New natural sesquiterpenes as modulators of daunomycin resistance in a multidrug-resistant Leishmania tropica line

被引:54
作者
Pérez-Victoria, JM
Tincusi, BM
Jiménez, IA
Bazzocchi, IL
Gupta, MP
Castanys, S
Gamarro, F
Ravelo, AG
机构
[1] CSIC, Inst Parasitol & Biomed Lopez Neyra, Granada 18001, Spain
[2] Univ La Laguna, Inst Bioorgan Antonio Gonzalez, La Laguna 38206, Tenerife, Spain
[3] Univ Panama, Fac Farm, CIFLORPAN, Panama City, Panama
关键词
D O I
10.1021/jm991066b
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The effects produced by nine dihydro-beta-agarofuran sesquiterpenes isolated from Crossopetalum tonduzii (1-8) and Maytenus macrocarpa (9) (Celastraceae) on the reversion of the resistant phenotype on a multidrug-resistant Leishmania line and their binding to recombinant C-terminal nucleotide-binding domain of Leishmania P-glycoprotein-like transporter were studied. The structures of the new compounds (1-5) were elucidated by spectroscopic methods, including H-1-C-13 heteronuclear correlation (HMQC), long-range correlation spectra with inversal detection (HMBC), ROESY experiments, and chemical correlations. The absolute configuration of one of them (1) was determined by CD studies. The structure-activity relationship is discussed.
引用
收藏
页码:4388 / 4393
页数:6
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