Literature DB >> 32435364

Improving the Potency of N-Aryl-2,5-dimethylpyrroles against Multidrug-Resistant and Intracellular Mycobacteria.

Meir Touitou1,2, Fabrizio Manetti3, Camila Maringolo Ribeiro4, Fernando Rogerio Pavan4, Nicolò Scalacci1, Katarina Zrebna1, Neelu Begum5, Dorothy Semenya1, Antima Gupta6, Sanjib Bhakta6, Timothy D McHugh5, Hanoch Senderowitz2, Melina Kyriazi1, Daniele Castagnolo1.   

Abstract

A series of N-phenyl-2,5-dimethylpyrrole derivatives, designed as hybrids of the antitubercular agents BM212 and SQ109, have been synthesized and evaluated against susceptible and drug-resistant mycobacteria strains. Compound 5d, bearing a cyclohexylmethylene side chain, showed high potency against M. tuberculosis including MDR-TB strains at submicromolar concentrations. The new compound shows bacteriostatic activity and low toxicity and proved to be effective against intracellular mycobacteria too, showing an activity profile similar to isoniazid.
Copyright © 2019 American Chemical Society.

Entities:  

Year:  2019        PMID： 32435364      PMCID： PMC7236041          DOI： 10.1021/acsmedchemlett.9b00515

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


  23 in total

1.  Building a pharmacophore model for a novel class of antitubercular compounds.

Authors:  F Manetti; F Corelli; M Biava; R Fioravanti; G C Porretta; M Botta
Journal:  Farmaco       Date:  2000 Jun-Jul

2.  Intracellular growth and drug susceptibility of Mycobacterium tuberculosis in macrophages.

Authors:  Sakarin Chanwong; Niwat Maneekarn; Luksana Makonkawkeyoon; Sanit Makonkawkeyoon
Journal:  Tuberculosis (Edinb)       Date:  2006-07-21       Impact factor: 3.131

Review 3.  Mycobacterium tuberculosis: immune evasion, latency and reactivation.

Authors:  Antima Gupta; Akshay Kaul; Anthony G Tsolaki; Uday Kishore; Sanjib Bhakta
Journal:  Immunobiology       Date:  2011-07-18       Impact factor: 3.144

4.  Ligand-based virtual screening, parallel solution-phase and microwave-assisted synthesis as tools to identify and synthesize new inhibitors of mycobacterium tuberculosis.

Authors:  Fabrizio Manetti; Matteo Magnani; Daniele Castagnolo; Laura Passalacqua; Maurizio Botta; Federico Corelli; Manuela Saddi; Delia Deidda; Alessandro De Logu
Journal:  ChemMedChem       Date:  2006-09       Impact factor: 3.466

5.  Novel insights into the mechanism of inhibition of MmpL3, a target of multiple pharmacophores in Mycobacterium tuberculosis.

Authors:  Wei Li; Ashutosh Upadhyay; Fabio L Fontes; E Jeffrey North; Yuehong Wang; Debbie C Crans; Anna E Grzegorzewicz; Victoria Jones; Scott G Franzblau; Richard E Lee; Dean C Crick; Mary Jackson
Journal:  Antimicrob Agents Chemother       Date:  2014-08-18       Impact factor: 5.191

Review 6.  Studies on the treatment of tuberculosis undertaken by the British Medical Research Council tuberculosis units, 1946-1986, with relevant subsequent publications.

Authors:  W Fox; G A Ellard; D A Mitchison
Journal:  Int J Tuberc Lung Dis       Date:  1999-10       Impact factor: 2.373

7.  Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models.

Authors:  Anne J Lenaerts; Veronica Gruppo; Karen S Marietta; Christine M Johnson; Diane K Driscoll; Nicholas M Tompkins; Jerry D Rose; Robert C Reynolds; Ian M Orme
Journal:  Antimicrob Agents Chemother       Date:  2005-06       Impact factor: 5.191

Review 8.  Tuberculosis: progress and advances in development of new drugs, treatment regimens, and host-directed therapies.

Authors:  Simon Tiberi; Nelita du Plessis; Gerhard Walzl; Michael J Vjecha; Martin Rao; Francine Ntoumi; Sayoki Mfinanga; Nathan Kapata; Peter Mwaba; Timothy D McHugh; Giuseppe Ippolito; Giovanni Battista Migliori; Markus J Maeurer; Alimuddin Zumla
Journal:  Lancet Infect Dis       Date:  2018-03-23       Impact factor: 25.071

9.  Multidrug- and extensively drug-resistant tuberculosis, Germany.

Authors:  Barbara Eker; Johannes Ortmann; Giovanni B Migliori; Giovanni Sotgiu; Ralf Muetterlein; Rosella Centis; Harald Hoffmann; Detlef Kirsten; Tom Schaberg; Sabine Ruesch-Gerdes; Christoph Lange
Journal:  Emerg Infect Dis       Date:  2008-11       Impact factor: 6.883

10.  Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.

Authors:  Guilherme Felipe Dos Santos Fernandes; Paula Carolina de Souza; Elsa Moreno-Viguri; Mery Santivañez-Veliz; Rocio Paucar; Silvia Pérez-Silanes; Konstantin Chegaev; Stefano Guglielmo; Loretta Lazzarato; Roberta Fruttero; Chung Man Chin; Patricia Bento da Silva; Marlus Chorilli; Mariana Cristina Solcia; Camila Maríngolo Ribeiro; Caio Sander Paiva Silva; Leonardo Biancolino Marino; Priscila Longhin Bosquesi; Debbie M Hunt; Luiz Pedro S de Carvalho; Carlos Alberto de Souza Costa; Sang Hyun Cho; Yuehong Wang; Scott Gary Franzblau; Fernando Rogério Pavan; Jean Leandro Dos Santos
Journal:  J Med Chem       Date:  2017-10-16       Impact factor: 7.446
View more
  2 in total

1.  Structural Rigidification of N-Aryl-pyrroles into Indoles Active against Intracellular and Drug-Resistant Mycobacteria.

Authors:  Dorothy Semenya; Meir Touitou; Camila Maringolo Ribeiro; Fernando Rogerio Pavan; Luca Pisano; Vinayak Singh; Kelly Chibale; Georg Bano; Anita Toscani; Fabrizio Manetti; Beatrice Gianibbi; Daniele Castagnolo
Journal:  ACS Med Chem Lett       Date:  2021-12-08       Impact factor: 4.345

2.  The greater wax moth Galleria mellonella: biology and use in immune studies.

Authors:  Iwona Wojda; Bernard Staniec; Michał Sułek; Jakub Kordaczuk
Journal:  Pathog Dis       Date:  2020-11-23       Impact factor: 3.166
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.