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

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

  • Bioorg Med Chem Lett. 2010 Feb 15;20(4):1347-51. doi: 10.1016/j.bmcl.2010.01.001.
Erin Milner 1,  William McCalmont,  Jayendra Bhonsle,  Diana Caridha,  Dustin Carroll,  Sean Gardner,  Lucia Gerena,  Montip Gettayacamin,  Charlotte Lanteri,  Thulan Luong,  Victor Melendez,  Jay Moon,  Norma Roncal,  Jason Sousa,  Anchalee Tungtaeng,  Peter Wipf,  Geoffrey Dow
Affiliations

Affiliation

  • 1 Walter Reed Army Institute of Research, Silver Spring, MD, USA. erin.milner@us.army.mil
PMID: 20097070 DOI: 10.1016/j.bmcl.2010.01.001
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.

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