40207-03-2Relevant articles and documents
A new organometallic palladium(II) compound derived of 2,6-diacetylpyridine mono(thiosemicarbazone): Synthesis, spectroscopic properties and crystal structure of two solvatomorphic forms
Matesanz, Ana I.,Hernández, Carolina,Souza, Pilar
, p. 374 - 378 (2014)
Preparation and characterization of a novel 2,6-diacetylpyridine mono(4-methoxyphenyl-thiosemicarbazone), H2L, is described. Treatment of H2L with PdCl2(PPh3)2 gave the neutral mononuclear complex [Pd
Oxadiazol-based mTOR inhibitors with potent antiproliferative activities: synthetic and computational modeling
Khanfar, Mohammad A.
, (2022/01/11)
Series of N-aryl-1,3,4-oxadiazole-2-amines and 3-aryl-1,2,4-oxadiazole-5-carboxamides derivatives were synthesized as novel chemotherapeutic agents. Synthesized compounds were evaluated for their anticancer activities against several cancer cell lines. Many analogues of 1,3,4-oxadiazole scaffold showed potent antiproliferative activities against breast cancer cell lines, with higher activities toward the metastatic breast cancer cell line (MDA-MB-231). Active analogues were profiled using in-house pharmacophore database in search for molecular target. Active analogues (2j and 2k) were found to fit the pharmacophoric map of ATP-competitive inhibitors of mTOR. The mTOR inhibitory activities of the most active compounds were confirmed with IC50 values in nanomolar range. The N-aryl-1,3,4-oxadiazole-2-amines linked to a basic head is a novel ATP-competitive inhibitors of mTOR with potential activities for treatment of different types of cancer. Graphical abstract: [Figure not available: see fulltext.].
Synthesis and antimicrobial activities of new thiosemicarbazones and thiazolidinones in indole series
Benmohammed, Abdelmadjid,Djafri, Ayada,Kadiri, Mokhtaria,Khoumeri, Omar,Louail, Ahmed Amine,Rekiba, Nawel,Sehanine, Yassine,Terme, Thierry,Vanelle, Patrice
, p. 977 - 986 (2021/08/13)
Abstract: New thiosemicarbazones were synthesized in excellent yield reaction of indole derivatives with thiosemicarbazides. These thiosemicarbazones were reacted with ethyl bromoacetate to produce original heterocyclic-substituted indole derivatives possessing a 4-oxo-thiazolidine group. Analytical IR and NMR spectra and elemental analysis were performed to reveal their structures. The antimicrobial activity of all synthesized compounds was evaluated for antibacterial activity in vitro against Gram-positive and Gram-negative bacteria. Antibacterial screening data showed that two compounds demonstrated activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. These preliminary results indicate that some of these newly synthesized compounds show a promising antibacterial potency. Graphic abstract: [Figure not available: see fulltext.].
Preparation and application of thiosemicarbazone compound
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Paragraph 0010; 0014; 0015, (2021/02/20)
The invention discloses a thiosemicarbazone compound, and biological activity analysis is carried out on the thiosemicarbazone compound. The invention also discloses application of the thiosemicarbazone compound in preparation of antibacterial drugs. According to the invention, important intermediates 6a-6h are synthesized from hydrazine hydrate and react with adamantane benzaldehyde respectivelyto synthesize eight adamantane aromatic aldehyde thiosemicarbazone compounds, the structures of the compounds can be confirmed by infrared, nuclear magnetic hydrogen spectrum, carbon spectrum and massspectrum methods, and the antibacterial activity of the compounds is tested in vitro. The result shows that the compound has a good antibacterial effect on escherichia coli and bacillus subtilis.