Literature DB >> 28835792

Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries.

Marc A Giulianotti1,2, Brian A Vesely3, Ala Azhari3, Ashley Souza3, Travis LaVoi2, Richard A Houghten2, Dennis E Kyle3, James W Leahy1,4,5.   

Abstract

From a screening campaign that included mixture-based libraries containing more than 6 million compounds, a lead series of bis-cyclic guanidines was identified as the most promising. Lead optimization resulted in the identification of potent (IC50 < 500 nM) and selective compounds within this series as well as potent and selective monoguanidines.

Entities:  

Keywords:  Leishmaniasis; lead optimization; mixture-based libraries; screening

Year:  2017        PMID： 28835792      PMCID： PMC5554901          DOI： 10.1021/acsmedchemlett.7b00045

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  10 in total

1.  Potent antimicrobial small molecules screened as inhibitors of tyrosine recombinases and Holliday junction-resolving enzymes.

Authors:  Marc C Rideout; Jeffrey L Boldt; Gabriel Vahi-Ferguson; Peter Salamon; Adel Nefzi; John M Ostresh; Marc Giulianotti; Clemencia Pinilla; Anca M Segall
Journal:  Mol Divers       Date:  2011-09-22       Impact factor: 2.943

2.  Strategies for the use of mixture-based synthetic combinatorial libraries: scaffold ranking, direct testing in vivo, and enhanced deconvolution by computational methods.

Authors:  Richard A Houghten; Clemencia Pinilla; Marc A Giulianotti; Jon R Appel; Colette T Dooley; Adel Nefzi; John M Ostresh; Yongping Yu; Gerald M Maggiora; Jose L Medina-Franco; Daniela Brunner; Jeff Schneider
Journal:  J Comb Chem       Date:  2007-12-08

3.  Control of the leishmaniases.

Authors: 
Journal:  World Health Organ Tech Rep Ser       Date:  2010

4.  Novel arylimidamides for treatment of visceral leishmaniasis.

Authors:  Michael Zhuo Wang; Xiaohua Zhu; Anuradha Srivastava; Qiang Liu; J Mark Sweat; Trupti Pandharkar; Chad E Stephens; Ed Riccio; Toufan Parman; Manoj Munde; Swati Mandal; Rentala Madhubala; Richard R Tidwell; W David Wilson; David W Boykin; James Edwin Hall; Dennis E Kyle; Karl A Werbovetz
Journal:  Antimicrob Agents Chemother       Date:  2010-04-05       Impact factor: 5.191

5.  Novel Amino-pyrazole Ureas with Potent In Vitro and In Vivo Antileishmanial Activity.

Authors:  Charles E Mowbray; Stéphanie Braillard; William Speed; Paul A Glossop; Gavin A Whitlock; Karl R Gibson; James E J Mills; Alan D Brown; J Mark F Gardner; Yafeng Cao; Wen Hua; Garreth L Morgans; Pim-Bart Feijens; An Matheeussen; Louis J Maes
Journal:  J Med Chem       Date:  2015-12-04       Impact factor: 7.446

6.  Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.

Authors:  Jinhua Wu; Yaohong Zhang; Laura E Maida; Radleigh G Santos; Gregory S Welmaker; Travis M LaVoi; Adel Nefzi; Yongping Yu; Richard A Houghten; Lawrence Toll; Marc A Giulianotti
Journal:  J Med Chem       Date:  2013-12-12       Impact factor: 7.446

7.  Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE Pathogens.

Authors:  Renee Fleeman; Travis M LaVoi; Radleigh G Santos; Angela Morales; Adel Nefzi; Gregory S Welmaker; José L Medina-Franco; Marc A Giulianotti; Richard A Houghten; Lindsey N Shaw
Journal:  J Med Chem       Date:  2015-04-01       Impact factor: 7.446

8.  An image-based high-content screening assay for compounds targeting intracellular Leishmania donovani amastigotes in human macrophages.

Authors:  Jair L Siqueira-Neto; Seunghyun Moon; Jiyeon Jang; Gyongseon Yang; Changbok Lee; Hong Kee Moon; Eric Chatelain; Auguste Genovesio; Jonathan Cechetto; Lucio H Freitas-Junior
Journal:  PLoS Negl Trop Dis       Date:  2012-06-12

Review 9.  One Health: the global challenge of epidemic and endemic leishmaniasis.

Authors:  Clarisa B Palatnik-de-Sousa; Michael J Day
Journal:  Parasit Vectors       Date:  2011-10-10       Impact factor: 3.876

10.  The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.

Authors:  Radleigh G Santos; Jon R Appel; Marc A Giulianotti; Bruce S Edwards; Larry A Sklar; Richard A Houghten; Clemencia Pinilla
Journal:  Molecules       Date:  2013-05-30       Impact factor: 4.411
  10 in total
  2 in total

1.  Highly Selective and Potent α4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.

Authors:  Jinhua Wu; Andrea Cippitelli; Yaohong Zhang; Ginamarie Debevec; Jennifer Schoch; Akihiko Ozawa; Yongping Yu; Huan Liu; Wenteng Chen; Richard A Houghten; Gregory S Welmaker; Marc A Giulianotti; Lawrence Toll
Journal:  J Med Chem       Date:  2017-12-13       Impact factor: 7.446

2.  Identification of Bis-Cyclic Guanidines as Antiplasmodial Compounds from Positional Scanning Mixture-Based Libraries.

Authors:  David L Perry; Bracken F Roberts; Ginamarie Debevec; Heather A Michaels; Debopam Chakrabarti; Adel Nefzi
Journal:  Molecules       Date:  2019-03-20       Impact factor: 4.411
  2 in total

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