Osarumwense Peter Osarodion
Ondo State University of Science and Techonology Okitipupa,Nigeria
Abstract Title:Synthesis, antibacterial activity of 3-amino 5-methoxyl-2-methyl quinazolin-4(3H)-one an amino-6- methoxyl-2-methyl of 4H–benzo[d] [1,3]–oxazine–4–one
Biography:
DR. OSARUMWENSE PETER OSARODION has completed his PhD at the age of 35 years from the University of Benin, Benin City, Edo State, Nigeria. He is the Lecturer of Ondo State University of Science and Technology, Ondo State, Nigeria a premier University. He has published more than 40 papers in reputed journals and has been serving as an editorial board member of repute. I am interested in synthesis of novel Heterocyclic compounds and to determine their antibacterial, activity. Thank you. DR. OSARUMWENSE PETER OSARODION.
Research Interest:
Introduction: The rapid a d appearance of antibiotic resistant strains t ns today and m nd misuse of antibiotics and more Quinazolinone ring sy ng system was rewarded as a s a promising m ng molecule because of its br s broad spectrum of biological activities like anti-histaminic[1], a , anticancer [2,3], anti-HIV [4], anti-inflammatory,[5]analgesic, [6] anti-diabetic [7], anti-bacterial [8], antifungal [9], anti- oxidant [10], a , anti-tubercular [11], anti-convulsant[12]. Objectives: These objectives of this st s study w udy was to e o eliminate the current challenges by syn by synthesizing these novel antibacterial quinazolinone derivatives with a h a high a gh antibacterial potential. Methods: The condensation of 2-amino-methyl-5-dimethoxybenzoate with acetic anhydride yielded the cyclic compound 2-methyl-5-substituted-1,3-benzo-oxazine-4-one which further produced a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate. 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 w pounds were screened against various st ous strains of microorganism; Staphylococcus aureus, Bacillus spe s species, Escherichia coli, Klebsiella pne a pneumonia, Serratia marcescens, and candida al da albicans. Results: Compounds 1 a pounds 1 a pounds 1 and 2 show nd 2 show nd 2 showed significant activity a y against Staphylococcus aureusand Se usand Serratia marcescenswith MI h MIC ranging f ng from 6 – 12 m 6 – 12 m 6 – 12 m 6 – 12 mg/mL. Discussion: Compound 1 displayed a singlet signal at: δ 3.78 attributed to methoxyl group and singlet at δ 3.68 which was due to methyl group. Also, 1H NMR spectrum of compound 2 showed a characteristic signal at δ 2.56 (singlet) corresponding to methyl group and duplet at: δ 3.90 for methoxy group. For the IR spectra, Compound 1 was characterized by absence of v NH2and presence of v C-O stretch in 1101cm-1 region of the compound. Compound 2 showed the highest antibacterial activity at 16 mm compared to compound 1 and Ciprofloxicin (CPX) for bacteria, Ketonaxol (PEF). The compounds synthesized had a higher activity than Ciprofloxicin (CPX) for bacteria, Ketonaxol (PEF) for fungus, a standard antibacterial drug. Conclusion: Compound 2 had a higher antibacterial activity than Compound 1. The compounds synthesized had a higher activity than Ciprofloxicin (CPX) for bacteria, Ketonaxol (PEF) for fungus, a standard antibacterial drug.