864684-98-0Relevant articles and documents
Synthesis, antimicrobial screening, and docking study of new 2-(2-ethylpyridin-4-yl)-4-methyl-N-phenylthiazole-5-carboxamide derivatives
Kasare, Sanghratna L.,Gund, Pornima N.,Sathe, Bhaurao P.,Patil, Pravin S.,Rehman, Naziya N. M. A.,Dixit, Prashant P.,Choudhari, Prafulla B.,Haval, Kishan P.
, p. 353 - 361 (2020/09/23)
A series of new 2-(2-ethylpyridin-4-yl)-4-methyl-N-phenylthiazole-5-carboxamide derivatives (5a-l) were synthesized and evaluated for their in vitro antimicrobial activities. Among the screened compounds, 5b, 5d, 5e, 5f, and 5j have shown promising antimicrobial activities against both bacterial and fungal pathogens. A molecular docking study was conducted to know the probable mode of action of synthesized derivatives for antimicrobial activity. The active compounds have shown excellent binding affinity toward DNA gyrase and lumazine synthase enzymes. The physicochemical properties of the synthesized thiazole-carboxamide derivatives were calculated. It has displayed the potential to be a reasonable oral bioavailability drug as determined by Lipinski's rule.
Aromatic heterocyclic small molecule organic compounds and derivatives, preparation method and medical use
-
Paragraph 0255-0256, (2016/11/17)
The invention discloses heterocyclic aromatic micromolecule organic compounds as shown in the structural formula (I) and derivatives thereof, or hydrates or pharmaceutically acceptable salts, and a preparation method of the corresponding compounds; the invention also discloses an application of the compounds and pharmaceutical compositions containing the compounds to the treatment of various metabolic syndrome-related diseases. The heterocyclic aromatic micromolecule organic compounds of the invention have excellent treatment effect on metabolic syndromes; experiment results show that the compounds may promote secretion of endogenous GLP-1, and are applicable to the preparation of anti-diabetic and fat-reducing candidate medicaments. Aiming at technical problems of easy degradation and short half life of current medicaments for treating diabetes, the invention provides novel, high-efficient micromolecule compounds for promoting secretion of endogenous GLP-1, and the compounds are applicable to the treatment of metabolic syndrome-related diseases such as diabetes, obesity and the like.