Soluble Synthetic Analogues of Malaria Pigment: Structure of Mesohematin Anhydride and its Interaction with Chloroquine in Solution

被引：21

作者：

Bohle, D. Scott ^{[1
]}

Dodd, Erin L. ^{[1
]}

Kosar, Aaron J. ^{[1
]}

Sharma, Lauren ^{[1
]}

Stephens, Peter W. ^{[2
]}

Suarez, Liliana ^{[1
]}

Tazoo, Dagobert ^{[1
]}

机构：

[1] McGill Univ, Dept Chem, Montreal, PQ H3A 2K6, Canada

[2] SUNY Stony Brook, Dept Phys & Astron, Stony Brook, NY 11794 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2011年 / 50卷 / 27期

基金：

加拿大自然科学与工程研究理事会;

关键词：

chloroquine; drug targets; malaria; porphyrinoids; structure elucidation; BETA-HEMATIN; TROPHOZOITES; FALCIPARUM; COMPLEXES; PRODUCTS; DRUGS; PHASE; EPR;

D O I：

10.1002/anie.201100910

中图分类号：

O6 [化学];

学科分类号：

070301 [无机化学];

摘要：

Where the action is: Changing the vinyl groups of hematin anhydride to either ethyl or hydrogen groups results in increased solubility (see picture; Por=porphyrin). Determination of the weak binding constants of the antimalarial drug chloroquine to dimers of these hematin anhydride analogues suggests that solution-phase heme/drug interactions alone are unlikely to be the origin of the action of the drug. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：6151 / 6154

页数：4

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