20022-44-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of imidazole and triazole-based carbamates as novel aromatase inhibitors
Ammazzalorso, Alessandra,Gallorini, Marialucia,Fantacuzzi, Marialuigia,Gambacorta, Nicola,De Filippis, Barbara,Giampietro, Letizia,Maccallini, Cristina,Nicolotti, Orazio,Cataldi, Amelia,Amoroso, Rosa
, (2021)
In the search for novel aromatase inhibitors, a series of triazole and imidazole-based carbamate derivatives were designed and synthesized. Final compounds were thus evaluated against human aromatase by in vitro kinetic experiments in a fluorimetric assay in comparison with letrozole. The effect of most active derivatives 13a and 15c was then evaluated in vitro on the human breast cancer cell line MCF7 by MTT assay, cytotoxicity assay (LDH release) and cell cycle analysis, revealing a dose-dependent inhibition profile of cell viability and low micromolar IC50 values. In addition, docking simulations were also carried out to elucidate at a molecular level of detail the binding modes adopted to target human aromatase.
Asymmetric transfer hydrogenation of heterocycle-containing acetophenone derivatives using N-functionalised [(benzene)Ru(II)(TsDPEN)] complexes
Barrios-Rivera, Jonathan,Xu, Yingjian,Clarkson, Guy J.,Wills, Martin
, (2021/12/02)
The application of enantiomerically-pure ruthenium(II) catalysts containing N - functionalised TsDPEN ligand to the asymmetric transfer hydrogenation of 15 examples of α-heterocyclic acetophenone derivatives is reported. Products of up to 99% ee were formed.
Selective Generation of (1H-1,2,4-Triazol-1-yl)methyl Carbanion and Condensation with Carbonyl Compounds
Lassalas, Pierrik,Claraz, Aurélie,Tran, Ga?l,Vors, Jean-Pierre,Tsuchiya, Tomoki,Coqueron, Pierre-Yves,Cossy, Janine
supporting information, p. 6991 - 6996 (2017/12/26)
2-(1H-1,2,4-Triazol-1-yl)ethanols have received significant interest in agricultural and medicinal chemistry owing to their herbicidal and antifungal activities. To develop a versatile method to access these substituted triazoles, we explored the generation of the (1H-1,2,4-triazol-1-yl)methyl carbanion and its condensation with carbonyl compounds. By judicious choice of a suitable anion precursor (tributylstannyl group) or a stabilizing anion group (phenylsulfanyl or phenylsulfinyl group), a wide range of aldehydes and ketones reacted with the carbanions to give a large diversity of 2-(1H-1,2,4-triazol-1-yl)ethanols in good yields.
Research on antibacterial and antifungal agents. X. Synthesis and antimicrobial activities of 1-phenyl-2-(1H-azol-1-yl) ethane derivatives. Anticonvulsant activity of 1-(4-methylphenyl)-2-(1H-imidazol-1-yl) ethanol.
Porretta, G. C.,Fioravanti, R.,Biava, M.,Cirilli, R.,Simonetti, N.,et al.
, p. 749 - 760 (2007/10/02)
The synthesis and antimicrobial activity of new phenylazolylethane derivatives are reported.Antimicrobial data in comparison with those obtained with miconazole, fluconazole, enilconazole, imazalil sulfate, pipemidic acid and minocycline showed that tested compounds generally possessed poor or weak activity.Toxicity and anticonvulsant activity of 1-(4-methylphenyl)-2-(1H-imidazol-1-yl)ethanol and structural likeness to Denzimol were also tested.The obtained results showed interesting anticonvulsant activity but only on the supraspinal region. azoles / antifungal / anticonvulsant agent
