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.
Synthesis and Structure-Activity Relationships of Lansine Analogues as Antileishmanial Agents / Pieroni, Marco; Girmay, Sisay; Sun, Dianqing; Sahu, Rajnish; Tekwani, Babu L.; Tan, Ghee T.. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 7:11(2012), pp. 1895-1900. [10.1002/cmdc.201200346]
Synthesis and Structure-Activity Relationships of Lansine Analogues as Antileishmanial Agents
PIERONI, Marco;
2012-01-01
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.