Literature DB >> 18055204

Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes.

Priyadarshini Jaishankar1, Elizabeth Hansell, Dong-Mei Zhao, Patricia S Doyle, James H McKerrow, Adam R Renslo.   

Abstract

A systematic study of P2 and P3 substitution in a series of vinyl sulfone cysteine protease inhibitors is described. The introduction of a methyl substituent in the P2 phenylalanine aryl ring had a favorable effect on protease inhibition and conferred modest selectivity for rhodesain over cruzain. Rhodesain selectivity could be enhanced further by combining these P2 modifications with certain P3 amide substituents.

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Year:  2007        PMID： 18055204     DOI： 10.1016/j.bmcl.2007.11.070

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


  13 in total

1.  Structural basis for inhibition of cathepsin B drug target from the human blood fluke, Schistosoma mansoni.

Authors:  Adéla Jílková; Pavlína Rezácová; Martin Lepsík; Martin Horn; Jana Váchová; Jindrich Fanfrlík; Jirí Brynda; James H McKerrow; Conor R Caffrey; Michael Mares
Journal:  J Biol Chem       Date:  2011-08-10       Impact factor: 5.157

Review 2.  Host-parasite interactions in trypanosomiasis: on the way to an antidisease strategy.

Authors:  Nicolas Antoine-Moussiaux; Philippe Büscher; Daniel Desmecht
Journal:  Infect Immun       Date:  2009-01-21       Impact factor: 3.441

3.  Automated molecule editing in molecular design.

Authors:  Peter W Kenny; Carlos A Montanari; Igor M Prokopczyk; Fernanda A Sala; Geraldo Rodrigues Sartori
Journal:  J Comput Aided Mol Des       Date:  2013-09-04       Impact factor: 3.686

4.  Divergent modes of enzyme inhibition in a homologous structure-activity series.

Authors:  Rafaela S Ferreira; Clifford Bryant; Kenny K H Ang; James H McKerrow; Brian K Shoichet; Adam R Renslo
Journal:  J Med Chem       Date:  2009-08-27       Impact factor: 7.446

5.  Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.

Authors:  Yen Ting Chen; Ricardo Lira; Elizabeth Hansell; James H McKerrow; William R Roush
Journal:  Bioorg Med Chem Lett       Date:  2008-06-10       Impact factor: 2.823

6.  Two approaches to discovering and developing new drugs for Chagas disease.

Authors:  J H McKerrow; P S Doyle; J C Engel; L M Podust; S A Robertson; R Ferreira; T Saxton; M Arkin; I D Kerr; L S Brinen; C S Craik
Journal:  Mem Inst Oswaldo Cruz       Date:  2009-07       Impact factor: 2.743

7.  Benzimidazole inhibitors of the major cysteine protease of Trypanosoma brucei.

Authors:  Glaécia An Pereira; Lucianna H Santos; Steven C Wang; Luan C Martins; Filipe S Villela; Weiting Liao; Marco A Dessoy; Luiz C Dias; Adriano D Andricopulo; Mariana Af Costa; Ronaldo Ap Nagem; Conor R Caffrey; Klaus R Liedl; Ernesto R Caffarena; Rafaela S Ferreira
Journal:  Future Med Chem       Date:  2019-07       Impact factor: 3.808

8.  Drug discovery for neglected tropical diseases at the Sandler Center.

Authors:  Stephanie A Robertson; Adam R Renslo
Journal:  Future Med Chem       Date:  2011-08       Impact factor: 3.808

9.  Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.

Authors:  Clifford Bryant; Iain D Kerr; Moumita Debnath; Kenny K H Ang; Joseline Ratnam; Rafaela S Ferreira; Priyadarshini Jaishankar; DongMei Zhao; Michelle R Arkin; James H McKerrow; Linda S Brinen; Adam R Renslo
Journal:  Bioorg Med Chem Lett       Date:  2009-09-03       Impact factor: 2.823

10.  Vinyl sulfones as antiparasitic agents and a structural basis for drug design.

Authors:  Iain D Kerr; Ji H Lee; Christopher J Farady; Rachael Marion; Mathias Rickert; Mohammed Sajid; Kailash C Pandey; Conor R Caffrey; Jennifer Legac; Elizabeth Hansell; James H McKerrow; Charles S Craik; Philip J Rosenthal; Linda S Brinen
Journal:  J Biol Chem       Date:  2009-07-20       Impact factor: 5.157
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