Literature DB >> 19091562

Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity.

Chitalu C Musonda1, Gavin A Whitlock, Michael J Witty, Reto Brun, Marcel Kaiser.   

Abstract

A series of 2-pyridyl pyrimidines, reported inhibitors of Plasmodium falciparum methionine aminopeptidase 1b were synthesized and evaluated for their antiplasmodial activities. An analysis of physicochemical properties demonstrated a link between lipophilicity and antiparasitic activity. Cross screening of the library against cultured Leishmania donovani parasites revealed this class of compounds as potent inhibitors of parasite development in vitro.

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Year:  2008        PMID： 19091562     DOI： 10.1016/j.bmcl.2008.11.098

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


  8 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

2.  The identification of inhibitory compounds of Rickettsia prowazekii methionine aminopeptidase for antibacterial applications.

Authors:  Travis R Helgren; Elif S Seven; Congling Chen; Thomas E Edwards; Bart L Staker; Jan Abendroth; Peter J Myler; James R Horn; Timothy J Hagen
Journal:  Bioorg Med Chem Lett       Date:  2018-03-15       Impact factor: 2.823

3.  Antiparasitic activities of novel, orally available fumagillin analogs.

Authors:  Christopher Arico-Muendel; Paolo A Centrella; Brooke D Contonio; Barry A Morgan; Gary O'Donovan; Christopher L Paradise; Steven R Skinner; Barbara Sluboski; Jennifer L Svendsen; Kerry F White; Anjan Debnath; Jiri Gut; Nathan Wilson; James H McKerrow; Joseph L DeRisi; Philip J Rosenthal; Peter K Chiang
Journal:  Bioorg Med Chem Lett       Date:  2009-07-10       Impact factor: 2.823

4.  In Vitro and In Vivo Characterization of Potent Antileishmanial Methionine Aminopeptidase 1 Inhibitors.

Authors:  Felipe Rodriguez; Sarah F John; Eva Iniguez; Sebastian Montalvo; Karina Michael; Lyndsey White; Dong Liang; Omonike A Olaleye; Rosa A Maldonado
Journal:  Antimicrob Agents Chemother       Date:  2020-05-21       Impact factor: 5.191

Review 5.  Advances in Bacterial Methionine Aminopeptidase Inhibition.

Authors:  Travis R Helgren; Phumvadee Wangtrakuldee; Bart L Staker; Timothy J Hagen
Journal:  Curr Top Med Chem       Date:  2016       Impact factor: 3.295

Review 6.  Rapid analysis of pharmacology for infectious diseases.

Authors:  Andrew L Hopkins; G Richard Bickerton; Ian M Carruthers; Stephen K Boyer; Harvey Rubin; John P Overington
Journal:  Curr Top Med Chem       Date:  2011       Impact factor: 3.295

7.  Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery.

Authors:  Sandra Duffy; Melissa L Sykes; Amy J Jones; Todd B Shelper; Moana Simpson; Rebecca Lang; Sally-Ann Poulsen; Brad E Sleebs; Vicky M Avery
Journal:  Antimicrob Agents Chemother       Date:  2017-08-24       Impact factor: 5.191

8.  Discovery of New Chemical Tools against Leishmania amazonensis via the MMV Pathogen Box.

Authors:  Atteneri López-Arencibia; Ines Sifaoui; María Reyes-Batlle; Carlos J Bethencourt-Estrella; Desirée San Nicolás-Hernández; Jacob Lorenzo-Morales; José E Piñero
Journal:  Pharmaceuticals (Basel)       Date:  2021-11-24
  8 in total

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