Literature DB >> 23182089

A natural product inspired hybrid approach towards the synthesis of novel pentamidine based scaffolds as potential anti-parasitic agents.

Vikas Tyagi1, Shahnawaz Khan, Rahul Shivahare, Khushboo Srivastava, Suman Gupta, Saqib Kidwai, Kumkum Srivastava, S K Puri, Prem M S Chauhan.   

Abstract

A natural product inspired molecular hybridization approach led us to a series of novel pentamidine based pyrimidine and chalcone scaffolds. All the hybrids were evaluated for their anti-leishmanial potential. Most of the screened compounds have showed significant in vitro anti-leishmanial activity with less cytotoxicity in comparison to the standard drugs (pentamidine, sodium stibogluconate, and miltefosine). Additionally, anti-malarial screening of these compounds was also done and four compounds have shown superior activity against chloroquine resistance strain (K1) of Plasmodium falciparum.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23182089     DOI: 10.1016/j.bmcl.2012.10.101

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Synthesis and preliminary biological evaluation of a small library of hybrid compounds based on Ugi isocyanide multicomponent reactions with a marine natural product scaffold.

Authors:  Edward Avilés; Jacques Prudhomme; Karine G Le Roch; Scott G Franzblau; Kevin Chandrasena; Alejandro M S Mayer; Abimael D Rodríguez
Journal:  Bioorg Med Chem Lett       Date:  2015-09-15       Impact factor: 2.823

2.  Discovery of triazine mimetics as potent antileishmanial agents.

Authors:  Kuldeep Chauhan; Moni Sharma; Rahul Shivahare; Utsab Debnath; Suman Gupta; Yenamandra S Prabhakar; Prem M S Chauhan
Journal:  ACS Med Chem Lett       Date:  2013-10-01       Impact factor: 4.345

3.  Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes.

Authors:  Karinel Nieves; Jacques Prudhomme; Karine G Le Roch; Scott G Franzblau; Abimael D Rodríguez
Journal:  Bioorg Med Chem Lett       Date:  2015-12-22       Impact factor: 2.823

4.  Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker.

Authors:  Ahmed Abdelhameed; Mei Feng; April C Joice; Emilia M Zywot; Yiru Jin; Chris La Rosa; Xiaoping Liao; Heidi L Meeds; Yena Kim; Junan Li; Craig A McElroy; Michael Zhuo Wang; Karl A Werbovetz
Journal:  ACS Infect Dis       Date:  2021-02-04       Impact factor: 5.578

  4 in total

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