Synthesis and antibacterial activity of n-(6-x-7-methyl-5-oxo-5 h-1,3,4-thiadiazolo[3,2-a]-pyrimidin-2-yl)diazo-18-crown-6

Сангов, З. Г.; Ashurova, Z. J.; Khalikova, Z. D.; Kukaniev, M. A.; Salimov, T. M.; Dzhamshedov, J. N.

doi:10.1007/s11094-012-0710-7

Cited by 3 publications

(2 citation statements)

References 3 publications

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“…For our investigation, we chose chloro‐functionalized benzothiazolo[3,2‐ a ]pyrimidin‐4‐one 1 as a readily available starting material . Compound 1 was synthesized by condensation of commercially available 2 ‐ amino ‐ 6 ‐ chlorobenzothiazole with ethyl acetoacetate (Scheme ) …”

Section: Resultsmentioning

confidence: 99%

Synthesis of Novel Benzothiazolo[3,2‐a]pyridimidin‐4‐ones with Potential Cytotoxic and Pro‐Apoptotic Potential

et al. 2018

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The combination of cyclocondensation with palladium catalysed cross‐coupling reactions, afforded a variety of 8‐functionalized benzothiazolo[3,2‐a]pyridimidin‐4‐ones in good to excellent yields. The anti‐proliferative potential of the synthetic compounds was evaluated in human cervical adenocarcinoma cells (HeLa) and hamster normal fibroblasts (BHK‐21). Three of the test derivatives exhibited the strongest cytotoxicity in HeLa cells with the median inhibitory concentration (IC50) of 0.93, 1.55 and 1.84 μM, respectively. Moreover, their anti‐proliferative effect was three times less strong in normal fibroblasts, asserting their possible anti‐cancer potential.

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Section: Resultsmentioning

confidence: 99%

Synthesis of Novel Benzothiazolo[3,2‐a]pyridimidin‐4‐ones with Potential Cytotoxic and Pro‐Apoptotic Potential

et al. 2018

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“…It is obvious that grouping of two different moieties in one molecule will lead to a pharmacological influence greater than that of each individual moiety . In particular, merging of thiadiazole and pyrimidine moieties as a fused system, such as 1,3,4‐thiadiazolo[3,2‐ a ] pyrimidine, has shown pharmacodynamics and chemotherapeutics actions, including antimicrobial , anticancer , antiquorum sensing and antitumor , herbicidal , antibacterial , anti‐inflammatory, analgesic, and xanthine oxidase inhibitory activities . Furthermore, 1,3,4‐thiadiazolo[3,2‐ a ] pyrimidines have been also used as key building blocks for the preparation of a variety of novel biologically active derivatives .…”

Section: Introductionmentioning

confidence: 99%

Novel Bridgehead Thiadiazolopyrimidine Derivatives with Antimicrobial and Antitumor Activities

Azab

Abdelwahab

Mahmoud

et al. 2018

Journal of Heterocyclic Chem

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Because of the remarkable pharmacodynamics and chemotherapeutics activities of thiadiazolopyrimidines, a new series of 1,3,4‐thiadiazolo[3,2‐a] pyrimidine derivatives have been synthesized by reacting 5‐substituted‐2‐aminothiadiazoles 1a,b with different reagents: active methylenic compounds, benzaldehyde under different conditions, isatin, and cyclic ketones. The structures of the novel compounds have been inferred by spectroscopic methods (infrared, 1H‐NMR, 13C‐NMR, and mass spectrometry) and elemental analyses. The newly synthesized compounds were screened against four bacterial strains (Staphylococcus aureus and Listeria monocytogenes as Gram positive and Pseudomonas aeruginosa and Salmonella typhimurium as Gram negative) and two fungi (Aspergillus niger and Candida albicans) using agar diffusion assay. Most of the compounds showed activity against the tested microorganisms with different extents. The in vitro anticancer activities of these compounds were assessed against four human tumor cell lines; they were found to exhibit different cytotoxic effects. Such results mean that these derivatives can be further utilized as promising anticancer agents.

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2-Substituted 7-trifluoromethyl-thiadiazolopyrimidones as alkaline phosphatase inhibitors. Synthesis, structure activity relationship and molecular docking study

Jafari

Ospanov

Ejaz

et al. 2018

European Journal of Medicinal Chemistry

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Synthesis and antibacterial activity of n-(6-x-7-methyl-5-oxo-5 h-1,3,4-thiadiazolo[3,2-a]-pyrimidin-2-yl)diazo-18-crown-6

Cited by 3 publications

References 3 publications

Synthesis of Novel Benzothiazolo[3,2‐a]pyridimidin‐4‐ones with Potential Cytotoxic and Pro‐Apoptotic Potential

Synthesis of Novel Benzothiazolo[3,2‐a]pyridimidin‐4‐ones with Potential Cytotoxic and Pro‐Apoptotic Potential

Novel Bridgehead Thiadiazolopyrimidine Derivatives with Antimicrobial and Antitumor Activities

2-Substituted 7-trifluoromethyl-thiadiazolopyrimidones as alkaline phosphatase inhibitors. Synthesis, structure activity relationship and molecular docking study

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