当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Discovery of a bulky 2-tert-butyl group containing primaquine analogue that exhibits potent blood-schizontocidal antimalarial activities and complete elimination of methemoglobin toxicity.

Discovery of a bulky 2-tert-butyl group containing primaquine analogue that exhibits potent blood-schizontocidal antimalarial activities and complete elimination of methemoglobin toxicity.

Abstract：

:To eliminate an unwarranted metabolic pathway of the quinoline ring, a set of two compounds, where C-2 position of the antimalarial drug primaquine is blocked by metabolically stable bulky alkyl group are synthesized. Compound 2 [R = C(CH(3))(3)] of the series has produced excellent antimalarial efficacy against P. berghei and highly virulent multidrug-resistant P. yoelii nigeriensis strain in vivo. Compound 2 was also evaluated for methemoglobin (MetHb) toxicity. This study describes the discovery of a highly potent blood-schizontocidal antimalarial analogue 2, completely devoid of MetHb toxicity.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Jain M,Vangapandu S,Sachdeva S,Singh S,Singh PP,Jena GB,Tikoo K,Ramarao P,Kaul CL,Jain R

doi

10.1021/jm0304562

keywords:

subject

Has Abstract

pub_date

2004-01-15 00:00:00

pages

285-7

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

47

pub_type

杂志文章

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