- Synthesis and evaluation of α-glucosidase inhibitory activity of sulfonylurea derivatives
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Two series of sulfonylureas derivatives including 24 compounds (4, 7, 5a-5o, 8a-8h), among them 17 new derivatives, have been synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 5c, 5h and 8e showed significant in vitro α-glucosidase inhibition with IC50 values of 5.58, 79.85 and 213.36 μm, respectively, comparing with the standard compounds acarbose (IC50 = 268.29 μm) and glipizide (IC50 = 300.47 μm). The preliminary structure-activity relationships (SARs) of the synthesized compounds were also investigated.
- Bui, Thi Thoi,Tran, Van Loc,Ngo, Dai Quang,Tran, Van Chien,Tran, Van Sung,Tran, Thi Phuong Thao
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p. 163 - 171
(2021/03/16)
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- Hapten for broad-spectrum detection of sulfonylurea drugs,artificial antigen, antibody and application
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The invention discloses a hapten for broad-spectrum detection of sulfonylurea drugs, an artificial antigen, an antibody and application The hapten for detecting sulfonylurea drugs comprises a hapten 1and a hapten 2; the structural formula of the hapten 1 is shown as a formula (I) descried in the descriptions of the invention; the structural formula of the hapten 2 is shown as a formula (II)descried in the descriptions of the invention. According to the hapten for the broad-spectrum detection of the sulfonylurea drugs, the artificial antigen, the antibody and application of the invention, on the basis of the two designed haptens, the two haptens are coupled with a carrier protein by utilizing a carbodiimide method, so that the artificial antigens can be prepared; New Zealand rabbits are immunized by utilizing the two artificial antigens, so that two polyclonal antibodies which are completely complementary aiming at the specificity of seven sulfonylurea drugs; according to the characteristics of the two antibodies, a colloidal gold immunochromatographic test strip rapid detection method for broad-spectrum detection of sulfonylurea drugs is successfully established, and the method can simply, conveniently and rapidly detect seven sulfonylurea drugs at the same time, and has a good application prospect.
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Paragraph 0041-0044
(2021/01/29)
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- Styrene sulfone NLRP3 inflammasome inhibitor, preparation method and application thereof
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The invention relates to the field of styrene sulfone compounds and NLRP3 inhibitors, and particularly provides a styrene sulfone NLRP3 inflammasome inhibitor, a preparation method and application thereof, wherein the inhibitor is represented by a formula (1), n is selected from 0 and 1, X is selected from N and O, R1 is selected from different electron withdrawing or electron donating substituents, and R2 is selected from different fat or aromatic substituents. According to the invention, it is verified that the compounds represented by the general formula have NLRP3 inhibitory activity.
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Paragraph 0053; 0150-0151
(2020/10/30)
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- PROCESS FOR PREPARATION OF GLIPIZIDE
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The present invention discloses a simple, economic, consistent, commercially viable and industrially applicable process for preparation of Glipizide in high yield and highly pure Glipizide having purity more than 95%, preferably more than 96%, more preferably more than 98% and most preferably more than 99%.
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Page/Page column 16
(2018/05/24)
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- NOVEL COMPOUNDS AND USES
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The present invention relates to compounds of formula (I): wherein Q is O or S; R1 is a cyclic group substituted with at least one group X, wherein R1 may optionally be further substituted; X is any group comprising a carbonyl group; and R2 is a cyclic group substituted at the α-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the dual action of NLRP3 inhibition and the stimulation of insulin secretion.
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Page/Page column 64
(2018/12/13)
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- 7-MEMBERED RING COMPOUND, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL USE THEREOF
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A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.
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Page/Page column 42
(2008/06/13)
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- Indole sPLA2 inhibitors
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A class of novel acylsulfonamide substituted indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2mediated release of fatty acids for treatment of inflammatory diseases.
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