Literature DB >> 12873488

Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors.

Marian Flipo1, Isabelle Florent, Philippe Grellier, Christian Sergheraert, Rebecca Deprez-Poulain.   

Abstract

PfA-M1, a neutral zinc aminopeptidase of Plasmodium falciparum, is a new potential target for the discovery of antimalarials. The design and synthesis of a library of 45 quinoline-based inhibitors of PfA-M1 is reported. The best inhibitor displays an IC(50) of 854 nM. The antimalarial activity on a CQ-resistant strain and the specificity towards mammalian aminopeptidase N are also discussed.

Entities:  

Mesh：

Substances：

Year:  2003        PMID： 12873488     DOI： 10.1016/s0960-894x(03)00550-x

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


  13 in total

1.  IgG antibody response against Plasmodium falciparum aminopeptidase 1 antigen in Gabonese children living in Makokou and Franceville.

Authors:  S L Oyegue-Liabagui; R-K Imboumy-Limoukou; C L Kouna; F Bangueboussa; M Schmitt; I Florent; J B Lekana-Douki
Journal:  Clin Exp Immunol       Date:  2020-02-21       Impact factor: 4.330

Review 2.  Are Antimalarial Hybrid Molecules a Close Reality or a Distant Dream?

Authors:  Drishti Agarwal; Rinkoo D Gupta; Satish K Awasthi
Journal:  Antimicrob Agents Chemother       Date:  2017-04-24       Impact factor: 5.191

3.  Engagement of the S1, S1' and S2' subsites drives efficient catalysis of peptide bond hydrolysis by the M1-family aminopeptidase from Plasmodium falciparum.

Authors:  Seema Dalal; Daniel R T Ragheb; Michael Klemba
Journal:  Mol Biochem Parasitol       Date:  2012-02-13       Impact factor: 1.759

4.  Two cap residues in the S1 subsite of a Plasmodium falciparum M1-family aminopeptidase promote broad specificity and enhance catalysis.

Authors:  Matthew Rosati; Seema Dalal; Michael Klemba
Journal:  Mol Biochem Parasitol       Date:  2017-08-12       Impact factor: 1.759

5.  Chemical target validation studies of aminopeptidase in malaria parasites using alpha-aminoalkylphosphonate and phosphonopeptide inhibitors.

Authors:  Eithne Cunningham; Marcin Drag; Pawel Kafarski; Angus Bell
Journal:  Antimicrob Agents Chemother       Date:  2008-05-05       Impact factor: 5.191

6.  Plasmodium falciparum PfA-M1 aminopeptidase is trafficked via the parasitophorous vacuole and marginally delivered to the food vacuole.

Authors:  Omid Azimzadeh; Cissé Sow; Marc Gèze; Julius Nyalwidhe; Isabelle Florent
Journal:  Malar J       Date:  2010-06-30       Impact factor: 2.979

7.  Exploration of structural and physicochemical requirements and search of virtual hits for aminopeptidase N inhibitors.

Authors:  Amit K Halder; Achintya Saha; Tarun Jha
Journal:  Mol Divers       Date:  2013-01-23       Impact factor: 2.943

8.  Fingerprinting the substrate specificity of M1 and M17 aminopeptidases of human malaria, Plasmodium falciparum.

Authors:  Marcin Poreba; Sheena McGowan; Tina S Skinner-Adams; Katharine R Trenholme; Donald L Gardiner; James C Whisstock; Joyce To; Guy S Salvesen; John P Dalton; Marcin Drag
Journal:  PLoS One       Date:  2012-02-16       Impact factor: 3.240

9.  Structural modifications of quinoline-based antimalarial agents: Recent developments.

Authors:  Sandhya Bawa; Suresh Kumar; Sushma Drabu; Rajiv Kumar
Journal:  J Pharm Bioallied Sci       Date:  2010-04

10.  A Multilayer Network Approach for Guiding Drug Repositioning in Neglected Diseases.

Authors:  Ariel José Berenstein; María Paula Magariños; Ariel Chernomoretz; Fernán Agüero
Journal:  PLoS Negl Trop Dis       Date:  2016-01-06
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.