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Veerachamy Alagarsamy, Kunchu Kavitha, Mani Rupeshkumar, Viswas Solomon, Jaya Kumar, Dinakaran Kumar and Hemant Sharma

Synthesis and pharmacological investigation of novel 4-(3-ethylphenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a] quinazolin-5-ones as a new class of H1-antihistaminic agents

A series of novel 4-(3-ethylphenyl)-1-substituted-4H-[1,2,4] triazolo[4,3-a]quinazolin-5-ones (4a-j) were synthesized by the cyclization of 3-(3-ethylphenyl)-2-hydrazino-3H-quinazolin-4-one (3) with various one-carbon donors. The starting material, compound 3, was synthesized from 3-ethyl aniline by a new innovative route with improved yield. When tested for their in vivo H1-antihistaminic activity on conscious guinea pigs, all test compounds protected the animals from histamine induced bronchospasm significantly. Compound 4-(3-ethylphenyl)-1-methyl-4H - [1,2,4]triazolo[4,3-a]quinazolin-5-one (4b) emerged as the most active compound of the series and it is more potent (74.6 % protection) compared to the reference standard chlorpheniramine maleate (71 % protection). Compound 4b shows negligible sedation (10 %) compared to chlorpheniramine maleate (30 %). Therefore compound 4b can serve as the leading compound for further development of a new class of H1-antihistamines.

Open access

Neeraj Sharma, Hemant Batra, Manjula Mehta and Jagdish Chander

Abstract

In the maxillofacial skeleton, chronic osteomyelitis is more often observed in the mandible than maxilla. Maxillary osteomyelitis is rare because of its rich blood supply. It is usually seen in individuals with impaired immune response, uncontrolled diabetes and hospitalized patients. It can be caused by bacterial, fungal or viral infections. We report a rare case of maxillary osteomyelitis caused by an emerging mucormycete, Apophysomyces variabilis.