Search for new pharmacophores for antimalarial activity. Part I: Synthesis and antimalarial activity of new 2-methyl-6-ureido-4-quinolinamides

被引：47
|
作者：
Madapa, S. [1 ]
Tusi, Z. [1 ]
Sridhar, D. [1 ]
Kumar, A. [2 ]
Siddiqi, M. I. [2 ]
Srivastava, K. [3 ]
Rizvi, A. [3 ]
Tripathi, R. [3 ]
Puri, S. K. [3 ]
Keshava, G. B. Shiva [4 ]
Shukla, P. K. [4 ]
Batra, S. [1 ]
机构：
[1] Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Mol & Struct Biol Div, Lucknow 226001, Uttar Pradesh, India
[3] Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India
[4] Cent Drug Res Inst, Fermentat Div, Lucknow 226001, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 01期
关键词：
Quinoline; Antimalarial; Urea; In vitro; Docking; PROTEIN-LIGAND INTERACTIONS; PLASMODIUM-FALCIPARUM; BINDING AFFINITIES; SCORING FUNCTION; DERIVATIVES; DOCKING; DESIGN; AGENTS;
D O I：
10.1016/j.bmc.2008.11.021
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A total of 80 new 2-methyl-6-ureido-4-quinolinamides were synthesized and evaluated for their antimalarial activity. Several analogs elicited the antimalarial effect at MIC of 0.25 mg/mL against the chlooquine-sensitive P. falciparum strain. The IC50 values of the active compounds were observed to be in ng/mL range and two of the analogs have better IC50 value than the standard chloroquine. In the in vivo assay against mdr CQ resistant P. yoelii N67/P. yoelii nigeriensis, however, none of the compound showed complete suppression of parasitemia on day 7. One of the compounds displayed significant antibacterial effect against several strains of bacteria and was many-fold better than the standard drug gentamicin. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：203 / 221
页数：19
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