2015-16-9Relevant articles and documents
Synthesis and evaluation of α-glucosidase inhibitory activity of sulfonylurea derivatives
Bui, Thi Thoi,Tran, Van Loc,Ngo, Dai Quang,Tran, Van Chien,Tran, Van Sung,Tran, Thi Phuong Thao
, p. 163 - 171 (2021/03/16)
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.
Hapten for broad-spectrum detection of sulfonylurea drugs,artificial antigen, antibody and application
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Paragraph 0041-0043; 0046, (2021/01/29)
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.
Styrene sulfone NLRP3 inflammasome inhibitor, preparation method and application thereof
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Paragraph 0053; 0154-0155, (2020/10/30)
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.
PROCESS FOR PREPARATION OF GLIPIZIDE
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Page/Page column 19, (2018/05/24)
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%.
N-(4-[2-(pyrazole-1-carbonamide)-ethyl]-benzenesulphonyl)-urea
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, (2008/06/13)
N-{4-[2-(Pyrazole-1-carbonamide)-ethyl]-benzenesulphonyl}-ureas of the formula 1 STR1 wherein R, R2 are a hydrogen atom or lower alkyl of up to 4 carbon atoms, R1 is a hydrogen, chlorine or lower alkyl atom containing up to 4 carbon atoms and R3 is an alkyl of 2 to 5 carbon atoms or cycloalkyl of 5 to 6 carbon atoms, and their method of preparation is described, said compounds possessing biological properties, capable of decreasing the sugar level in blood.