Journal ArticleDOI
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
TLDR
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.Abstract:
The purpose of this study was to prepare various 4-substituted N-phenyl-1,2,3-triazole derivatives using click chemistry. The derivatives were screened in vitro for antimicrobial activity against Mycobacterium tuberculosis strain H37Rv (ATCC 27294) using the Alamar Blue susceptibility test. The activity was expressed as the minimum inhibitory concentration (MIC) in μg/mL (μM). Derivatives of isoniazid (INH), (E)-N'-[(1-aryl)-1H-1,2,3-triazole-4-yl)methylene] isonicotinoyl hydrazides, exhibited significant activity with MIC values ranging from 2.5 to 0.62 μg/mL. In addition, they displayed low cytotoxicity against liver cells (hepatoma HepG2) and kidney cells (BGM), thereby providing a high therapeutic index. The results demonstrated the potential and importance of developing new INH derivatives to treat mycobacterial infections.read more
Citations
More filters
Journal ArticleDOI
Click Chemistry for Drug Development and Diverse Chemical–Biology Applications
Journal ArticleDOI
Medicinal attributes of 1,2,3-triazoles: Current developments
TL;DR: The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors, HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials.
Journal ArticleDOI
Recent researches in triazole compounds as medicinal drugs.
TL;DR: This work systematically reviewed the recent researches and developments of the whole range of triazole compounds as medicinal drugs, including antifungal, anticancer, antibacterial, antitubercular, antiviral, anti-inflammatory and analgesic, anticonvulsant, antiparasitic, antidiabetic and anti-obesitic.
Journal ArticleDOI
Triazole derivatives and their anti-tubercular activity
TL;DR: 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.
Journal ArticleDOI
Design, Synthesis, and Structure–Activity Correlations of Novel Dibenzo[b,d]furan, Dibenzo[b,d]thiophene, and N-Methylcarbazole Clubbed 1,2,3-Triazoles as Potent Inhibitors of Mycobacterium tuberculosis
Santhosh Reddy Patpi,Lokesh Pulipati,Perumal Yogeeswari,Dharmarajan Sriram,Nishant Jain,Balasubramanian Sridhar,Ramalinga Murthy,Anjana Devi T,Shasi V. Kalivendi,Srinivas Kantevari +9 more
TL;DR: The results together provided the potential importance of molecular hybridization and the development of triazole clubbed dibenzo[b,d]thiophene-based lead candidates to treat mycobacterial infections.
References
More filters
Journal ArticleDOI
A stepwise huisgen cycloaddition process: copper(I)-catalyzed regioselective "ligation" of azides and terminal alkynes.
Journal ArticleDOI
Click Chemistry: Diverse Chemical Function from a Few Good Reactions.
TL;DR: In this paper, a set of powerful, highly reliable, and selective reactions for the rapid synthesis of useful new compounds and combinatorial libraries through heteroatom links (C-X-C), an approach called click chemistry is defined, enabled, and constrained by a handful of nearly perfect "springloaded" reactions.
Journal ArticleDOI
Rapid colorimetric assay for cell growth and survival. Modifications to the tetrazolium dye procedure giving improved sensitivity and reliability.
François Denizot,Rita Lang +1 more
TL;DR: The reliability and sensitivity of the test have been increased to the point where it can in many cases replace the [3H]thymidine uptake assay to measure cell proliferation or survival in growth factor or cytotoxicity assays.
Journal ArticleDOI
Click Chemistry: Diverse Chemical Function from a Few Good Reactions
TL;DR: In this article, a set of powerful, highly reliable, and selective reactions for the rapid synthesis of useful new compounds and combinatorial libraries through heteroatom links (C-X-C), an approach called click chemistry is defined, enabled, and constrained by a handful of nearly perfect "springloaded" reactions.
Journal ArticleDOI
Rapid, Low-Technology MIC Determination with Clinical Mycobacterium tuberculosis Isolates by Using the Microplate Alamar Blue Assay
Scott G. Franzblau,Richard S. Witzig,J. C. McLaughlin,Patricia Torres,Guillermo Madico,Antonio Moreno Hernández,Michelle T. Degnan,Mary B. Cook,Virginia K. Quenzer,Robert M. Ferguson,Robert H. Gilman,Robert H. Gilman +11 more
TL;DR: The MABA is a simple, rapid, low-cost, appropriate technology which does not require expensive instrumentation and which makes use of a nontoxic, temperature-stable reagent.