scholarly journals Organic Salts Based on Isoniazid Drug: Synthesis, Bioavailability and Cytotoxicity Studies

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 952
Author(s):  
Filipa Santos ◽  
Luís C. Branco ◽  
Ana Rita C. Duarte
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Organic Cation ◽  
Mycobacterium Tuberculosis Complex ◽  
Tuberculosis Complex ◽  
Organic Salts ◽  
Cytotoxicity Studies ◽  
Drug Regimens ◽  
Drug Synthesis ◽  
Polymorphic Forms

Tuberculosis is one of the ten causes of morbidity and mortality worldwide caused by Mycobacterium tuberculosis complex. Some of the anti-tuberculosis drugs used in clinic studies, despite being effective for the treatment of tuberculosis, present serious adverse effects as well as poor bioavailability, stability, and drug-resistance problems. Thus, it is important to develop approaches that could provide shorter drug regimens, preventing drug resistance, toxicity of the antibiotics, and improve their bioavailability. Herein, we reported the use of organic salts based on the isoniazid drug, which can act as an organic cation combined with suitable organic anions such as alkylsulfonate-based (mesylate, R or S-Camphorsulfonate), carboxylate-based (glycolate, vanylate) and sacharinate. The synthesis, characterization, and cytotoxicity studies comparing with the original isoniazid drug have been performed. The possibility to explore dicationic salts seems promising in order to improve original bioavailability, and promote the elimination of polymorphic forms as well as higher stability, which are relevant characteristics that the pharmaceutical industry pursues.

scholarly journals Diversified lineages and drug-resistance profiles of clinical isolates of Mycobacterium tuberculosis complex in Malaysia

2019 ◽  
Vol 8 (4) ◽  
pp. 320
Author(s):  
MohdSalleh Zaki ◽  
MohdNur Noorizhab Fakhruzzaman ◽  
NorzulianaZainal Abidin ◽  
ZirwatulAdilah Aziz ◽  
WaiFeng Lim ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Mycobacterium Tuberculosis Complex ◽  
Clinical Isolates ◽  
Tuberculosis Complex

scholarly journals Drug Resistance of Mycobacterium tuberculosis Complex in a Rural Setting, Angola

2018 ◽  
Vol 24 (3) ◽  
pp. 569-572 ◽  
Author(s):  
Ariadna Rando-Segura ◽  
María Luisa Aznar ◽  
María Milagros Moreno ◽  
Mateu Espasa ◽  
Elena Sulleiro ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Mycobacterium Tuberculosis Complex ◽  
Rural Setting ◽  
Tuberculosis Complex

scholarly journals Drug Resistance of Mycobacterium tuberculosis Complex in a Rural Setting, Angola

2018 ◽  
Vol 24 (3) ◽  
pp. 569-572
Author(s):  
Ariadna Rando-Segura ◽  
María Luisa Aznar ◽  
María Milagros Moreno ◽  
Mateu Espasa ◽  
Elena Sulleiro ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Mycobacterium Tuberculosis Complex ◽  
Rural Setting ◽  
Tuberculosis Complex

scholarly journals Sequence analysis for detection of drug resistance in Mycobacterium tuberculosis complex isolates from the Central Region of Cameroon

2014 ◽  
Vol 14 (1) ◽  
pp. 113 ◽  
Author(s):  
Emmanuel Tekwu ◽  
Larissa Sidze ◽  
Jean-Paul Assam ◽  
Jean-Claude Tedom ◽  
Serges Tchatchouang ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Sequence Analysis ◽  
Central Region ◽  
Mycobacterium Tuberculosis Complex ◽  
Tuberculosis Complex

scholarly journals Genetic Diversity and Drug Resistance of Mycobacterium tuberculosis Complex Isolates and Nontuberculous Mycobacteria Identification from Presumptive Tuberculosis Cases in Oaxaca, Mexico

2020 ◽  
Vol 16 (1) ◽  
pp. 7-19
Author(s):  
Nakamura-Lopez Yuko ◽  
Valencia-Carmona Oscar Daniel ◽  
Martinez-Cruz Perla Monica ◽  
Palma-Nicolas Jose Prisco ◽  
Gonzalez-y-Merchand Jorge Alberto ◽  
...  
Keyword(s):  
Genetic Diversity ◽  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Mycobacterium Tuberculosis Complex ◽  
Nontuberculous Mycobacteria ◽  
Tuberculosis Complex

scholarly journals Mutations associated with pyrazinamide resistance in pncA of Mycobacterium tuberculosis complex organisms.

