Compounds with potential antitubercular activity

Sycheva, T. P.; Kiseleva, I. D.; Shchukina, M. N.

doi:10.1007/bf00480957

Cited by 3 publications

(5 citation statements)

References 3 publications

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“…2-Hydrazinobenzoxazole was synthesized according to the published method. 53 2,6-diacetylpyridine (99%) was acquired from Alfa Aesar. Copper salts (98%) were purchased from Alfa Aesar.…”

Section: Methodsmentioning

confidence: 99%

Crystal structure and cytotoxic activity of Cu(ii) complexes with bis-benzoxazolylhydrazone of 2,6-diacetylpyridine

et al. 2023

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“…2-Hydrazinobenzoxazole was synthesized according to the published method. 53 2,6-diacetylpyridine (99%) was acquired from Alfa Aesar. Copper salts (98%) were purchased from Alfa Aesar.…”

Section: Methodsmentioning

confidence: 99%

Crystal structure and cytotoxic activity of Cu(ii) complexes with bis-benzoxazolylhydrazone of 2,6-diacetylpyridine

et al. 2023

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“…Between 1966–1973 Sycheva and others reported several papers describing various benzoxazoles amino‐(or hydrazino)‐modified at the position 2 (Figure ) …”

Section: Benzoxazoles As Anti‐tb Agentsmentioning

confidence: 99%

“…The consecutive in vitro tests of derivatives 14 (Figure ) revealed interesting activity against H 37 Rv strain of thiazoyl compound 14b with MIC value 0.5 μg/mL in absence of serum and 2 μg/mL in serum . On the other hand, 2‐pyridyl derivative 14 a showed lower activity (with MIC value 4 μg/mL in absence of serum and 15 μg/mL in serum).…”

Section: Benzoxazoles As Anti‐tb Agentsmentioning

confidence: 99%

“…In 1967, Sycheva et al. broaden the series of their benzoxazole derivatives with (benzoxazol‐2‐yl) hydrazines 15 and 16 (Figure ) . In vitro tuberculostatic activity testing showed 1‐phenyl‐2‐(benzoxazolyl‐2')hydrazine and (6‐nitrobenzoxazolyl‐2) hydrazine as the most active compounds from this series (MIC=4 μg/mL, without serum).…”

Section: Benzoxazoles As Anti‐tb Agentsmentioning

confidence: 99%

“…Sycheva et al. also described a number of N ‐(benzoxazol‐2‐yl)‐ N '‐phenylthioureas 18 (Figure ) . Biological evaluation of 18 revealed, that the most active compound from this series, N ‐(2‐benzoxazolyl)‐ N '‐ p ‐ethoxyphenyl)thiourea, inhibited the growth of MTB (strain H 37 Rv) at concentration of 2 μg/mL in the absence of serum (15 μg/mL in the presence of serum).…”

Section: Benzoxazoles As Anti‐tb Agentsmentioning

confidence: 99%

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Benzoxazole Derivatives as Promising Antitubercular Agents

Šlachtová

Brulíková

2018

ChemistrySelect

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Tuberculosis (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. Over the past years, several benzoxazole derivatives have been synthesized and screened for their biological activity. Interestingly, some of them had promising antitubercular activity. Despite that, none of the benzoxazole derivatives has entered the phase of the preclinical hit‐to‐lead optimization step in anti‐TB research. In this review, we are summarizing recently published articles that evaluate the potency of benzoxazole heterocycle in the development of novel anti‐TB agents and outlined the future aspects of this promising heterocycle.

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Synthesis of Novel Substituted 1,5-Benzothiazepines Containing 1,4-Benzodioxane Sulfonyl Moiety

Chhakra

Mukherjee

Singh

et al. 2019

Asian J. Org. Med. Chem.

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An efficient synthesis of novel 2,3,4-trisubstituted 1,5-benzothiazepines (4a-e) incorporating the sulfonyl group is described. Compound (4a-e) was synthesized by the reaction of 3-(1,4-dioxane-6-sulfonyl)-2,4-dimethyl/4-methyl-2-phenyl/2,4-diphenyl/2-ethoxy-4-methyl/2,4-diethoxy propane-1,3-dione (3ae) with 2-aminobenzenethiol with ZnOnanoparticles/pyridine. Formation of compound (3a-e) was achieved by the reaction of 1,4-dioxane-6-sulfonyl chloride (1) with 2,4-dimethyl/4-methyl-2-phenyl/2,4-diphenyl/2-ethoxy-4-methyl/2,4-diethoxy propane-1,3-dione (2a-e). The benzothiazepines (4a-e) obtained were purified by column chromatography (benzene: CHCl3, 40:60, 30:70, 20:80, 10:90) and crystallized from methanol. The purity of the compounds was checked by TLC using (CHCl3: CH3OH, 9:1) as the mobile phase. The structure of the compounds has been established by elemental, IR, 1H NMR, 13C NMR and Mass spectral analyses. Frontier molecular orbitals of the title compounds have been studied in the ground state speculatively. The reactivity of a molecule using diverse descriptors such as softness, electrophilicity, electronegativity, HOMO-LUMO energy gap is calculated additionally discussed.

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Compounds with potential antitubercular activity

Cited by 3 publications

References 3 publications

Crystal structure and cytotoxic activity of Cu(ii) complexes with bis-benzoxazolylhydrazone of 2,6-diacetylpyridine

Crystal structure and cytotoxic activity of Cu(ii) complexes with bis-benzoxazolylhydrazone of 2,6-diacetylpyridine

Benzoxazole Derivatives as Promising Antitubercular Agents

Synthesis of Novel Substituted 1,5-Benzothiazepines Containing 1,4-Benzodioxane Sulfonyl Moiety

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