Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents

被引:242
作者
Amir, Mohammad [1 ]
Kumar, Harish [1 ]
Khan, Suroor A. [1 ]
机构
[1] Hamdard Univ, Fac Pharm, Dept Pharmaceut Chem, New Delhi 110062, India
关键词
pyrazoline; anti-inflammatory; analgesic; ulcerogenic; lipid peroxidation;
D O I
10.1016/j.bmcl.2007.12.043
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
A series of 3-(4-biphenyl)-5-substituted phenyl-2-pyrazolines (2a-h) and 1-benzoyl-3-(4-biphenyl)-5-substituted phenyl-2-pyrazolines (3a-h) were synthesized by condensation of chalcones with hydrazine hydrate in solvent system ethanol and DMF. The newly synthesized compounds were screened for their anti-inflammatory and analgesic activity, and were compared with standard drug. Among the compounds studied, compound 2e showed more potent anti-inflammatory and analgesic activity than the standard drug along with minimum ulcerogenic index. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:918 / 922
页数:5
相关论文
共 27 条
[1]
The analgesic effect of the methanolic extract of Acanthus montanus [J].
Adeyemi, OO ;
Okpo, SO ;
Okpaka, O .
JOURNAL OF ETHNOPHARMACOLOGY, 2004, 90 (01) :45-48
[2]
Synthesis and structure -: Activity relationship of a new series of COX-2 selective inhibitors:: 1,5-diarylimidazoles [J].
Almansa, C ;
Alfón, J ;
de Arriba, AF ;
Cavalcanti, FL ;
Escamilla, I ;
Gómez, LA ;
Miralles, A ;
Soliva, R ;
Bartrolí, J ;
Carceller, E ;
Merlos, M ;
García-Rafanell, J .
JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (16) :3463-3475
[3]
Amir M, 2005, INDIAN J CHEM B, V44, P2532
[4]
Anti-inflammatory and gastro sparing activity of some new indomethacin derivatives [J].
Amir, M ;
Kumar, S .
ARCHIV DER PHARMAZIE, 2005, 338 (01) :24-31
[5]
Amir Mohammad, 2007, Acta Pharmaceutica (Zagreb), V57, P31, DOI 10.2478/v10007-007-0003-y
[6]
Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives of naproxen [J].
Amir, Mohammad ;
Kumar, Harish ;
Javed, Sadique A. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (16) :4504-4508
[7]
Inhibitors of cyclooxygenase-2: November 1999-April 2000 [J].
Carter, JS .
EXPERT OPINION ON THERAPEUTIC PATENTS, 2000, 10 (07) :1011-1020
[8]
ROLE OF DIRECT TISSUE CONTACT IN THE PRODUCTION OF GASTRO-INTESTINAL ULCERS BY ANTI-INFLAMMATORY DRUGS IN RATS [J].
CIOLI, V ;
ROSSI, V ;
PUTZOLU, S ;
BARCELLONA, PS ;
CORRADINO, C .
TOXICOLOGY AND APPLIED PHARMACOLOGY, 1979, 50 (02) :283-289
[9]
NOVEL ANTI-INFLAMMATORY AGENTS [J].
CULLEN, E .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1984, 73 (05) :579-589
[10]
Cyclooxygenase inhibitors - current status and future prospects [J].
Dannhardt, G ;
Kiefer, W .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2001, 36 (02) :109-126