Results 211 to 220 of about 64,020 (238)

Efficacy and Mode of Action of a Direct Inhibitor of Mycobacterium abscessus InhA.

ACS Infectious Diseases, 2022
There is an unmet medical need for effective treatments against Mycobacterium abscessus pulmonary infections, to which cystic fibrosis (CF) patients are particularly vulnerable.
Matthéo Alcaraz, Françoise Roquet-Banères, S. Leon-Icaza, J. Abendroth, Yves-Marie Boudehen, C. Cougoule, T. Edwards, L. Kremer   +7 more
semanticscholar   +1 more source

Novel compounds targeting InhA for TB therapy

Pharmacological Reports, 2018
Tuberculosis (TB) is described as lethal disease in the world. Resistant to TB drugs is the main reason to have unfavourable outcomes in the treatment of TB. Therefore, new agents to replace existing drugs are urgently needed. Previous reports suggested that InhA inhibitors, an enoyl-ACP-reductase, might provide auspicious candidates which can be ...
Manaf, AlMatar, Essam A, Makky, Işıl, Var, Begüm, Kayar, Fatih, Köksal   +4 more
openaire   +2 more sources

Novel diaryl ether derivatives as InhA inhibitors: Design, synthesis and antimycobacterial activity.

Bioorganic chemistry (Print), 2022
A new series of triclosan (TCL)-mimicking diaryl ether derivatives 7-25 were synthesized and evaluated as inhibitors of enoyl acyl carrier protein reductase InhA enzyme. In addition, these derivatives were screened as inhibitors of drug-susceptible (DS),
O. A. Abdelaziz, D. Othman, M. Abdel-Aziz, Sahar M. I. Badr, H. Eisa   +4 more
semanticscholar   +1 more source

Is Mycobacterial InhA a Suitable Target for Rational Drug Design?

ChemMedChem
InhA, an NAD‐dependent enoyl‐acyl carrier protein reductase, is involved in the biosynthesis of mycolic acids, specific lipids to mycobacteria. InhA is the target of isoniazid, a first‐line antituberculosis drug used since the 1950s.
Julien Rizet, L. Maveyraud, D. Rengel, V. Guillet, Gabriel Publicola, Frédéric Rodriguez, C. Lherbet, Lionel Mourey   +7 more
semanticscholar   +1 more source

Identification of new anti-mycobacterial agents based on quinoline-isatin hybrids targeting enoyl acyl carrier protein reductase (InhA).

Bioorganic chemistry (Print)
Tuberculosis (TB) is a global issue that poses a significant economic burden as a result of the ongoing emergence of drug-resistant strains. The urgent requirement for the development of novel antitubercular drugs can be addressed by targeting specific ...
E. F. Khaleel, Ahmed Sabt, M. Korycka-Machała, R. Badi, Ninh The Son, Nguyen Xuan Ha, Mohamed Farouk Hamissa, Ahmed E Elsawi, E. Elkaeed, B. Dziadek, Wagdy M. Eldehna, J. Dziadek   +11 more
semanticscholar   +1 more source

Synthesis and in vitro studies for structure-based design of novel chalcones as antitubercular agents targeting InhA.

Future Medicinal Chemistry, 2022
Background: The authors aimed to estimate the therapeutic potential of novel chalcones against tuberculosis. Methods: 11 synthesized compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis (H37RV; American Type ...
L. S. Dhivya, B. R. Pradeepa, S. Sarvesh
semanticscholar   +1 more source

Molecular dynamics-based investigation of InhA substrate binding loop for diverse biological activity of direct InhA inhibitors

Journal of Biomolecular Structure and Dynamics, 2016
The closed conformation of substrate binding loop (SBL) is considered significant for biological activity of direct InhA inhibitors (DIIs). However, exact interactions of SBL with inhibitors are not characterized yet to emphasize over SBL conformations.
Vivek, Kumar, M Elizabeth, Sobhia
openaire   +2 more sources

The first-in-class pyrazole-based dual InhA-VEGFR inhibitors towards integrated antitubercular host-directed therapy.

Bioorganic chemistry (Print)
Several facets of the host response to tuberculosis have been tapped for clinical investigation, especially targeting angiogenesis mediated by VEGF signaling from infected macrophages. Herein, we rationalized combining the antiangiogenic effects of VEGFR-
Marwa M Shaaban, Mohamed Teleb, Hanan M. Ragab, Monica Singh, Bassma H. Elwakil, Lamia A Heikal, D. Sriram, M. Mahran   +7 more
semanticscholar   +1 more source

New coumarin linked thiazole derivatives as antimycobacterial agents: Design, synthesis, enoyl acyl carrier protein reductase (InhA) inhibition and molecular modeling.

Bioorganic chemistry (Print)
Tuberculosis is a global serious problem that imposes major health, economic and social challenges worldwide. The search for new antitubercular drugs is extremely important which could be achieved via inhibition of different druggable targets ...
A. Kassem, Ahmed Sabt, M. Korycka-Machała, Moataz A. Shaldam, M. Kawka, B. Dziadek, M. Kuzioła, J. Dziadek, Rasha Z. Batran   +8 more
semanticscholar   +1 more source

Association analysis between reproduction genes INHA, PGR, RARG with lamb and other traits of Liaoning cashmere goats

Animal Biotechnology, 2022
Reproductive traits have a high economic value in goat breeding, and increasing the number of lambs produced by ewes is of great importance to improve the production efficiency of goat farming.
Rui Chen, Jichang Liu, Yurou Zhang, Wei Cai, Xinjiang Zhang, Yanan Xu, Xingtang Dou, Zhanhong Wang, Di Han, Jiaming Wang, Guangyu Lin, Lingling Wang, Ying Sun, Zhi-chuan Bai, M. Gu, Zeying Wang   +15 more
semanticscholar   +1 more source