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

Taha M 1 , Uddin I 2 , Gollapalli M 3 , Almandil NB 1 , Rahim F 2 , Farooq RK 4 Show all authors , Nawaz M 5 , Ibrahim M 1 , Alqahtani MA 1 , Bamarouf YA 3 , Selvaraj M 6

Affiliations 

  • 1 1Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam, 31441 Saudi Arabia
  • 2 2Department of Chemistry, Hazara University, Mansehra, 21300 Khyber Pakhtunkhwa Pakistan
  • 3 3Department of Computer Information Systems, College of Computer Science & Information Technology, Imam Abdulrahman Bin Faisal University, P. O. Box 1982, Dammam, 31441 Saudi Arabia
  • 4 4Department of Neuroscience Research, Institute of Research and Medical Consultations, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam, 31441 Saudi Arabia
  • 5 5Department of Nano-Medicine Research, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam, 31441 Saudi Arabia
  • 6 6Monash University School of Chemical Engineering, 47500 Bandar Sunway, Selangor Malaysia
BMC Chem, 2019 Dec;13(1):102.
PMID: 31410413 DOI: 10.1186/s13065-019-0617-4

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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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