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Allylic thiocyanates as a new class of antitubercular agents

Bioorganic & Medicinal Chemistry Letters, 2012
TB is a global public health emergency in which new drugs are desperately needed. Herein we report on the synthesis of a diverse panel of 41 aryl allylic azides, thiocyanates, isothiouronium salts, and N,N'-diacetylisothioureas that were evaluated for their in vitro activity against replicating and non-replicating Mycobacterium tuberculosis (Mtb) H(37 ...
Scott G. Franzblau   +7 more
openaire   +3 more sources

Demethoxycurcumin and its Semisynthetic Analogues as Antitubercular Agents

Planta Medica, 2008
Demethoxycurcumin, isolated from the rhizomes of Curcuma longa, was found to possess antitubercular activity against Mycobacterium tuberculosis H (37)Rv strain at 200 microg/mL. Derivatisation of this active principle yielded a potent agent 6, exhibiting considerable activity with a minimum inhibitory concentration (MIC) value of 7.8 microg/mL.
Arvind S. Negi   +9 more
openaire   +3 more sources

Benzoxazole Derivatives as Promising Antitubercular Agents

ChemistrySelect, 2018
AbstractTuberculosis (TB) is an infectious disease caused predominantly by bacillus Mycobacterium tuberculosis (MTB). The increasing prevalence of multidrug‐resistant MTB necessitates the discovery and development of alternative drugs against tuberculosis with a new mechanism of action.
Veronika Šlachtová, Lucie Brulíková
openaire   +2 more sources

ChemInform Abstract: Global Bayesian Models for the Prioritization of Antitubercular Agents.

ChemInform, 2008
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Thomas H. Keller   +2 more
openaire   +4 more sources

Juglone derivatives as antitubercular agents: A rationale for the activity profile

European Journal of Medicinal Chemistry, 2009
The antitubercular activity and cytotoxicity of juglone derivatives were analyzed with the topological and molecular surface features from a web-based server, MODEL (MOlecular DEscriptor Lab). Analysis of the structural features in conjunction with the biological endpoints in Combinatorial Protocol in Multiple Linear Regression led to the ...
Brij Kishore Sharma   +2 more
openaire   +3 more sources

Repurposing antitubercular agent isoniazid for treatment of prostate cancer

Biomaterials Science, 2019
Development of isoniazid–dye conjugates as versatile antitumor agents for mitochondria-targeting, NIR imaging and potent antitumor efficacy.
Qingzhi Lv   +7 more
openaire   +3 more sources

Recent Advances in the Research of Heterocyclic Compounds as Antitubercular Agents

ChemMedChem, 2012
AbstractTuberculosis (TB) is a major health problem, with approximately one‐third of the world′s population infected with Mycobacterium tuberculosis, eight million people in the active disease state, and two million dying annually. Furthermore, the prevalence of TB/HIV co‐infection, and the emergence of multidrug‐resistant tuberculosis (MDR‐TB) and ...
Mi Yan, Shutao Ma
openaire   +4 more sources

Recent Developments in Azole Compounds as Antitubercular Agent

Mini-Reviews in Organic Chemistry, 2019
Tuberculosis (TB) is a global health disaster and is a wide-reaching hitch. The improper use of antibiotics in chemotherapy of TB patients led to the current problem of tuberculosis therapy which gives rise to Multi-Drug Resistant (MDR) strains. Nitrogen heterocycles including azole compounds are an important class of therapeutic agent with electron ...
Gyati Shilakari Asthana   +4 more
openaire   +2 more sources

Nitroarenes as Antitubercular Agents: Stereoelectronic Modulation to Mitigate Mutagenicity

ChemMedChem, 2016
AbstractNitroarenes are less preferred in drug discovery due to their potential to be mutagenic. However, several nitroarenes were shown to be promising antitubercular agents with specific modes of action, namely, nitroimidazoles and benzothiazinones. The nitro group in these compounds is activated through different mechanisms, both enzymatic and non ...
Claire Sadler   +19 more
openaire   +3 more sources

A small library of trisubstituted pyrimidines as antimalarial and antitubercular agents

Bioorganic & Medicinal Chemistry Letters, 2005
A small library of 20 trisubstituted pyrimidines were synthesized and evaluated for their in vitro antimalarial and antitubercular activities. Out of the total screened compounds, 16 compounds have shown in vitro antimalarial activity against Plasmodium falciparum in the range of 0.25-2microg/mL and 8 compounds have shown antitubercular activity ...
Sunil K. Puri   +4 more
openaire   +3 more sources

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