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Antileishmanial pyrazolopyridine derivatives: synthesis and structure-activity relationship analysis.

Abstract：

:Three series of 4-anilino-1H-pyrazolo[3,4-b]pyridine-5-carboxylic esters were synthesized as part of a program to study potential anti-Leishmania drugs. These compounds were obtained by a condensation reaction of 4-chloro-1H-pyrazolo[3,4-b]pyridine with several aniline derivatives. Some of them were also obtained by an alternative pathway involving a Mannich-type reaction. The hydrophobic parameter, log P, was determined by shake-flask methodology, and using the Hansch-Fujita addictive hydrophobic fragmental constants. These compounds were tested against promastigote forms of Leishmania amazonensis. The very promising results showed the 3'-diethylaminomethyl-substituted compounds as the most active [IC50 = 0.39 (21) and 0.12 microM (22)]. Molecular modeling, using semiempirical AM1 method, predicted the most active compounds through the low-energy conformers superimposition on amodiaquine structure. QSAR equations, derived from the IC50 values against L. amazonensis, showed the hydrophobic (log P) and Sterimol steric (L and B2) parameters as most significant contributions on biological activity.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

de Mello H,Echevarria A,Bernardino AM,Canto-Cavalheiro M,Leon LL

doi

10.1021/jm0401006

keywords:

subject

Has Abstract

pub_date

2004-10-21 00:00:00

pages

5427-32

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

47

pub_type

杂志文章

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