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3‐(3‐Ethylphenyl)‐2‐substituted hydrazino‐3H‐quinazolin‐4‐one Derivatives: New Class of Analgesic and Anti‐Inflammatory Agents
Authors:V Alagarsamy  V Raja Solomon  R V Sheorey  R Jayakumar
Institution:1. Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Fasalwadi, Sangareddy‐502 294, AP, India;2. Medicinal & Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, UP, India;3. Department of Pharmacology, Institute of Pharmacy, Raipur Institute of Technology, Mandir Hasaud, Raipur 492 101, MP, India
Abstract:A new series of 3‐(3‐ethylphenyl)‐2‐substituted hydrazino‐3H‐quinazolin‐4‐ones were synthesized by reacting the amino group of 2‐hydrazino‐3‐(3‐ethylphenyl)‐3H‐quinazolin‐4‐one with a variety of aldehydes and ketones. The title compounds were investigated for analgesic, anti‐inflammatory and ulcerogenic index behavior. The compound 2‐(N′‐3‐pentylidene‐hydrazino)‐3‐(3‐ethylphenyl)‐3H‐quinazolin‐4‐one ( AS2 ) emerged as the most active compound in exhibiting analgesic activity and the compound 2‐(N′‐2‐pentylidene‐hydrazino)‐3‐(3‐ethylphenyl)‐3H‐quinazolin‐4‐one ( AS3 ) emerged as the most active compound in exhibiting anti‐inflammatory activity; and these compounds are moderately potent when compared with the reference standard diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential when compared with aspirin.
Keywords:analgesic  anti‐inflammatory activity  quinazoline  structure–  activity relationship
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