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Abstract

Synthesis, structure activity relationship studies and pharmacological evaluation of 2-phenyl-3-(substituted phenyl)-3h-quinazolin-4-ones as serotonin 5-ht 2 antagonists

Author(s): N Sati1, S Kumar2, M. S. M Rawat3
1 Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar Garhwal-246 174, India 2 College of Pharmacy, IFTM, Lodipur-Raipur, Delhi Road, Moradabad-244 001, India 3 Department of Chemistry, H. N. B. Garhwal University, Srinagar Garhwal-246 174, India

Correspondence Address:
N Sati Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar Garhwal-246 174 India [email protected]


Benzoyl chloride was added to the solution of anthranilic acid in pyridine to afford crude 2-phenyl-benzo[d][1, 3] oxazin-4-one (1). To the solution of compound 1 in dry toluene, various substituted anilines were added and the mixture refluxed for 8 h to afford 2-phenyl-3-(substituted phenyl)-3H-quinazolin-4-ones (2a-2f). All the compounds were obtained in solid state in yields varying between 40 to 70%. Spectral characterization included FTIR, 1 H NMR and Electrospray MS. The synthesized compounds were screened for 5-HT 2 antagonist activity. Some of the title compounds have been found to show significant 5-HT 2 antagonist activity. The compound 2b, 3-(2-chlorophenyl)-2-phenyl-3H-quinazolin-4-one was the most potent derivative in the series of compound synthesized.

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