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合成取代的吖啶基吡唑啉衍生物及其抗炎活性评价。

Synthesis of substituted acridinyl pyrazoline derivatives and their evaluation for anti-inflammatory activity.

机构信息

Medicinal Chemistry Division, Department of Pharmacology, L.L.R.M. Medical College, Meerut (U.P.)-250004, India.

出版信息

Eur J Med Chem. 2010 May;45(5):1772-6. doi: 10.1016/j.ejmech.2010.01.009. Epub 2010 Jan 15.

DOI:10.1016/j.ejmech.2010.01.009
PMID:20149499
Abstract

A rapid preparation of compounds (1-24), with the objective of discovering novel and potent anti-inflammatory agent. All the compounds exhibited anti-inflammatory and analgesic activities at the dose 50 mg/kg p.o. The compound 1-(2',4'-Chloroacridine-9'-yl)-3-(5'-pyridine-4-yl)-(1,3,4-oxadiazol-2-yl-thiomethyl)-pyrazole-5-one 24 showed better anti-inflammatory and analgesic activities at the three graded dose of 25, 50 and 100 mg/kg p.o.

摘要

一种快速制备化合物（1-24）的方法，旨在发现新型强效抗炎剂。所有化合物在 50mg/kg 口服剂量下均表现出抗炎和镇痛活性。化合物 1-(2',4'-氯吖啶-9'-基)-3-(5'-吡啶-4-基)-(1,3,4-恶二唑-2-基-硫代甲基)-吡唑-5-酮 24 在 25、50 和 100mg/kg 口服三个不同剂量下表现出更好的抗炎和镇痛活性。

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