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New antiprotozoal agents: their synthesis and biological evaluations.

Abstract：

:Here we report identification of new lead compounds based on quinoline and indenoquinolines with variable side chains as antiprotozoal agents. Quinolines 32, 36 and 37 (Table 1) and indenoquinoline derivatives 14 and 23 (Table 2) inhibit the in vitro growth of the Trypanosoma cruzi, Trypanosoma brucei, Trypanosoma brucei rhodesiense subspecies and Leishmania infantum with IC50=0.25 μM. These five compounds have superior activity to that of the front-line drugs such as benznidazole, nifurtimox and comparable to amphotericin B. Thus these compounds constitute new 'leads' for further structure-activity studies as potential active antiprotozoal agents.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Upadhayaya RS,Dixit SS,Földesi A,Chattopadhyaya J

doi

10.1016/j.bmcl.2013.02.054

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

2750-8

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00230-8

journal_volume

23

pub_type

杂志文章

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