Synthesis of 2,3-diaryl-1,3-benzoxazine and preliminary studies on its activity against Leishmania infantum CYP51
TANG Zilong1， HAN Xinya2， LI Xinxing1， XU Zhifeng3， WANG Yichao1
1.Key Laboratory of Theoretical Organic Chemistry and Functional Molecule of Ministry of Education， Hunan University of Science and Technology， Xiangtan， Hunan 411201；2. School of Chemistry， Central China Normal University， Wuhan 430079； 3.School of Chemistry and Material Science， Hengyang Normal University， Hengyang， Hunan 421002
Abstract：The interaction of 2-(-2nitrophenyl)-3-(4-methylphenyl)-1,3-benzoxazine (1) and Leishmaniainfantum CYP51 was preliminarily investigated for the first time. The results indicated that compound 1 exhibited relatively strong inhibitory activity with I type mode of action similar to the model between the substrate and Leishmaniainfantum CYP51. The study has not only discovered a new kind of nonazole inhibitor (1,3-benzoxazine) against Leishmania infantum CYP51， butalsoprovidedexperimentalbasisforthediscoveryofnewCYP51 inhibitorywithnewmodeofaction.
