Journal ArticleDOI
Triazole derivatives and their anti-tubercular activity
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TLDR
Molecules containing triazole moiety may show promising in vitro and in vivo anti-TB activities and might be able to prevent the drug resistant to certain extent.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2017-09-29. It has received 327 citations till now. The article focuses on the topics: Population.read more
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1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
Zhi Xu,Shi‐Jia Zhao,Yi Liu +2 more
TL;DR: This review emphasizes the recent advances in 1,2,3-triazole-containing hybrids with anticancer potential, covering articles published between 2015 and 2019, and the structure-activity relationships, together with mechanisms of action are discussed.
Journal ArticleDOI
Quinoline hybrids and their antiplasmodial and antimalarial activities.
TL;DR: This review aims to summarize the recent advances towards the discovery of antiplasmodial and antimalarial hybrids including quinoline skeleton to provide an insight for rational designs of more active and less toxic quinolines hybrids antimalarials.
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Ciprofloxacin derivatives and their antibacterial activities
TL;DR: The recent advances made towards the discovery of ciprofloxacin derivatives as antibacterial agents and the structure-activity relationship of these derivatives was also discussed.
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Recent advances of pyrazole-containing derivatives as anti-tubercular agents.
TL;DR: This review aims to outline the recent achievements in pyrazole-containing derivatives as anti-TB agents and their structure-activity relationship.
Journal ArticleDOI
4-Quinolone hybrids and their antibacterial activities.
TL;DR: This review aims to summarize the recent advances made towards the discovery of 4-quinolone hybrids as potential antibacterial agents as well as their structure-activity relationship (SAR) and suggests that the enriched SAR may pave the way for the further rational development of 4+1+1 hybrids with excellent potency against both drug-susceptible and drug-resistant bacteria.
References
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Journal ArticleDOI
The diarylquinoline TMC207 for multidrug-resistant tuberculosis
Andreas H. Diacon,Alexander S. Pym,Martin P. Grobusch,R. F. Patientia,Roxana Rustomjee,Liesl Page-Shipp,Christoffel Pistorius,Rene Krause,Mampedi Bogoshi,Gavin J. Churchyard,Amour Venter,Jenny Allen,Juan Carlos Palomino,Tine De Marez,Rolf van Heeswijk,Nacer Lounis,Paul Meyvisch,Johan Verbeeck,Wim Parys,Karel de Beule,Koen Andries,David F Mc Neeley +21 more
TL;DR: The clinical activity of TMC207 validates ATP synthase as a viable target for the treatment of tuberculosis.
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Piperaquine, A Resurgent Antimalarial Drug
TL;DR: The tolerability, efficacy, pharmacokinetic profile and low cost of piperaquine make it a promising partner drug for use as part of an ACT, endorsed by the WHO.
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Novel 1,2,3-triazole derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain.
Nubia Boechat,Vitor F. Ferreira,Sabrina B. Ferreira,Maria de Lourdes G. Ferreira,Fernando de C. da Silva,Mônica M. Bastos,Marilia S. Costa,Maria C.S. Lourenço,Angelo C. Pinto,Antoniana U. Krettli,Anna Caroline Campos Aguiar,Brunno M Teixeira,Nathalia V da Silva,Priscila R. C. Martins,Flávio A. F. M. Bezerra,Ane Louise S Camilo,Gerson P. da Silva,Gerson P. da Silva,Carolina C. P. Costa +18 more
TL;DR: Derivatives of isoniazid (INH), (E)-N'-[(1-aryl)-1H-1,2,3-triazole-4-yl)methylene] isonicotinoyl hydrazides, exhibited significant activity and displayed low cytotoxicity against liver cells and kidney cells, thereby providing a high therapeutic index.
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Targeting mycobacterium protein tyrosine phosphatase B for antituberculosis agents
Bo Zhou,Yantao He,Xian Zhang,Xian Zhang,Jie Xu,Yong Luo,Yuehong Wang,Scott G. Franzblau,Zhenyun Yang,Rebecca J. Chan,Yan Liu,Jianyu Zheng,Zhong Yin Zhang +12 more
TL;DR: It is demonstrated that inhibition of mPTPB with I-A09 in macrophages reverses the altered host immune responses induced by the bacterial phosphatase and prevents TB growth in host cells.
Journal ArticleDOI
Clubbed [1,2,3] triazoles by fluorine benzimidazole: a novel approach to H37Rv inhibitors as a potential treatment for tuberculosis.
Charansingh H. Gill,Ganesh R. Jadhav,Mohammad U. Shaikh,Rajesh P. Kale,Anant R. Ghawalkar,Deepak R. Nagargoje,Mahendra Ramesh Shiradkar +6 more
TL;DR: A Novel Clubbed [1,2,3] triazoles with fluorine benzimidazole series of H37Rv strain inhibitors, potentially useful for the treatment of tuberculosis is disclosed on the basis of promising results of preliminary antimicrobial study.