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

We have synthesized new series of bisindole analogs (1–27), characterized by (1)HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC(50) values ranging from 0.7 ± 0.01 to 13.30 ± 0.50 µM respectively when compared with st...

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Detalles Bibliográficos
Autores principales: Taha, Muhammad, Uddin, Imad, Gollapalli, Mohammed, Almandil, Noor Barak, Rahim, Fazal, Farooq, Rai Khalid, Nawaz, Muhammad, Ibrahim, Mohamed, Alqahtani, Mohammed A., Bamarouf, Yasser A., Selvaraj, Manikandan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6685257/
https://www.ncbi.nlm.nih.gov/pubmed/31410413
http://dx.doi.org/10.1186/s13065-019-0617-4
Descripción
Sumario:We have synthesized new series of bisindole analogs (1–27), characterized by (1)HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC(50) values ranging from 0.7 ± 0.01 to 13.30 ± 0.50 µM respectively when compared with standard pentamidine with IC(50) 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. [Image: see text] ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1186/s13065-019-0617-4) contains supplementary material, which is available to authorized users.