El-Hashash Maher Abd El-Aziz, Azab Mohammad Emad, Faty Rasha Abd El-Aziz, Amr Abd El-Galil Elsyed
Chemistry Department, Faculty of Science, Ain Shams University.
Chem Pharm Bull (Tokyo). 2016;64(3):263-71. doi: 10.1248/cpb.c15-00904. Epub 2015 Dec 22.
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.
苯并恶嗪酮和喹唑啉酮具有广泛的生物活性。在本文中，我们着重研究了一些新合成的苯并恶嗪酮和喹唑啉酮衍生物的抗菌和抗炎活性。因此，我们制备了2-[α-苯甲酰氨基苯乙烯基]-6,8-二溴-3,1-苯并恶嗪-4(H)-酮2，其分别与伯胺、仲胺和水合肼反应，得到化合物3、4和5。用盐酸羟胺、甲酰胺和/或NaN3/AcOH处理2，分别得到化合物7、8、11和12。此外，化合物2与马来酸酐、芳烃和/或活性亚甲基化合物反应，分别生成化合物13、15a - c和16。大多数新合成的化合物显示出与氨苄青霉素、制霉菌素和吲哚美辛阳性对照相当的显著抗菌和抗炎活性。
