYL-1H-PYRAZOLE-4-ACETONITRILES, 4-METHYL-1-PHENYL-1H-PYRAZOLE-3-CARBONITRILES AND PHARMACOLOGICALLY ACTIVE 1-ARYL-1H-PYRAZOLE-4-ACETIC ACIDS [J].
MENOZZI, G ;
SCHENONE, P ;
MOSTI, L ;
MATTIOLI, F .
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1993, 30 (04) :997-1002
[9]   omega-Dialkylaminoalkyl ethers of phenyl-(5-substituted 1-phenyl-1H-pyrazol-4-yl)methanols with analgesic and anti-inflammatory activity [J].
Menozzi, G ;
Mosti, L ;
Fossa, P ;
Mattioli, F ;
Ghia, M .
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1997, 34 (03) :963-968
[10]  
MENOZZI G, 1994, FARMACO, V49, P115