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Structure-activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum.

Abstract：

:Utilizing mefloquine as a scaffold, a next generation quinoline methanol (NGQM) library was constructed to identify early lead compounds that possess biological properties consistent with the target product profile for malaria chemoprophylaxis while reducing permeability across the blood-brain barrier. The library of 200 analogs resulted in compounds that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum. Herein we report selected chemotypes and the emerging structure-activity relationship for this library of quinoline methanols.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Milner E,McCalmont W,Bhonsle J,Caridha D,Carroll D,Gardner S,Gerena L,Gettayacamin M,Lanteri C,Luong T,Melendez V,Moon J,Roncal N,Sousa J,Tungtaeng A,Wipf P,Dow G

doi

10.1016/j.bmcl.2010.01.001

subject

Has Abstract

pub_date

2010-02-15 00:00:00

pages

1347-51

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00003-X

journal_volume

20

pub_type

杂志文章

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