<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>A series of novel 3-cyclohexyl-2-substituted hydrazino-quinazolin-4(3<italic>H</italic>)-ones were synthesized by reacting the amino group of 3-cyclohexyl-2-hydrazino quinazolin-4(3<italic>H</italic>)-one with a variety of aldehydes and ketones. The starting material, 3-cyclohexyl-2-hydrazino quinazolin-4(3<italic>H</italic>)-one, was synthesized from cyclohexyl amine. Title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic behavior. The compound 3-cyclohexyl-2-(1-methylbutylidene-hydrazino)-3<italic>H</italic>-quinazolin-4-one (<bold>4c</bold>) emerged as the most active compound of the series and is moderately more potent in its analgesic and anti-inflammatory activities compared to the reference standard diclofenac sodium. Interestingly, test compounds showed only mild ulcerogenic potential when compared to acetylsalicylic acid.</p></abstract>

A series of novel 3-cyclohexyl-2-substituted hydrazino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 3-cyclohexyl-2-hydrazino quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material, 3-cyclohexyl-2-hydrazino quinazolin-4(3H)-one, was synthesized from cyclohexyl amine. Title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic behavior. The compound 3-cyclohexyl-2-(1-methylbutylidene-hydrazino)-3H-quinazolin-4-one (4c) emerged as the most active compound of the series and is moderately more potent in its analgesic and anti-inflammatory activities compared to the reference standard diclofenac sodium. Interestingly, test compounds showed only mild ulcerogenic potential when compared to acetylsalicylic acid.

Synthesis and pharmacological evaluation of 3-cyclohexyl-2-substituted hydrazino-3<italic>H</italic>-quinazolin-4-ones as analgesic and anti-inflammatory agents

Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy-502294, India

Department of Pharmacy (CARISM), SASTRA University, Tirumalaisamudram Thanjavur-613402, India

Medicinal & Process Chemistry Division, Central Drug Research Institute, Lucknow-226001, India

Department of Pharmacology Institute of Pharmacy, Raipur Institute of Technology, Raipur-492001, India

Acta Pharmaceutica

Synthesis and pharmacological evaluation of 3-cyclohexyl-2-substituted hydrazino-3-quinazolin-4-ones as analgesic and anti-inflammatory agents

A series of novel 3-cyclohexyl-2-substituted hydrazino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 3-cyclohexyl-2-hydrazino...

Synthesis and pharmacological evaluation of 3-cyclohexyl-2-substituted hydrazino-3H-quinazolin-4-ones as analgesic and anti-inflammatory agents

Publié en ligne: 20 mars 2009

Pages: 75 - 88

DOI: https://doi.org/10.2478/v10007-009-0004-0

Mots clés
kinazolin-4(3H)-on, analgetsko djelovanje, protuupalno djelovanje, ulcerogenost

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