- Synthesis, antimicrobial screening, and docking study of new 2-(2-ethylpyridin-4-yl)-4-methyl-N-phenylthiazole-5-carboxamide derivatives
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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.
- 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.
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p. 353 - 361
(2020/09/23)
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- PUF60-targeting t-butyloxycarbonyl micromolecular organic compound and derivative and application thereof
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The invention discloses a tert-butyloxycarbonyl micromolecular organic compound or related analogue or pharmaceutically acceptable salt thereof. The structure of the tert-butyloxycarbonyl micromolecular organic compound is as shown in formulas (I)-(V). The invention also discloses application of the t-butyloxycarbonyl micromolecular organic compound or the pharmaceutical composition thereof in preparation of medicines for preventing and/or treating various malignant tumors and the like, and application of the t-butyloxycarbonyl micromolecular organic compound or the pharmaceutical composition thereof as a PUF60 inhibitor in preparation of medicines for preventing and/or treating PUF60-mediated diseases. The invention further innovatively provides the application of the t-butyloxycarboryl micromolecular organic compound or the targeted PUF60 of the pharmaceutical composition of the t-butyloxycarboryl micromolecular organic compound in preparation of medicines for treating ovarian cancer for the first time.
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Paragraph 0095-0097
(2021/07/24)
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- Aromatic heterocyclic small molecule organic compounds and derivatives, preparation method and medical use
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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.
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Paragraph 0255-0256
(2016/11/17)
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