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Synthesis, anti-leishmanial and molecular docking study of bis-indole derivatives.


ABSTRACT: We have synthesized new series of bisindole analogs (1-27), characterized by 1HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC50 values ranging from 0.7?±?0.01 to 13.30?±?0.50 µM respectively when compared with standard pentamidine with IC50 value of 7.20?±?0.20 µM. All analogs showed greater potential than standard except 10, 19 and 23 when compared with standard. Structure activity relationship has been also established for all compounds. Molecular docking studies were carried out to understand the binding interaction of active molecules.

SUBMITTER: Taha M 

PROVIDER: S-EPMC6685257 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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We have synthesized new series of bisindole analogs (<b>1</b>-<b>27</b>), characterized by <sup>1</sup>HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC<sub>50</sub> values ranging from 0.7 ± 0.01 to 13.30 ± 0.50 µM respectively when compared with standard pentamidine with IC<sub>50</sub> value of 7.20 ± 0.20 µM. All analogs showed greater potential than standard except <b>10</b>, <b>19</b> and <b>23</b> when compa  ...[more]

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