ChemInform Abstract: NEUE SEMI- UND THIOSEMICARBAZIDE UND IHRE CYCLISIERUNGSPRODUKTE

Tutoveanu, M.; Constantinescu, C.; Maerean, V.

doi:10.1002/chin.197330294

Cited by 2 publications

(3 citation statements)

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“…Refluxing compound 1 (commercial phenylacetohydrazide), and compound 2 (Ibuprofen hydrazide) with methyl-/ethylisothiocyanate in ethanol yielded substituted thiosemicarbazides (compounds 3-6, Figs. S5-S15) [25,[35][36][37][38][39][40][41][42][43][44][45]. All cyclization products (compound 7-10, Figs.…”

Section: Chemistrymentioning

confidence: 99%

“…All cyclization products (compound 7-10, Figs. S16-S27) were prepared by refluxing all substituted thiosemicarbazide compounds in NaOH solution followed by acidifying the produced sodium salts with dilute solution of HCl [25,26,39,[42][43][44][45][46][47][48][49]. The compounds 7-10 and bromo/chloroacetophenone derivatives were reacted in acetonitrile with TEA to gain thioether compounds 11-28 (Figs.…”

Section: Chemistrymentioning

confidence: 99%

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Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity

et al. 2022

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Some novel triazole-bearing ketone and oxime derivatives were synthesized from Ibuprofen. In vitro cytotoxic activities of all synthesized molecules against five cancer lines (human breast cancer MCF-7, human lung cancer A549, human prostate cancer PC-3, human cervix cancer HeLa, and human chronic myelogenous leukemia K562 cell lines) were evaluated by MTT assay. In addition, mouse embryonic fibroblast cells (NIH/3T3) were also evaluated to determine the selectivity. Compounds 18, 36, and 45 were found to be the most cytotoxic, and their IC 50 values were in the range of 17.46-68.76 µM, against the tested cancer cells. According to the results, compounds 7 and 13 demonstrated good anti-inflammatory activity against the microsomal enzyme prostaglandin E2 synthase-1 (mPGES-1) enzyme at IC50 values of 13.6 and 4.95 µM. The low cytotoxicity and non-mutagenity of these compounds were found interesting. Also, these compounds significantly prevented tube formation in angiogenesis studies. In conclusion, the anti-inflammatory and angiogenesis inhibitory activities of these compounds without toxicity suggested that they may be promising agents in anti-inflammatory treatment and they may be supportive agents for the cancer treatment.

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Section: Chemistrymentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity

et al. 2022

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“…Such compounds were prepared previously in several steps (etherification, chlorination, thionation, and cyclocondensation) with 45% yield by Bansal et al . and also by cyclization reaction with bases . In our research, two‐step synthesis was used to prepare 1,2,4‐triazole.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Evaluation of Novel Derivatives of Semicarbazide and 1,2,4‐triazole

Pachuta‐Stec

Biernasiuk

Malm

et al. 2017

Journal of Heterocyclic Chem

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Reaction of phenoxyacetic acid hydrazide with isocyanate was used to the synthesis of new semicarbazide derivatives. Cyclization of these compounds in a 2% aqueous solution of sodium hydroxide led to formation of 1,2,4‐triazole‐3‐one. The chemical structure of synthesized compounds was confirmed by elemental analysis and spectroscopic methods (1H and 13C NMR). On the basis of the NMR, spectra were found that cyclic compounds 1,2,4‐triazole exist in the ‐one form. Moreover, all derivatives were examined for their in vitro activity against some species of bacteria. New compounds presented mild or moderate antimicrobial activity only against reference Gram‐positive bacteria. Two derivatives (one semicarbazide and one triazole) showed bactericidal or bacteriostatic activity.

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ChemInform Abstract: NEUE SEMI- UND THIOSEMICARBAZIDE UND IHRE CYCLISIERUNGSPRODUKTE

Cited by 2 publications

References 0 publications

Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity

Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity

Synthesis and Antimicrobial Evaluation of Novel Derivatives of Semicarbazide and 1,2,4‐triazole

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