Molecules (2016)
Update date:2022-08-02
Topics:
Seixas Xavier, Francisco José
Da Franca Rodrigues, Klinger Antonio
De Oliveira, Ramon Guerra
Lima, Claudio Gabriel
Da Camara Rocha, Juliana
Keesen, Tatjana Souza Lima
De Oliveira, Marcia Rosa
Silva, Fábio Pedrosa Lins
De Almeida Vasconcellos, Mário Luiz Araújo
Leishmaniasis represents a series of severe neglected tropical diseases caused by protozoa of the genus Leishmania and is widely distributed around the world. Here, we present the syntheses of Morita-Baylis-Hillman adducts (MBHAs) prepared from eugenol, thymol and carvacrol, and their bioevaluation against promastigotes of Leishmania amazonensis. The new MBHAs are prepared in two steps from essential oils in moderate to good yields and present IC50 values in the range of 22.30-4.71 μM. Moreover, the selectivity index to the most potent compound is very high (SIrb > 84.92), far better than that of Glucantime (SIrb 1.39) and amphotericin B (SIrb = 22.34). Conformational analysis were carried out at the M062X//6-31+G(d,p) level of theory to corroborate a hypothesis about the nitroaromatic bioreduction mechanism.
View MoreZhengzhou Minzhong Pharmaceutical Co.,ltd
Contact:0086-371-65797115
Address:15/F,Jiangshan Bldg, NO.126 Huanghe Road,Zhengzhou, China
Tianjin Anda North Industrial & Business Co.Ltd.
Contact:86-22-24999306
Address:No.11 Erwei Road,Dongli Development Area,Tianjin,China
Nantong LiKai Chemical Co.,Ltd
Contact:+86-513-89068669
Address:Jincheng Science Park
Nanjing Chemical Material Corp.(NCMC)
website:http://www.njchemm.com
Contact:0086-25-83172879
Address:B12 Technology and Innovation Building, Nanjing Tech University, No.5 New Model Road
Zhejiang Rongkai Chemical Technology Co.,Ltd.
Contact:+86-578-8185786
Address:Shangjiang Industrial Zone,Suichang
Doi:10.1002/ardp.19863190209
(1986)Doi:10.1080/00397919908086114
(1999)Doi:10.1007/BF00765909
(1980)Doi:10.3390/molecules201219743
(2015)Doi:10.1016/S0008-6215(00)85332-X
(1980)Doi:10.1016/S0040-4039(97)00650-3
(1997)