Literature DB >> 31706668

A new chemotype with promise against Trypanosoma cruzi.

Xiaofang Wang1, Monica Cal2, Marcel Kaiser2, Frederick S Buckner3, Galina I Lepesheva4, Austin G Sanford5, Alexander I Wallick5, Paul H Davis5, Jonathan L Vennerstrom6.   

Abstract

Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of ≥10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity against T. cruzi. Compound 2 and its active analogs had low to moderate metabolic stabilities in human and mouse liver microsomes.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Chagas disease; SAR; Trypanosoma cruzi

Year:  2019        PMID： 31706668      PMCID： PMC6892603          DOI： 10.1016/j.bmcl.2019.126778

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


  23 in total

1.  Synthesis and evaluation of new hydrazide derivatives as neuropeptide Y Y5 receptor antagonists for the treatment of obesity.

Authors:  Laura Juanenea; Silvia Galiano; Oihana Erviti; Antonio Moreno; Silvia Pérez; Ignacio Aldana; Antonio Monge
Journal:  Bioorg Med Chem       Date:  2004-09-01       Impact factor: 3.641

2.  CYP51 from Trypanosoma cruzi: a phyla-specific residue in the B' helix defines substrate preferences of sterol 14alpha-demethylase.

Authors:  Galina I Lepesheva; Natalia G Zaitseva; W David Nes; Wenxu Zhou; Miharu Arase; Jialin Liu; George C Hill; Michael R Waterman
Journal:  J Biol Chem       Date:  2005-11-30       Impact factor: 5.157

3.  Novel Toxoplasma gondii inhibitor chemotypes.

Authors:  A G Sanford; T T Schulze; L P Potluri; R M Hemsley; J J Larson; A K Judge; S J Zach; X Wang; S A Charman; J L Vennerstrom; P H Davis
Journal:  Parasitol Int       Date:  2018-01-04       Impact factor: 2.230

4.  Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality.

Authors:  Denise A Chan; Patrick D Sutphin; Phuong Nguyen; Sandra Turcotte; Edwin W Lai; Alice Banh; Gloria E Reynolds; Jen-Tsan Chi; Jason Wu; David E Solow-Cordero; Muriel Bonnet; Jack U Flanagan; Donna M Bouley; Edward E Graves; William A Denny; Michael P Hay; Amato J Giaccia
Journal:  Sci Transl Med       Date:  2011-08-03       Impact factor: 17.956

5.  Anticancer agents interacting with membrane glucose transporters.

Authors:  C Granchi; S Fortunato; F Minutolo
Journal:  Medchemcomm       Date:  2016-07-08       Impact factor: 3.597

6.  Polar molecular surface properties predict the intestinal absorption of drugs in humans.

Authors:  K Palm; P Stenberg; K Luthman; P Artursson
Journal:  Pharm Res       Date:  1997-05       Impact factor: 4.200

7.  Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.

Authors:  Martine Keenan; Paul W Alexander; Jason H Chaplin; Michael J Abbott; Hugo Diao; Zhisen Wang; Wayne M Best; Catherine J Perez; Scott M J Cornwall; Sarah K Keatley; R C Andrew Thompson; Susan A Charman; Karen L White; Eileen Ryan; Gong Chen; Jean-Robert Ioset; Thomas W von Geldern; Eric Chatelain
Journal:  Future Med Chem       Date:  2013-10       Impact factor: 3.808

Review 8.  Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.

Authors:  Mark C Field; David Horn; Alan H Fairlamb; Michael A J Ferguson; David W Gray; Kevin D Read; Manu De Rycker; Leah S Torrie; Paul G Wyatt; Susan Wyllie; Ian H Gilbert
Journal:  Nat Rev Microbiol       Date:  2017-02-27       Impact factor: 60.633

9.  Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51.

Authors:  Shamila S Gunatilleke; Claudia M Calvet; Jonathan B Johnston; Chiung-Kuang Chen; Grigori Erenburg; Jiri Gut; Juan C Engel; Kenny K H Ang; Joseph Mulvaney; Steven Chen; Michelle R Arkin; James H McKerrow; Larissa M Podust
Journal:  PLoS Negl Trop Dis       Date:  2012-07-31

10.  Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.

Authors:  Martine Keenan; Jason H Chaplin; Paul W Alexander; Michael J Abbott; Wayne M Best; Andrea Khong; Adriana Botero; Catherine Perez; Scott Cornwall; R Andrew Thompson; Karen L White; David M Shackleford; Maria Koltun; Francis C K Chiu; Julia Morizzi; Eileen Ryan; Michael Campbell; Thomas W von Geldern; Ivan Scandale; Eric Chatelain; Susan A Charman
Journal:  J Med Chem       Date:  2013-12-04       Impact factor: 7.446
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