Literature DB >> 24900706

New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.

Laura Friggeri1, Luigi Scipione1, Roberta Costi2, Marcel Kaiser3, Francesca Moraca4, Claudio Zamperini4, Bruno Botta1, Roberto Di Santo2, Daniela De Vita1, Reto Brun5, Silvano Tortorella1.   

Abstract

The antiparasitic activity of azole and new 4-aminopyridine derivatives has been investigated. The imidazoles 1 and 3-5 showed a potent in vitro antichagasic activity with IC50 values in the low nanomolar concentration range. The (S)-1, (S)-3, and (S)-5 enantiomers showed (up to) a thousand-fold higher activity than the reference drug benznidazole and furthermore low cytotoxicity on rat myogenic L6 cells.

Entities:  

Keywords:  CYP51; Chagas disease; Trypanosoma cruzi; aminopyridine; antiparasitic activity; azole

Year:  2013        PMID： 24900706      PMCID： PMC4027138          DOI： 10.1021/ml400039r

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


  18 in total

1.  Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14alpha-demethylase (CYP51) from Leishmania infantum.

Authors:  Tatiana Y Hargrove; Zdzislaw Wawrzak; Jialin Liu; W David Nes; Michael R Waterman; Galina I Lepesheva
Journal:  J Biol Chem       Date:  2011-05-31       Impact factor: 5.157

2.  Structural insights into inhibition of sterol 14alpha-demethylase in the human pathogen Trypanosoma cruzi.

Authors:  Galina I Lepesheva; Tatiana Y Hargrove; Spencer Anderson; Yuliya Kleshchenko; Vyacheslav Furtak; Zdzislaw Wawrzak; Fernando Villalta; Michael R Waterman
Journal:  J Biol Chem       Date:  2010-06-08       Impact factor: 5.157

Review 3.  Targeting Trypanosoma cruzi sterol 14α-demethylase (CYP51).

Authors:  Galina I Lepesheva; Fernando Villalta; Michael R Waterman
Journal:  Adv Parasitol       Date:  2011       Impact factor: 3.870

4.  Molecular recognition of receptor sites using a genetic algorithm with a description of desolvation.

Authors:  G Jones; P Willett; R C Glen
Journal:  J Mol Biol       Date:  1995-01-06       Impact factor: 5.469

Review 5.  Mechanism-based enzyme inactivators.

Authors:  R R Rando
Journal:  Pharmacol Rev       Date:  1984-06       Impact factor: 25.468

Review 6.  Chagas' disease: an ecological appraisal with special emphasis on its insect vectors.

Authors:  R Zeledón; J E Rabinovich
Journal:  Annu Rev Entomol       Date:  1981       Impact factor: 19.686

7.  CYP51: A major drug target in the cytochrome P450 superfamily.

Authors:  Galina I Lepesheva; Tatyana Y Hargrove; Yuliya Kleshchenko; W David Nes; Fernando Villalta; Michael R Waterman
Journal:  Lipids       Date:  2008-09-04       Impact factor: 1.880

8.  Effect of CYP3A inhibition on vesnarinone metabolism in humans.

Authors:  C Wandel; C C Lang; D C Cowart; A F Girard; S Bramer; D A Flockhart; A J Wood
Journal:  Clin Pharmacol Ther       Date:  1998-05       Impact factor: 6.875

9.  Inhibitory activity of marine sponge-derived natural products against parasitic protozoa.

Authors:  Ilkay Orhan; Bilge Sener; Marcel Kaiser; Reto Brun; Deniz Tasdemir
Journal:  Mar Drugs       Date:  2010-01-15       Impact factor: 5.118

10.  Trypanosoma cruzi CYP51 inhibitor derived from a Mycobacterium tuberculosis screen hit.

Authors:  Chiung-Kuang Chen; Patricia S Doyle; Liudmila V Yermalitskaya; Zachary B Mackey; Kenny K H Ang; James H McKerrow; Larissa M Podust
Journal:  PLoS Negl Trop Dis       Date:  2009-02-03
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  6 in total

1.  Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.

Authors:  Laura Friggeri; Tatiana Y Hargrove; Zdzislaw Wawrzak; Anna L Blobaum; Girish Rachakonda; Craig W Lindsley; Fernando Villalta; W David Nes; Maurizio Botta; F Peter Guengerich; Galina I Lepesheva
Journal:  J Med Chem       Date:  2018-06-25       Impact factor: 7.446

2.  Efficient electrochemical N-alkylation of N-boc-protected 4-aminopyridines: towards new biologically active compounds.

Authors:  Marta Feroci; Isabella Chiarotto; Gianpiero Forte; Giovanna Simonetti; Felicia Diodata D'Auria; Louis Maes; Daniela De Vita; Luigi Scipione; Laura Friggeri; Roberto Di Santo; Silvano Tortorella
Journal:  ISRN Org Chem       Date:  2014-03-05

Review 3.  Drug strategies targeting CYP51 in neglected tropical diseases.

Authors:  Jun Yong Choi; Larissa M Podust; William R Roush
Journal:  Chem Rev       Date:  2014-10-22       Impact factor: 60.622

4.  Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.

Authors:  Stephen Brand; Eun Jung Ko; Elisabet Viayna; Stephen Thompson; Daniel Spinks; Michael Thomas; Lars Sandberg; Amanda F Francisco; Shiromani Jayawardhana; Victoria C Smith; Chimed Jansen; Manu De Rycker; John Thomas; Lorna MacLean; Maria Osuna-Cabello; Jennifer Riley; Paul Scullion; Laste Stojanovski; Frederick R C Simeons; Ola Epemolu; Yoko Shishikura; Sabrinia D Crouch; Tania S Bakshi; Christopher J Nixon; Iain H Reid; Alan P Hill; Tim Z Underwood; Sean J Hindley; Sharon A Robinson; John M Kelly; Jose M Fiandor; Paul G Wyatt; Maria Marco; Timothy J Miles; Kevin D Read; Ian H Gilbert
Journal:  J Med Chem       Date:  2017-08-27       Impact factor: 7.446

5.  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

6.  Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14α-demethylase: two regions of the enzyme molecule potentiate its inhibition.

Authors:  Laura Friggeri; Tatiana Y Hargrove; Girish Rachakonda; Amanda D Williams; Zdzislaw Wawrzak; Roberto Di Santo; Daniela De Vita; Michael R Waterman; Silvano Tortorella; Fernando Villalta; Galina I Lepesheva
Journal:  J Med Chem       Date:  2014-07-29       Impact factor: 7.446
  6 in total

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