Literature DB >> 15225694

Application of multi-component reactions to antimalarial drug discovery. Part 1: Parallel synthesis and antiplasmodial activity of new 4-aminoquinoline Ugi adducts.

Chitalu C Musonda1, Dale Taylor, Julie Lehman, Jiri Gut, Philip J Rosenthal, Kelly Chibale.   

Abstract

The synthesis of a new class of Ugi adducts incorporating the 4-aminoquinoline moiety is described. The novel compounds are active against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum with the best compound showing an IC(50) value of 73 nM against a resistant K1 strain.

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Year:  2004        PMID： 15225694     DOI： 10.1016/j.bmcl.2004.05.063

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


  12 in total

Review 1.  Chemistry and biology of multicomponent reactions.

Authors:  Alexander Dömling; Wei Wang; Kan Wang
Journal:  Chem Rev       Date:  2012-03-22       Impact factor: 60.622

2.  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

3.  Validation of microsatellite markers for use in genotyping polyclonal Plasmodium falciparum infections.

Authors:  Bryan Greenhouse; Alissa Myrick; Christian Dokomajilar; Jonathan M Woo; Elaine J Carlson; Philip J Rosenthal; Grant Dorsey
Journal:  Am J Trop Med Hyg       Date:  2006-11       Impact factor: 2.345

4.  Synthesis and antimalarial activity of new 4-amino-7-chloroquinolyl amides, sulfonamides, ureas and thioureas.

Authors:  Kekeli Ekoue-Kovi; Kimberly Yearick; Daniel P Iwaniuk; Jayakumar K Natarajan; John Alumasa; Angel C de Dios; Paul D Roepe; Christian Wolf
Journal:  Bioorg Med Chem       Date:  2008-11-12       Impact factor: 3.641

5.  Synthesis of some new triamide derivatives via Ugi five-component reaction in aqueous solution.

Authors:  Ali Asghar Mohammadi; Salman Taheri; Arman Amini; Reza Ahdenov
Journal:  Mol Divers       Date:  2018-06-27       Impact factor: 2.943

6.  Novel Anticancer Fused Pyrazole Derivatives as EGFR and VEGFR-2 Dual TK Inhibitors.

Authors:  Nashwa M Saleh; Marwa G El-Gazzar; Hala M Aly; Rana A Othman
Journal:  Front Chem       Date:  2020-01-24       Impact factor: 5.221

7.  Identification of two novel RET kinase inhibitors through MCR-based drug discovery: design, synthesis and evaluation.

Authors:  Brendan Frett; Marialuisa Moccia; Francesca Carlomagno; Massimo Santoro; Hong-yu Li
Journal:  Eur J Med Chem       Date:  2014-09-08       Impact factor: 6.514

Review 8.  Use of multicomponent reactions in developing small-molecule tools to study GABAA receptor mechanism and function.

Authors:  Ryan W Lewis; George P Hess; Bruce Ganem
Journal:  Future Med Chem       Date:  2011-02       Impact factor: 3.808

9.  Synthesis of Constrained Heterocycles Employing Two Post-Ugi Cyclization Methods for Rapid Library Generation with In Cellulo Activity.

Authors:  Nicholas McConnell; Zhigang Xu; Vishnu Kumarasamy; Daekyu Sun; Brendan Frett; Hong-Yu Li
Journal:  ChemistrySelect       Date:  2017-12-19       Impact factor: 2.109

10.  4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria.

Authors:  Jayakumar K Natarajan; John N Alumasa; Kimberly Yearick; Kekeli A Ekoue-Kovi; Leah B Casabianca; Angel C de Dios; Christian Wolf; Paul D Roepe
Journal:  J Med Chem       Date:  2008-06-26       Impact factor: 7.446
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