scholarly journals Benzothiazinone-piperazine derivatives as efficient Mycobacterium tuberculosis DNA gyrase inhibitors

2015 ◽  
Vol 4 (2) ◽  
pp. 104-115 ◽  
Author(s):  
Manoj Chandran ◽  
Janupally Renuka ◽  
Jonnalagadda Padma Sridevi ◽  
Ganesh S. Pedgaonkar ◽  
Vanaparthi Asmitha ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Dna Gyrase ◽  
Piperazine Derivatives ◽  
Gyrase Inhibitors

scholarly journals A Mycobacterium tuberculosis NBTI DNA gyrase inhibitor is active against Mycobacterium abscessus

2021 ◽  
Author(s):  
Uday S. Ganapathy ◽  
Rubén González del Río ◽  
Mónica Cacho-Izquierdo ◽  
Fátima Ortega ◽  
Joël Lelièvre ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Low Frequency ◽  
Dna Gyrase ◽  
Resistant Mutant ◽  
Mycobacterium Abscessus ◽  
Mutant Selection ◽  
Intrinsic Drug Resistance ◽  
Lung Infections ◽  
Gyrase Inhibitors

Fluoroquinolones – the only clinically used DNA gyrase inhibitors – are effective against tuberculosis (TB) but are in limited clinical use for non-tuberculous mycobacteria (NTM) lung infections due to intrinsic drug resistance. We sought to test alternative DNA gyrase inhibitors for anti-NTM activity. Mycobacterium tuberculosis Gyrase Inhibitors (MGIs), a subclass of Novel Bacterial Topoisomerase Inhibitors (NBTIs), were recently shown to be active against the tubercle bacillus. Here, we show that the MGI EC/11716 not only has potent anti-tubercular activity but is active against M. abscessus and M. avium in vitro . Focusing on M. abscessus , which causes the most difficult to cure NTM disease, we show that EC/11716 is bactericidal, active against drug-tolerant biofilms, and efficacious in a murine model of M. abscessus lung infection. Based on resistant mutant selection experiments, we report a low frequency of resistance to EC/11716 and confirm DNA gyrase as its target. Our findings demonstrate the potential of NBTIs as anti- M. abscessus and possibly broad spectrum anti-mycobacterial agents.

Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors

2016 ◽  
Vol 24 (4) ◽  
pp. 877-885 ◽  
Author(s):  
Brahmam Medapi ◽  
Nikhila Meda ◽  
Pushkar Kulkarni ◽  
Perumal Yogeeswari ◽  
Dharmarajan Sriram
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Dna Gyrase ◽  
Acridine Derivatives ◽  
Gyrase Inhibitors

scholarly journals Design and synthesis of new 3-((7-chloroquinolin-4-yl)amino)thiazolidin-4-one analogs as Mycobacterium tuberculosis DNA gyrase inhibitors

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Preeti S. Salve ◽  
Prajakta Parchure ◽  
Lisel Araujo ◽  
Rohini S. Kavalapure ◽  
Sunil S. Jalalpure ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Mycobacterium Smegmatis ◽  
Dna Gyrase ◽  
Docking Studies ◽  
Human Populations ◽  
Antitubercular Agents ◽  
Major Health ◽  
Design And Synthesis ◽  
Gyrase Inhibitors

Abstract Background Tuberculosis is evidently a major health threat among human populations worldwide. The current study presents the synthesis of new 3-((7-chloroquinolin-4-yl)amino)thiazolidin-4-one analogs (4a–o) as potential Mycobacterium tuberculosis DNA gyrase inhibitors. DNA gyrase regulates DNA topology in MTB and has been a target of choice for antibacterial therapy. With this in mind, the synthesized derivatives (4a–o) were subjected to in vitro antitubercular evaluation by the MABA method and were tested for MTB DNA gyrase inhibition by supercoiling assay. Results All the synthesized compounds displayed inhibition of MTB within the MIC range of 1.56–12.5 μM. Further, out of the selected compounds that underwent DNA gyrase inhibition, compound 4o proved to be a potent lead molecule by displaying 82% of enzyme inhibition at 1 μM. All the synthesized derivatives also underwent molecular docking studies to comprehend their hypothetical binding interactions with Mycobacterium smegmatis GyrB. Conclusion All the results suggested that most of the synthesized derivatives inhibited Mycobacterium tuberculosis, and some 3-((7-chloroquinolin-4-yl)amino)thiazolidin-4-one analogs could act as leads for the development of antitubercular agents.

