Literature DB >> 1560435

Antimycobacterial activity of a series of pyrazinoic acid esters.

M H Cynamon1, S P Klemens, T S Chou, R H Gimi, J T Welch.   

Abstract

A series of pyrazinoic acid esters has been prepared and evaluated for in vitro antimycobacterial activity. Several of the pyrazinoate esters have substantially better activity than the first-line antituberculous agent pyrazinamide against susceptible isolates of Mycobacterium turberculosis as well as activity against pyrazinamide-resistant isolates. The minimal inhibitory concentrations (MICs) were lower for each organism and at each pH than the MICs for pyrazinamide. The esters have activity against Mycobacterium bovis and Mycobacterium kansasii, two species resistant to pyrazinamide, but not against Mycobacterium avium complex.

Entities:  

Mesh:

Substances:

Year:  1992        PMID: 1560435     DOI: 10.1021/jm00085a007

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  22 in total

1.  Inhaled Pyrazinoic Acid Esters for the Treatment of Tuberculosis.

Authors:  E F Young; E Perkowski; S Malik; J D Hayden; P G Durham; L Zhong; J T Welch; Miriam S Braunstein; Anthony J Hickey
Journal:  Pharm Res       Date:  2016-06-28       Impact factor: 4.200

2.  Esters of Pyrazinoic Acid Are Active against Pyrazinamide-Resistant Strains of Mycobacterium tuberculosis and Other Naturally Resistant Mycobacteria In Vitro and Ex Vivo within Macrophages.

Authors:  David Pires; Emília Valente; Marta Filipa Simões; Nuno Carmo; Bernard Testa; Luís Constantino; Elsa Anes
Journal:  Antimicrob Agents Chemother       Date:  2015-10-05       Impact factor: 5.191

3.  The antituberculosis drug pyrazinamide affects the course of cutaneous leishmaniasis in vivo and increases activation of macrophages and dendritic cells.

Authors:  Susana Mendez; Ryan Traslavina; Meleana Hinchman; Lu Huang; Patricia Green; Michael H Cynamon; John T Welch
Journal:  Antimicrob Agents Chemother       Date:  2009-09-21       Impact factor: 5.191

4.  High Systemic Exposure of Pyrazinoic Acid Has Limited Antituberculosis Activity in Murine and Rabbit Models of Tuberculosis.

Authors:  Jean-Philippe Lanoix; Rokeya Tasneen; Paul O'Brien; Jansy Sarathy; Hassan Safi; Michael Pinn; David Alland; Véronique Dartois; Eric Nuermberger
Journal:  Antimicrob Agents Chemother       Date:  2016-06-20       Impact factor: 5.191

5.  Inhibition of isolated Mycobacterium tuberculosis fatty acid synthase I by pyrazinamide analogs.

Authors:  Silvana C Ngo; Oren Zimhony; Woo Jin Chung; Halimah Sayahi; William R Jacobs; John T Welch
Journal:  Antimicrob Agents Chemother       Date:  2007-05-07       Impact factor: 5.191

6.  Activity of n-propyl pyrazinoate against pyrazinamide-resistant Mycobacterium tuberculosis: investigations into mechanism of action of and mechanism of resistance to pyrazinamide.

Authors:  R J Speirs; J T Welch; M H Cynamon
Journal:  Antimicrob Agents Chemother       Date:  1995-06       Impact factor: 5.191

7.  Ester-prodrugs of ethambutol control its antibacterial activity and provide rapid screening for mycobacterial hydrolase activity.

Authors:  Erik M Larsen; Dominique C Stephens; Nathan H Clarke; R Jeremy Johnson
Journal:  Bioorg Med Chem Lett       Date:  2017-08-30       Impact factor: 2.823

8.  Emergence of potential superbug mycobacterium tuberculosis, lessons from new delhi mutant-1 bacterial strains.

Authors:  Taha Nazir; Suraj Abraham; Azharul Islam
Journal:  Int J Health Sci (Qassim)       Date:  2012-01

Review 9.  Microbial esterases and ester prodrugs: An unlikely marriage for combating antibiotic resistance.

Authors:  Erik M Larsen; R Jeremy Johnson
Journal:  Drug Dev Res       Date:  2018-10-10       Impact factor: 4.360

Review 10.  Why Wait? The Case for Treating Tuberculosis with Inhaled Drugs.

Authors:  Miriam Braunstein; Anthony J Hickey; Sean Ekins
Journal:  Pharm Res       Date:  2019-10-24       Impact factor: 4.200

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.