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作为新型抗炎和镇痛药的吡唑啉衍生物的合成及药理评价

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

作者信息

Amir Mohammad, Kumar Harish, Khan Suroor A

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi 110 062, India.

出版信息

Bioorg Med Chem Lett. 2008 Feb 1;18(3):918-22. doi: 10.1016/j.bmcl.2007.12.043. Epub 2008 Jan 7.

Abstract

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.

摘要

通过在乙醇和N,N-二甲基甲酰胺溶剂体系中,将查尔酮与水合肼缩合,合成了一系列3-(4-联苯基)-5-取代苯基-2-吡唑啉(2a-h)和1-苯甲酰基-3-(4-联苯基)-5-取代苯基-2-吡唑啉(3a-h)。对新合成的化合物进行抗炎和镇痛活性筛选,并与标准药物进行比较。在所研究的化合物中,化合物2e表现出比标准药物更强的抗炎和镇痛活性,同时致溃疡指数最低。

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