1997 ◽  
Vol 41 (3) ◽  
pp. 636-640 ◽  
Author(s):  
S Sreevatsan ◽  
X Pan ◽  
Y Zhang ◽  
B N Kreiswirth ◽  
J M Musser
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Amino Acid ◽  
Amino Acid Sequence ◽  
Mycobacterium Tuberculosis Complex ◽  
Tuberculosis Complex ◽  
Primary Amino Acid Sequence ◽  
Primary Amino ◽  
Nucleotide Insertions ◽  
Striking Contrast

A gene (pncA) with mutations associated with pyrazinamide resistance in Mycobacterium tuberculosis complex members was characterized in 67 pyrazinamide-resistant and 51 pyrazinamide-susceptible isolates recovered from diverse geographic localities and anatomic sites and typed by IS6110 profiling. All pyrazinamide-susceptible organisms had identical pncA alleles. In striking contrast, 72% of the 67 resistant organisms had pncA mutations that altered the primary amino acid sequence of pyrazinamidase. A total of 17 previously undescribed mutations were found, including upstream mutations, missense changes, nucleotide insertions and deletions, and termination mutations. The mutations were arrayed along virtually the entire length of the gene. These data are further evidence that most drug resistance in M. tuberculosis is due to simple mutations occurring in chromosomally encoded genes rather than to acquisition of resistance genes by horizontal transfer events.

scholarly journals Polymorphisms in Isoniazid and Prothionamide Resistance Genes of the Mycobacterium tuberculosis Complex

2011 ◽  
Vol 55 (9) ◽  
pp. 4408-4411 ◽  
Author(s):  
Michaela Projahn ◽  
Claudio U. Köser ◽  
Susanne Homolka ◽  
David K. Summers ◽  
John A. C. Archer ◽  
...  
Keyword(s):  
Genetic Diversity ◽  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Resistance Genes ◽  
Mycobacterium Tuberculosis Complex ◽  
Tuberculosis Complex ◽  
Sequence Analyses ◽  
Content Type ◽  
Molecular Tests ◽  
Phylogenetic Lineages

ABSTRACTSequence analyses of 74 strains that encompassed major phylogenetic lineages of theMycobacterium tuberculosiscomplex revealed 10 polymorphisms inmshA(Rv0486) and four polymorphisms ininhA(Rv1484) that were not responsible for isoniazid or prothionamide resistance. Instead, some of these mutations were phylogenetically informative. This genetic diversity must be taken into consideration for drug development and for the design of molecular tests for drug resistance.

scholarly journals Evaluation of susceptibility to antimycobacterial drugs in Mycobacterium tuberculosis complex strains isolated from cattle in Poland

2017 ◽  
Vol 61 (1) ◽  
pp. 23-26 ◽  
Author(s):  
Monika Krajewska-Wędzina ◽  
Anna Zabost ◽  
Ewa Augustynowicz-Kopeć ◽  
Marcin Weiner ◽  
Krzysztof Szulowski
Keyword(s):  
Drug Resistance ◽  
Mycobacterium Tuberculosis ◽  
Mycobacterium Tuberculosis Complex ◽  
Natural Resistance ◽  
Microbiological Analysis ◽  
Tuberculosis Complex ◽  
First Line ◽  
Eradication Programme ◽  
Dynamic Changes ◽  
Environmental Resistance

Abstract Introduction: Tuberculosis is a highly infectious disease affecting humans and animals. It is caused by the Mycobacterium tuberculosis complex (MTBC) – Mycobacterium bovis and Mycobacterium caprae, which are aetiological factors of bovine tuberculosis (bTB). In Poland, the bTB eradication programme exists. Animals diagnosed with tuberculosis are in the majority of cases not treated, but removed from their herd and then sanitary slaughtered. Material and Methods: In total, 134 MTBC strains isolated from cattle in Poland were subjected to microbiological analysis. The resistance phenotype was tested for first-line antimycobacterial drugs used in tuberculosis treatment in humans: streptomycin, isoniazid, rifampicin, ethambutol, and pyrazinamide. The strains were isolated from tissues collected post mortem, so the test for drug resistance fulfilled only epidemiological criterion. Results: The analysis of drug-resistance of MTBC strains revealed that strains classified as M. bovis were susceptible to 4 antimycobacterial drugs: isoniazid, rifampicin, streptomycin, and ethambutol, and resistant to pyrazynamide. The strains classified as M. caprae were sensitive to all tested drugs. Conclusion: The results indicate that despite enormously dynamic changes in mycobacterial phenotype, Polish strains of MTBC isolated from cattle have not acquired environmental resistance. The strains classified as M. bovis are characterised by natural resistance to pyrazinamide, which is typical for this species.

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