New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors

2017 ◽  
Vol 27 (5) ◽  
pp. 1162-1168 ◽  
Author(s):  
Hülya Karaca Gençer ◽  
Serkan Levent ◽  
Ulviye Acar Çevik ◽  
Yusuf Özkay ◽  
Sinem Ilgın
Keyword(s):  
Dna Gyrase ◽  
Gyrase Inhibitors

Synthesis and antibacterial activity of a novel series of DNA gyrase inhibitors: 5-[(E)-2-arylvinyl]pyrazoles

2005 ◽  
Vol 15 (19) ◽  
pp. 4299-4303 ◽  
Author(s):  
Akihiko Tanitame ◽  
Yoshihiro Oyamada ◽  
Keiko Ofuji ◽  
Hideo Terauchi ◽  
Motoji Kawasaki ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Dna Gyrase ◽  
Gyrase Inhibitors

Synthesis, Antimicrobial Evaluation, and Docking Studies of Novel 4-Substituted Quinazoline Derivatives as DNA-Gyrase Inhibitors

2010 ◽  
Vol 343 (10) ◽  
pp. 570-576 ◽  
Author(s):  
Shireesha Boyapati ◽  
Umasankar Kulandaivelu ◽  
Srinivas Sangu ◽  
Malla Reddy Vanga
Keyword(s):  
Dna Gyrase ◽  
Docking Studies ◽  
Antimicrobial Evaluation ◽  
Quinazoline Derivatives ◽  
Gyrase Inhibitors

ChemInform Abstract: A Concise, Practical Synthesis of the Pyrido(3.2.1-ij)cinnoline Ring System of Potent DNA Gyrase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 26 (46) ◽  
pp. no-no
Author(s):  
D. BARRETT ◽  
H. SASAKI ◽  
H. TSUTSUMI ◽  
M. MURATA ◽  
T. TERASAWA ◽  
...  
Keyword(s):  
Dna Gyrase ◽  
Ring System ◽  
Practical Synthesis ◽  
Gyrase Inhibitors

scholarly journals Synthesis, Characterization and in vitro Antimicrobial Evaluation of Chalconeimine Derivatives as Potential Inhibitors against Enzymes Produced from S. aureus: A Computational Approach

2019 ◽  
Vol 31 (10) ◽  
pp. 2157-2164
Author(s):  
B. Prithivirajan ◽  
M. Jebastin Sonia Jas ◽  
G. Marimuthu
Keyword(s):  
Antibacterial Agents ◽  
Dna Gyrase ◽  
Bacterial Strains ◽  
Bacterial Proteins ◽  
Antibiotic Drug ◽  
In Vitro Antibacterial Activity ◽  
Antimicrobial Evaluation ◽  
Potential Inhibitors ◽  
Gyrase Inhibitors

(Z)-1-(Benzo[d][1,3]dioxol-5-yl)-3-(4-(difluoromethoxy)-3-hydroxyphenyl)prop-2-en-1-one hydrazone derivatives pronounced in this manuscript represents a new collection of antibacterial agents in addition to the DNA gyrase inhibitors. Efforts had been made to synthesize those chalcone-hydrazone derivatives (4a-e) in good yields. The literature survey confirms that nano-ZnO as heterogeneous catalyst has obtained big interest because of its ecofriendly nature and has been explored as a effective catalyst for several organic ameliorations. Subsequently, induced by way of these observations and in continuation to our interest in organic synthesis with using nanocatalyst. in vitro Antibacterial activity has been evaluated towards Gram-positive and Gram-negative bacterial strains for all compounds. So one can discover the affinity to bacterial proteins docking have a look at have been carried out for 5 synthesized derivatives, antibiotic drug and co-crystallized ligands with special mechanism of action DNA gyrase B and methylthioadenosine/S-adenosylhomocysteine nucleosidase (MTAN) the usage of AutoDock 4.

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