Display options
Cite
Sati N, Kumar S, Rawat MS. Synthesis, Structure Activity Relationship Studies and Pharmacological Evaluation of 2-Phenyl-3-(Substituted Phenyl)-3H-Quinazolin-4-ones as Serotonin 5-HT(2) Antagonists. Indian J Pharm Sci. 2009;71(5):572-5doi: 10.4103/0250-474X.58185.
Sati, N., Kumar, S., & Rawat, M. S. (2009). Synthesis, Structure Activity Relationship Studies and Pharmacological Evaluation of 2-Phenyl-3-(Substituted Phenyl)-3H-Quinazolin-4-ones as Serotonin 5-HT(2) Antagonists. Indian journal of pharmaceutical sciences, 71(5), 572-5. https://doi.org/10.4103/0250-474X.58185
Sati, N, et al. "Synthesis, Structure Activity Relationship Studies and Pharmacological Evaluation of 2-Phenyl-3-(Substituted Phenyl)-3H-Quinazolin-4-ones as Serotonin 5-HT(2) Antagonists." Indian journal of pharmaceutical sciences vol. 71,5 (2009): 572-5. doi: https://doi.org/10.4103/0250-474X.58185
Sati N, Kumar S, Rawat MS. Synthesis, Structure Activity Relationship Studies and Pharmacological Evaluation of 2-Phenyl-3-(Substituted Phenyl)-3H-Quinazolin-4-ones as Serotonin 5-HT(2) Antagonists. Indian J Pharm Sci. 2009 Sep;71(5):572-5. doi: 10.4103/0250-474X.58185. PMID: 20502582; PMCID: PMC2866355.
Copy Download .nbib Format: NLM
Share it on

Indian J Pharm Sci. 2009 Sep;71(5):572-5. doi: 10.4103/0250-474X.58185.

Synthesis, Structure Activity Relationship Studies and Pharmacological Evaluation of 2-Phenyl-3-(Substituted Phenyl)-3H-Quinazolin-4-ones as Serotonin 5-HT(2) Antagonists.

Indian journal of pharmaceutical sciences

N Sati, S Kumar, M S M Rawat

Affiliations

  1. Department of Pharmaceutical Sciences, H. N. B. Garhwal University, Srinagar Garhwal-246 174, India.

PMID: 20502582 PMCID: PMC2866355 DOI: 10.4103/0250-474X.58185

Abstract

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.

Keywords: 5-HT2 antagonists; aryl quinazolines; quinazolin-4-ones; serotonin antagonists

References

  1. Psychopharmacology (Berl). 1988;96(3):395-9 - PubMed
  2. J Med Chem. 1992 Dec 25;35(26):4903-10 - PubMed
  3. Psychopharmacology (Berl). 1985;86(1-2):45-54 - PubMed
  4. J Med Chem. 2003 Jan 2;46(1):138-47 - PubMed
  5. J Med Chem. 2006 Feb 23;49(4):1494-8 - PubMed
  6. J Med Chem. 1992 Dec 25;35(26):4823-31 - PubMed
  7. J Med Chem. 1984 Feb;27(2):190-5 - PubMed
  8. Pharmacopsychiatry. 1985 Sep;18(5):303-5 - PubMed
  9. J Med Chem. 1992 Dec 25;35(26):4893-902 - PubMed
  10. J Med Chem. 1995 Mar 31;38(7):1119-31 - PubMed
  11. J Pharmacol Exp Ther. 1989 Jul;250(1):52-9 - PubMed

Publication Types