Acta Pharm. 59 (2009) 75-88

full paper

Short communication

 

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

VEERACHAMY ALAGARSAMY, DURAIRAJ SHANKAR, VISWAS RAJA SOLOMON, RAJENDRA VASANT SHEOREY AND PERIYASAMY PARTHIBAN

drvalagarsamy@gmail.com

1 Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy-502294, India
2 Department of Pharmacy (CARISM), SASTRA University, Tirumalaisamudram, Thanjavur-613 402, India
3 Medicinal & Process Chemistry Division, Central Drug Research Institute, Lucknow-226001, India
4 Department of Pharmacology, Institute of Pharmacy, Raipur Institute of Technology Raipur-492001, India

Accepted January 15, 2009

 

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.

 

Keywords: quinazolin-4(3H)-one, analgesic activity, anti-inflammatory activity, ulcerogenicity