title: Synthesis, Antimicrobial and Anti-inflammatory Activity of Some New Benzoxazinone and Quinazolinone Candidates.
abstract: Benzoxazinones and quinazolinones have a wide spectrum of biological activity. In this paper we focused on studying the antimicrobial and anti-inflammatory activities of some newly synthesized benzoxazinone and quinazolinone derivatives. Thus we prepared 2-[α-benzoylaminostyryl]-6,8-dibromo-3,1-benzoxazin-4(H)-one 2 which underwent a reaction with primary and secondary amines, and hydrazine hydrate to give compounds 3, 4 and 5, respectively. Treatment of 2 with hydroxylamine hydrochloride, formamide and/or NaN3/AcOH afforded compounds 7, 8, 11 and 12, respectively. Also, compound 2 reacted with maleic anhydride, aromatic hydrocarbons and/or active methylene compounds to produce compounds 13, 15a-c and 16, respectively. Most of the newly synthesized compounds showed significant antimicrobial and anti-inflammatory activities comparable to ampicillin, mycostatine and indomethacin positive controls.
authors.affiliation: Chemistry Department, Faculty of Science, Ain Shams University.
authors.forename: Maher Abd El-Aziz
authors.initials: MA
authors.lastname: El-Hashash
authors.forename: Mohammad Emad
authors.initials: ME
authors.lastname: Azab
authors.forename: Rasha Abd El-Aziz
authors.initials: RA
authors.lastname: Faty
authors.forename: Abd El-Galil Elsyed
authors.initials: Ael-G
authors.lastname: Amr
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D048588:Benzoxazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000890:Anti-Infective Agents; D000893:Anti-Inflammatory Agents; D048588:Benzoxazines; D052999:Quinazolinones