The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines

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

doi:10.1016/j.ejmech.2017.07.060

Cited by 18 publications

(11 citation statements)

References 23 publications

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“…gambiense infection compared with nifurtomox-eflornithine combination therapy in late-stage HAT patients. No method of action for nitroimidazoles has yet been elucidated, though it is known to be a substrate for a type I nitro-reductase and is theorized to function in vivo as a pro-drug ( Wyllie et al, 2016 ; Papadopoulou et al, 2017 ).…”

Section: Host-targeted Therapeutics and Approaches For Treatment Of Hmentioning

confidence: 99%

Host-Directed Drug Therapies for Neglected Tropical Diseases Caused by Protozoan Parasites

et al. 2018

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The neglected tropical diseases (NTDs) caused by protozoan parasites are responsible for significant morbidity and mortality worldwide. Current treatments using anti-parasitic drugs are toxic and prolonged with poor patient compliance. In addition, emergence of drug-resistant parasites is increasing worldwide. Hence, there is a need for safer and better therapeutics for these infections. Host-directed therapy using drugs that target host pathways required for pathogen survival or its clearance is a promising approach for treating infections. This review will give a summary of the current status and advances of host-targeted therapies for treating NTDs caused by protozoa.

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Section: Host-targeted Therapeutics and Approaches For Treatment Of Hmentioning

confidence: 99%

Host-Directed Drug Therapies for Neglected Tropical Diseases Caused by Protozoan Parasites

et al. 2018

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“…Papadopoulou et al. reported antichagasic activity of 3-nitro-1 H -1,2,4-triazole-based aliphatic and aromatic amines [ [200] , [201] , [202] ]. Compounds 218 – 227 ( Fig.…”

Section: Biological Activities Of 124-triazole Derivativesmentioning

confidence: 99%

“…Compounds 218 – 220 also exhibited significant activity against bloodstream-form (BSF) Trypanosoma brucei rhodesiense trypomastigotes with IC 50 ranged from 0.117 to 0.435 μM levels and SI of 220–973. In addition, 3-nitrotriazole based piperazine 225a , benzothiazoles ( 226a and 226b ) and quinoline derivative 227 exhibited significant anti-HAT activity against T. b. rhodesiense trypomastigotes with IC 50 of 0.231, 0.204, 0.355 and 0.038 μM, respectively [ 201 , 202 ].…”

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

199

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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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“…Several imidazole compounds 25 , 26 , and 27 (Figure ) that were used as antitubercular agents and possessed outstanding anti‐TB activities under low oxygen conditions had been synthesized and evaluated to determine their activity. In particular, Compound 26 demonstrated an MIC value against Mtb that was as low as 10 μg/ml, but the activity of 26 was still worse than that of positive RIF (Papadopoulou, Bloomer, Rosenzweig, & Kaiser, ).…”

Section: Five‐membered Ring Compoundsmentioning

confidence: 99%

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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The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines

Cited by 18 publications

References 23 publications

Host-Directed Drug Therapies for Neglected Tropical Diseases Caused by Protozoan Parasites

Host-Directed Drug Therapies for Neglected Tropical Diseases Caused by Protozoan Parasites

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

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

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