1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria

Karabanovich, Galina; Roh, Jaroslav; Smutný, Tomás̆; Němeček, Jan; Vicherek, Petr; Stolaříková, Jiřina; Vejsová, Marcela; Dufková, Ida; Vávrová, Kateřina; Pávek, Petr; Klimešová, Věra; Hrabálek, Alexandr

doi:10.1016/j.ejmech.2014.05.069

Cited by 48 publications

(47 citation statements)

References 29 publications

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“…generated a series of tetrazoles, which included compounds 422 and 423 as some of the more promising compounds. This study included the phenyl analogue 424 , which was less impressive . Compound 424 is structurally related to MMV376388 ( 425 ), which has been reported in the patent literature as Gram‐positive bacterial inhibitor…”

Section: Tuberculosismentioning

confidence: 99%

Unpacking the Pathogen Box—An Open Source Tool for Fighting Neglected Tropical Disease

Veale

2019

ChemMedChem

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The Pathogen Box is a 400‐strong collection of drug‐like compounds, selected for their potential against several of the world's most important neglected tropical diseases, including trypanosomiasis, leishmaniasis, cryptosporidiosis, toxoplasmosis, filariasis, schistosomiasis, dengue virus and trichuriasis, in addition to malaria and tuberculosis. This library represents an ensemble of numerous successful drug discovery programmes from around the globe, aimed at providing a powerful resource to stimulate open source drug discovery for diseases threatening the most vulnerable communities in the world. This review seeks to provide an in‐depth analysis of the literature pertaining to the compounds in the Pathogen Box, including structure–activity relationship highlights, mechanisms of action, related compounds with reported activity against different diseases, and, where appropriate, discussion on the known and putative targets of compounds, thereby providing context and increasing the accessibility of the Pathogen Box to the drug discovery community.

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Section: Tuberculosismentioning

confidence: 99%

Unpacking the Pathogen Box—An Open Source Tool for Fighting Neglected Tropical Disease

Veale

2019

ChemMedChem

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“…The three compounds 272 (X = S, O, Se) showed very low cytotoxicity and high selectivity. These compounds exhibited MIC values of 1 μM against M. tuberculosis CNCTC My 331/88, and 0.25–1 μM against six multidrug‐resistant clinically isolates of M. tuberculosis . In another report, tetrazole regioisomers 273 – 274 exhibited good activity at MIC of 0.37–0.47 μg/mL against M. tuberculosis CNCTC My 331/88, Mycobacterium kansasii 6509/96, and INH‐resistant M. kansasii CNCTC My 235/80, while no mutagenic effects were observed …”

Section: Tetrazolesmentioning

confidence: 97%

New structural classes of antituberculosis agents

Kumar

Patel

Jain

2017

Medicinal Research Reviews

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Tuberculosis (TB), one of the deadliest diseases is shattering the health and socioeconomic status of the society. The emergence of multidrug resistant (MDR) and extremely drug resistant (XDR) strains has provided unprecedented lethal character to TB. The development of MDR and XDR strains of TB results in more deaths, longer duration of therapy, and appearance of the disease in the immunocompromised patients. Because of the development of rapid resistance by Mycobacterium tuberculosis, researchers are confronted with serious challenges in combating TB. For instance, the need for potency and specificity in therapeutic agents approaching clinics, and the increasing demand of low toxicity due to long duration of treatment. Recently, it is proposed that such challenges could be addressed by a shift from contemporary or known classes of drugs to new scaffold-containing or entirely new structural classes of drugs that possibly act on the previously unknown targets, resulting in possibly less instances of resistance development. The exploitation of advances made in the biology of TB in the last and present decades have created opportunities to discover a large number of new structural classes that specifically targets TB by molecular mechanism of action(s) unknown earlier. We have earlier reviewed new structural classes of anti-TB agents up to year 2005. This review covers literature reports of the subsequent 10 years on the discovery of new structural classes of synthetic anti-TB agents. Due to the availability of large number of research reports, we have divided new compounds in 38 structural classes, 368 structures, and 307 references.

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“…Organoselenium compounds are used as ligands in asymmetric catalysis [10] and promising "green chemistry" catalysts [11]. Selenium-containing organic compounds can be used in cancer therapy [12][13][14][15][16][17][18][19][20][21], in particular as cancer cell proliferation inhibitors [22][23][24][25][26][27][28][29][30][31][32], and they exhibit antihypertensive [33], antibacterial [13,[34][35][36][37][38][39], antifungal [40,41], antiparasitic [42], and antimicrobial activity [43]. During the past decade various selenium derivatives have been tested for biological activity as free radical [44][45][46] and superoxide anion scavengers [47], antioxidants [48][49][50][51][52][53], anti-inflammatory agents, and microglial activation inhibitors [54].…”

Section: Introductionmentioning

confidence: 99%