scholarly journals New Antituberculosis Drug FS-1

Author(s):  
Rinat Islamov ◽  
Bahkytzhan Kerimzhanova ◽  
Alexander Ilin
2017 ◽  
Vol 17 (19) ◽  
pp. 2129-2142 ◽  
Author(s):  
Renata Płocinska ◽  
Malgorzata Korycka-Machala ◽  
Przemyslaw Plocinski ◽  
Jaroslaw Dziadek

Background: Mycobacterium tuberculosis (M. tuberculosis), the causative agent of tuberculosis, is a leading infectious disease organism, causing millions of deaths each year. This serious pathogen has been greatly spread worldwide and recent years have observed an increase in the number of multi-drug resistant and totally drug resistant M. tuberculosis strains (WHO report, 2014). The danger of tuberculosis becoming an incurable disease has emphasized the need for the discovery of a new generation of antimicrobial agents. The development of novel alternative medical strategies, new drugs and the search for optimal drug targets are top priority areas of tuberculosis research. Factors: Key characteristics of mycobacteria include: slow growth, the ability to transform into a metabolically silent - latent state, intrinsic drug resistance and the relatively rapid development of acquired drug resistance. These factors make finding an ideal antituberculosis drug enormously challenging, even if it is designed to treat drug sensitive tuberculosis strains. A vast majority of canonical antibiotics including antituberculosis agents target bacterial cell wall biosynthesis or DNA/RNA processing. Novel therapeutic approaches are being tested to target mycobacterial cell division, twocomponent regulatory factors, lipid synthesis and the transition between the latent and actively growing states. Discussion and Conclusion: This review discusses the choice of cellular targets for an antituberculosis therapy, describes putative drug targets evaluated in the recent literature and summarizes potential candidates under clinical and pre-clinical development. We focus on the key cellular process of DNA replication, as a prominent target for future antituberculosis therapy. We describe two main pathways: the biosynthesis of nucleic acids precursors – the nucleotides, and the synthesis of DNA molecules. We summarize data regarding replication associated proteins that are critical for nucleotide synthesis, initiation, unwinding and elongation of the DNA during the replication process. They are pivotal processes required for successful multiplication of the bacterial cells and hence they are extensively investigated for the development of antituberculosis drugs. Finally, we summarize the most potent inhibitors of DNA synthesis and provide an up to date report on their status in the clinical trials.


2019 ◽  
Vol 8 (16) ◽  
Author(s):  
Aleksey A. Vatlin ◽  
Kirill V. Shur ◽  
Valery N. Danilenko ◽  
Dmitry A. Maslov

Here, we report 12 draft genome sequences of mutant Mycolicibacterium smegmatis strains resistant to imidazo[1,2-b][1,2,4,5]tetrazines, which are antituberculosis drug candidates. We have identified 7 different mutations in the MSMEG_1380 gene, which encodes the AcrR/TetR_N transcriptional repressor, which may activate efflux-mediated resistance.


Heliyon ◽  
2021 ◽  
Vol 7 (4) ◽  
pp. e06852
Author(s):  
Noppadol Chanhom ◽  
Sukanya Wattanapokayakit ◽  
Nusara Satproedprai ◽  
Supharat Suvichapanich ◽  
Surakameth Mahasirimongkol ◽  
...  

2012 ◽  
Vol 68 (4) ◽  
pp. o1205-o1205
Author(s):  
Andreas Lemmerer ◽  
Joel Bernstein ◽  
Volker Kahlenberg

The title compound, C18H27N3O, is a derivative of the antituberculosis drug isoniazid (systematic name: pyridine-4-carbohydrazidei). The crystal structure consists of repeatingC(4) chains along thebaxis, formed by N—H...O hydrogen bonds with adjacent amide functional groups that are related by ab-glide plane. The cyclododecyl ring has the same approximately `square' conformation, as seen in the parent hydrocarbon cyclododecane.


2013 ◽  
Vol 28 (8) ◽  
pp. 1368-1374 ◽  
Author(s):  
Vinod H Gupta ◽  
Deepak N Amarapurkar ◽  
Meenakshi Singh ◽  
Preetha Sasi ◽  
Jyotsna M Joshi ◽  
...  

2017 ◽  
Vol 48 ◽  
pp. 94-101 ◽  
Author(s):  
Jennifer Herrmann ◽  
Jan Rybniker ◽  
Rolf Müller

2014 ◽  
Vol 43 (2) ◽  
pp. 166-172 ◽  
Author(s):  
Samuel Sasu ◽  
Jörg Metzger ◽  
Martin Kranert ◽  
Klaus Kümmerer

2015 ◽  
Vol 105 (5) ◽  
pp. 393 ◽  
Author(s):  
S Naidoo ◽  
D Evans ◽  
E Jong ◽  
K Mellet ◽  
R Berhanu

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