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Synthesis and structure-activity relationships of lansine analogues as antileishmanial agents.

ABSTRACT: Clear and rational thinking: A series of rationally designed, lansine-derived carbazoles was synthesized and evaluated for activity against promastigotes and amastigotes of Leishmania donovani, the causative agent of leishmaniasis. Some structural modifications gave rise to compounds with enhanced activity and selectivity over lansine, allowing structure-activity relationships to be elucidated and providing a foundation for the further development of this pharmacophore.

SUBMITTER: Pieroni M 

PROVIDER: S-EPMC3565020 | biostudies-literature | 2012 Nov

REPOSITORIES: biostudies-literature

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Synthesis and structure-activity relationships of lansine analogues as antileishmanial agents.

Pieroni Marco M   Girmay Sisay S   Sun Dianqing D   Sahu Rajnish R   Tekwani Babu L BL   Tan Ghee T GT  

ChemMedChem 20120917 11

Clear and rational thinking: A series of rationally designed, lansine-derived carbazoles was synthesized and evaluated for activity against promastigotes and amastigotes of Leishmania donovani, the causative agent of leishmaniasis. Some structural modifications gave rise to compounds with enhanced activity and selectivity over lansine, allowing structure-activity relationships to be elucidated and providing a foundation for the further development of this pharmacophore. ...[more]

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