The antitubercular activity of various nitro(triazole/imidazole)-based compounds

Papadopoulou, Maria V.; Bloomer, William D.; Rosenzweig, Howard S.

doi:10.1016/j.bmc.2017.09.037

Cited by 23 publications

(13 citation statements)

References 39 publications

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“…Among the tested compounds, Compound 43 were the most active against aerobic M. tuberculosis and had an MIC value of 1.1 μg/ml. Under anaerobic conditions, Compound 42 exhibited an antitubercular activity of 8.17 μg/ml, which was 9 times better than the activity of the contrast medicine metronidazole (Papadopoulou, Bloomer, & Rosenzweig, ).…”

Section: Five‐membered Ring Compoundsmentioning

confidence: 93%

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

Wang

et al. 2020

Drug Development Research

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Tuberculosis (TB), a chronic infectious disease, is one of the greatest risks to human beings and 10 million people were diagnosed with TB and 1.6 million died from this disease in 2017. In addition, with the emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB), the TB situation has become even worse, which has aggravated the mortality and spread of this disease.To overcome this problem, research into novel antituberculosis agents with enhanced activities against MDR-TB, reduced toxicity, and shortened duration of therapy is of great importance. Fortunately, many novel potential anti-TB drug candidates with five-membered rings, which are most likely to be effective against sensitive and resistant strains, have recently entered clinical trials. Different five-membered rings such as furans, pyranoses, thiazoles, pyrazolines, imidazoles, oxazolidinone, thiazolidins, isoxazoles, triazoles, oxadiazoles, thiadiazoles, and tetrazoles have been designed, prepared, and evaluated for their antimycobacterial activity against Mycobacterium tuberculosis. In this article, we highlight the recent advances made in the discovery of novel five-membered ring compounds and focus on their antitubercular activities, toxicity, structure-activity relationships, and mechanisms of action. K E Y W O R D Santi-TB drug, antitubercular activities, five-membered ring, MDR-TB, tuberculosis

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Section: Five‐membered Ring Compoundsmentioning

confidence: 93%

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

Wang

et al. 2020

Drug Development Research

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“…screened the anti-TB potential of 3-nitro-1,2,4-triazole-linked sulfonamides 186 and amides 187 – 188 ( Fig. 39 ) against Mtb H 37 Rv under aerobic or hypoxic conditions [ 166 , 167 ]. Among them, compounds 186a and 186b exhibited excellent activity MIC of 1.56 and 3.13 μg/mL, respectively, superior to ethambutol (MIC: 6.25 μg/mL).…”

Section: Biological Activities Of 124-triazole Derivativesmentioning

confidence: 99%

An insight on medicinal attributes of 1,2,4-triazoles

Aggarwal

Sumran²

2020

European Journal of Medicinal Chemistry

203

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The present review aims to summarize the pharmacological profile of 1,2,4-triazole, one of the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant, antituberculosis, antiviral, antiparasitic, analgesic and anti-inflammatory agents, etc. along with structure-activity relationship. The comprehensive compilation of work carried out in the last decade on 1,2,4-triazole nucleus will provide inevitable scope for researchers for the advancement of novel potential drug candidates having better efficacy and selectivity.

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“…Moreover, imidazole derivatives have been reported to possess pharmacological properties such as antibacterial, [2] antifungal, [3] analgesic, [4] antitubercular, [5] antihistaminic (cimetidine), [6] anticancer, [7] antihypertensive (losartan), [8] proton pump inhibitor (omeprazole), [9] benzodiazepine antagonist (flumazenil), [10] and antitumor activities (Figure 1). Moreover, imidazole derivatives have been reported to possess pharmacological properties such as antibacterial, [2] antifungal, [3] analgesic, [4] antitubercular, [5] antihistaminic (cimetidine), [6] anticancer, [7] antihypertensive (losartan), [8] proton pump inhibitor (omeprazole), [9] benzodiazepine antagonist (flumazenil), [10] and antitumor activities (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

β‐Cyclodextrin catalyzed access to fused 1,8‐dihydroimidazo[2,3‐b]indoles via one‐pot multicomponent cascade in aqueous ethanol: Supramolecular approach toward sustainability

Nipate

Jadhav

Chate

et al. 2019

Journal of Heterocyclic Chem

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An eco-friendly multicomponent synthesis of substituted imidazole derivatives catalyzed by β-cyclodextrin (β-CD) was scrutinized for the first time via a onepot three-compound reaction of aldehyde, isatin, and ammonium acetate in H 2 O-EtOH at 80°C. β-CD is a supramolecule, highly efficient, biodegradable, and recyclable catalyst used to produce high yields of desired 1, 8dihydroimidazo[2,3-b]indoles. The developed protocol contains number of advantages like nontoxic, inexpensive catalyst; green reaction condition; easily available starting material; shorter reaction time; and good yields.

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The antitubercular activity of various nitro(triazole/imidazole)-based compounds

Cited by 23 publications

References 39 publications

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

An insight on medicinal attributes of 1,2,4-triazoles

β‐Cyclodextrin catalyzed access to fused 1,8‐dihydroimidazo[2,3‐b]indoles via one‐pot multicomponent cascade in aqueous ethanol: Supramolecular approach toward sustainability

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