当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > Synthesis and in-vitro anti-leishmanial activity of (4-arylpiperazin-1-yl)(1-(thiophen-2-yl)-9H-pyrido[3,4-b]indol-3-yl)methanone derivatives.

Synthesis and in-vitro anti-leishmanial activity of (4-arylpiperazin-1-yl)(1-(thiophen-2-yl)-9H-pyrido[3,4-b]indol-3-yl)methanone derivatives.

Abstract：

:In the present study, we have reported synthesis and biological evaluation of a series of fifteen 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole derivatives against both promastigotes and amastigotes of Leishmania parasites responsible for visceral (L. donovani) and cutaneous (L. amazonensis) leishmaniasis. Among these reported analogues, compounds 7b, 7c, 7f, 7g, 7i, 7j, 7m, 7o displayed potent activity (15.55, 7.70, 7.00, 3.80, 14.10, 9.25, 3.10, 4.85μM, respectively) against L. donovani promastigotes than standard drugs miltefosine (15.70μM) and pentamidine (32.70μM) with good selectivity index. In further, in-vitro evaluation against amastigote forms, two compounds 7g (8.80μM) and 7i (7.50μM) showed significant inhibition of L. donovani amastigotes. Standard drug amphotericin B is also used as control to compare inhibition potency of compounds against both promastigote (0.24μM) and amastigote (0.05μM) forms.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Ashok P,Chander S,Chow LM,Wong IL,Singh RP,Jha PN,Sankaranarayanan M

doi

10.1016/j.bioorg.2016.11.013

subject

Has Abstract

pub_date

2017-02-01 00:00:00

pages

100-106

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(16)30088-8

journal_volume

70

pub_type

杂志文章

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