Literature DB >> 11591518

Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain.

W R Roush1, J Cheng, B Knapp-Reed, A Alvarez-Hernandez, J H McKerrow, E Hansell, J C Engel.   

Abstract

A new family of potent N-alkoxyvinylsulfonamide inhibitors of cruzain have been developed. Inhibitor 13 has a second order inactivation rate constant of 6,480,000s(-1)M(-1) versus cruzain, and is also highly effective against Trypanosoma cruzi trypomastigotes in a tissue culture assay.

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Year:  2001        PMID： 11591518     DOI： 10.1016/s0960-894x(01)00566-2

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

2.  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

3.  Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

Authors:  Bryan T Mott; Rafaela S Ferreira; Anton Simeonov; Ajit Jadhav; Kenny Kean-Hooi Ang; William Leister; Min Shen; Julia T Silveira; Patricia S Doyle; Michelle R Arkin; James H McKerrow; James Inglese; Christopher P Austin; Craig J Thomas; Brian K Shoichet; David J Maloney
Journal:  J Med Chem       Date:  2010-01-14       Impact factor: 7.446

4.  A novel Entamoeba histolytica cysteine proteinase, EhCP4, is key for invasive amebiasis and a therapeutic target.

Authors:  Chen He; George P Nora; Eric L Schneider; Iain D Kerr; Elizabeth Hansell; Ken Hirata; David Gonzalez; Mohammed Sajid; Sarah E Boyd; Petr Hruz; Eduardo R Cobo; Christine Le; Wei-Ting Liu; Lars Eckmann; Pieter C Dorrestein; Eric R Houpt; Linda S Brinen; Charles S Craik; William R Roush; James McKerrow; Sharon L Reed
Journal:  J Biol Chem       Date:  2010-04-08       Impact factor: 5.157

5.  Synthesis of a sugar-based thiosemicarbazone series and structure-activity relationship versus the parasite cysteine proteases rhodesain, cruzain, and Schistosoma mansoni cathepsin B1.

Authors:  Nayara Cristina Fonseca; Luana Faria da Cruz; Filipe da Silva Villela; Glaécia Aparecida do Nascimento Pereira; Jair Lage de Siqueira-Neto; Danielle Kellar; Brian M Suzuki; Debalina Ray; Thiago Belarmino de Souza; Ricardo José Alves; Policarpo Ademar Sales Júnior; Alvaro José Romanha; Silvane Maria Fonseca Murta; James H McKerrow; Conor R Caffrey; Renata Barbosa de Oliveira; Rafaela Salgado Ferreira
Journal:  Antimicrob Agents Chemother       Date:  2015-02-23       Impact factor: 5.191

6.  Identification of cysteine protease inhibitors as new drug leads against Naegleria fowleri.

Authors:  Ingrid Zyserman; Deboprosad Mondal; Francisco Sarabia; James H McKerrow; William R Roush; Anjan Debnath
Journal:  Exp Parasitol       Date:  2018-03-15       Impact factor: 2.011

7.  Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.

Authors:  Ajit Jadhav; Rafaela S Ferreira; Carleen Klumpp; Bryan T Mott; Christopher P Austin; James Inglese; Craig J Thomas; David J Maloney; Brian K Shoichet; Anton Simeonov
Journal:  J Med Chem       Date:  2010-01-14       Impact factor: 7.446

8.  In vitro and in vivo studies of the trypanocidal properties of WRR-483 against Trypanosoma cruzi.

Authors:  Yen Ting Chen; Linda S Brinen; Iain D Kerr; Elizabeth Hansell; Patricia S Doyle; James H McKerrow; William R Roush
Journal:  PLoS Negl Trop Dis       Date:  2010-09-14

9.  Structure-activity relationships for inhibition of cysteine protease activity and development of Plasmodium falciparum by peptidyl vinyl sulfones.

Authors:  Bhaskar R Shenai; Belinda J Lee; Alejandro Alvarez-Hernandez; Pek Y Chong; Cory D Emal; R Jeffrey Neitz; William R Roush; Philip J Rosenthal
Journal:  Antimicrob Agents Chemother       Date:  2003-01       Impact factor: 5.191

10.  Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain.

Authors:  Brian D Jones; Anna Tochowicz; Yinyan Tang; Michael D Cameron; Laura-Isobel McCall; Ken Hirata; Jair L Siqueira-Neto; Sharon L Reed; James H McKerrow; William R Roush
Journal:  ACS Med Chem Lett       Date:  2015-12-15       Impact factor: 4.345
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