Synthesis and anti-tuberculosis activity of N-aryl-C-nitroazoles

Walczak, Krzysztof; Gondela, Andrzej; Suwiński, J.

doi:10.1016/j.ejmech.2004.06.014

Cited by 130 publications

(59 citation statements)

References 19 publications

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“…1,2,4-Oxadiazoles (21)(22)(23)(24)(25)(26)(27)(28)(29)(30) were obtained by the treatment of compounds (6)(7)(8)(9)(10)(11)(12)(13)(14)(15) with N-hydroxyacetamidine under EDC/ HOBT conditions. The acid hydrazides (18) was treated with acetic acid in the presence of phosphorus oxychloride afforded 1,3,4-oxadiazoles (31-32).…”

Section: Methodsmentioning

confidence: 99%

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Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position

Wubulikasimu¹,

Yang²,

Xue³

et al. 2013

Bulletin of the Korean Chemical Society

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A series of novel benzimidazole derivatives bearing a heterocyclic ring as oxadiazole (21-32), thiadiazole (33-34), triazole (35-36) were synthesized and evaluated for their activities against Coxsackie virus B3 and B6 in Vero cells. Compounds 21-26, 31-36 with moieties of 2'-pyridyl, 3'-pyridyl and 4'-pyridyl at the 2-position and oxadiazoles, thiadiazole, or triazole substituent at the 4-or 5-position generally displayed activities against CVB3 and CVB6. Especially compound 24 (IC 50 = 1.08 µg/mL, SI = 61.7 against CVB3) was the promising candidate as lead compound for anti-enteroviral drug. It was observed in the incorporation of heterocyclic rings in benzimidazole at the 5-position could enhance their biological activities.

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Section: Methodsmentioning

confidence: 99%

“…1,2,4-triazole derivatives are also known to exhibit antimicrobial, 23 antitubercular, 24 anticancer, 25 anticonvulsant, 26 anti-inflammatory and analgesic properties. 27 Enteroviruses are members of the picornavirus family, a large and diverse group of small RNA viruses characterized by a single positive-strand genomic RNA.…”

mentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position

Wubulikasimu¹,

Yang²,

Xue³

et al. 2013

Bulletin of the Korean Chemical Society

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“…Products 14 from dinitroimidazole 2 and halogenoanilines indicated very promising activity in tuberculosis inhibition. 56 Several new 1-(halogenophenyl)-4-nitro-1H-imidazoles and 1-(dihalogenophenyl)-4-nitro-1H-imidazoles were prepared using the ANRORC approach. 57 The latter compounds and some other arylnitroimidazoles 14 were examined in vitro against human African trypanosomes.…”

Section: Figure 6 Proposed Structure Of P-toluidine-2-merhyl-14-dinmentioning

confidence: 99%

1,4-Dinitro-1H-imidazoles

Suwiński¹

2015

Arkivoc

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“…In addition, triazole compounds are effective antifungal agents. Many such heavily marketed modern-day antifungal drugs containing triazole nucleus namely, fluconazole [4], voriconazole [5], itraconazole [6], ravuconazole [7] etc., are reported in the literature. The basic nitrogen of azole ring would be tightly bound to the heme iron of the fungal cytochrome P450 preventing substrate and oxygen binding, thus they act as cytochrome P450 14α-demethylase inhibitors [8].…”

Section: Introductionmentioning

confidence: 99%