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Synthesis and pharmacological evaluation of 3‐(4‐chloro phenyl)‐2‐substituted‐3H‐quinazolin‐4‐ones as analgesic and anti‐inflammatory agents
Authors:V Alagarsamy  S Meena  KV Ramseshu  V Raja Solomon  K Thirumurugan
Institution:1. Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Fasalwadi, Sangareddy, A.P. State, India;2. Department of Pharmaceutical Chemistry, K.M. College of Pharmacy, Madurai, India;3. Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow, India
Abstract:A new series of 3‐(4‐chloro phenyl)‐2‐substituted‐3H‐quinazolin‐4‐ones were synthesized by reacting the amino group of 2‐hydrazino‐3‐(4‐chloro phenyl)‐3H‐quinazolin‐4‐one with different aldehydes and ketones. The compounds were investigated for their analgesic activity in albino mice, and for their anti‐inflammatory and ulcerogenic activities in Wistar rats. All test compounds exhibited analgesic and anti‐inflammatory activities. Compound VA2 (2‐(1‐ethylpropylidene‐hydrazino)‐3‐(4‐chloro phenyl)‐3H‐quinazolin‐4‐one) showed moderately more potent analgesic activity and compound VA3 (2‐(1‐methylbutylidene‐hydrazino)‐3‐(4‐chlorophenyl)‐3H‐quinazolin‐4‐one) showed moderately more potent anti‐inflammatory activity when compared with the reference standard, diclofenac sodium. The test compounds showed only mild ulcerogenic side effects when compared with aspirin. Drug Dev Res 69: 226–233, 2008 ©2008 Wiley‐Liss, Inc.
Keywords:quinazolin‐4‐ones  analgesic  anti‐inflammatory activity
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