Synthesis And Anagesic activities of Quinazolin-4(3H)-One, 2-Methyl-4(3H)-Quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one

  • P.O. Osarumwense Department of Chemical Sciences, Ondo State University of Sciences and Technology, Okitipupa, Ondo State, Nigeria
  • M.O. Edema Provost Office, College of Education, Warri, Delta State, Nigeria
  • C.O. Usifoh Faculty of Pharmaceutical Chemistry, University of Benin, Benin City, Nigeria

Abstract

Background: Objective: The current study is aimed at the synthesis of these quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their analgesic activity. Method: The condensation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride yielded the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which further produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate The quinazolinone derivatives quinazolin-4(3H)-One,  2-Methyl-4(3H)-quinazolinone  and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were unequivocally confirmed by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis.The synthesized compounds were screened for their analgesic activity.Compounds 1,2 and 3 showed significant analgesic activity. Discussion: Compound 1 was characterized by the absence of methyl group and the presence of methyl group for compound 2. The test investigated compounds exhibited significant analgesic activity when compared with the control test sample. The compounds  synthesized  exhibited promising analgesic  activities against .  Conclusion: The compounds have high analgesic activity. Compound 3 has a higher activity  compared to Compound 2 and compound 2 has a higher analgesic activity compared to compound  1.  Compound 3 has a higher analgesic activity compared to the standard drugs Aspirin and Indomethacin.


Keywords:  quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one quinazolin-4(3H)-one, analgesic activity.

Keywords: quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one quinazolin-4(3H)-one, analgesic activity

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Author Biographies

P.O. Osarumwense, Department of Chemical Sciences, Ondo State University of Sciences and Technology, Okitipupa, Ondo State, Nigeria

Department of Chemical Sciences, Ondo State University of Sciences and Technology, Okitipupa, Ondo State, Nigeria

M.O. Edema, Provost Office, College of Education, Warri, Delta State, Nigeria

Provost Office, College of Education, Warri, Delta State, Nigeria

C.O. Usifoh, Faculty of Pharmaceutical Chemistry, University of Benin, Benin City, Nigeria

Faculty of Pharmaceutical Chemistry, University of Benin, Benin City, Nigeria

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Osarumwense P, Edema M, Usifoh C. Synthesis And Anagesic activities of Quinazolin-4(3H)-One, 2-Methyl-4(3H)-Quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one. JDDT [Internet]. 15Aug.2020 [cited 18May2021];10(4-s):87-1. Available from: https://jddtonline.info/index.php/jddt/article/view/4209