China
Africa
Explore chapters and articles related to this topic
Galactosialidosis
Published in William L. Nyhan, Georg F. Hoffmann, Aida I. Al-Aqeel, Bruce A. Barshop, Atlas of Inherited Metabolic Diseases, 2020
Effective specific therapy has not been devised. The availability of animal models should permit studies on gene transfer as an approach to therapy. Bone marrow transplantation has been successful in PPCA (2/2) mice [87]. Chemical Chaperone therapy with N-Octyl-4-epi-β-valienamine (NOEV) was found [89] to stabilize and enhance β-galactosidase activity in cultured fibroblasts derivred from 4 patients.
Biocatalyzed Synthesis of Antidiabetic Drugs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Voglibose (Fig. 11.53, 191), ATC Code A10BF03, DrugBank Code DB04878 (trade name Voglib, marketed by Mascot Health Series), an N-substituted derivative of valiolamine 192, is a branched-chain aminocyclitol, or pseudo-amino sugar, whose N-substituted moiety is derived from glycerol. Voglibose is an alpha-glucosidase inhibitor used for lowering post-prandial blood glucose levels in people with diabetes mellitus (Kawamori et al., 2009; Derosa and Maffioli, 2012; Campo et al., 2013). The chemical synthesis of 191 starting from 192 has been described by different methodologies (Chen et al., 2006); on the other hand, 192 was first isolated from the fermentation broth of Streptomyces hygroscopicus subsp. Limoneus IFO12703 (Kameda et al., 1984), although it can be also be obtained either through stereoselective transformation of valienamine 193 or validamine 194 (Horii et al., 1985), or by chemical total syntheses starting from different natural precursors (Shing and Cheng, 2008; Ji et al., 2013; Quan et al., 2013). Finally, 193 can be obtained from biocatalytic hydrolysis of naturally occurring validoxylamine A 195 or validamycin 196 (Zheng et al., 2006; Xue et al., 2007); on the other hand, 193 is one of the components of acarbose 197, a pseudotetrasaccharide in which this polyhydroxylated aminocyclohexene portion is linked via its nitrogen atom to an acarviosine unit, constituted by 6-deoxyglucose α-1,4-linked to a maltose moiety. Acarbose (ATC Code A10BF01, DrugBank Code DB00284) is generic sold in Europe and China as Glucobay (Bayer AG), in North America as Precose (Bayer Pharmaceuticals), and in Canada as Prandase (Bayer AG). Some aminocylclitol-type of glycosidase inhibitors.
Diaryl azo derivatives as anti-diabetic and antimicrobial agents: synthesis, in vitro, kinetic and docking studies
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Tehreem Tahir, Mirza Imran Shahzad, Rukhsana Tabassum, Muhammad Rafiq, Muhammad Ashfaq, Mubashir Hassan, Katarzyna Kotwica-Mojzych, Mariusz Mojzych
Diabetes Mellitus (DM) is a well characterised metabolic disease that results in defects in insulin output i.e. insulin secretion (type-1 diabetes) and insulin action (type-2 diabetes) or both. Type-2 diabetes accounts for 70–80% of all diabetic patients worldwide and it leads to postprandial hyperglycaemia. One of the critical strategies to prevent postprandial hyperglycaemia is to inhibit the enzymes which are responsible for the carbohydrate hydrolysis e.g. α-amylase and α-glucosidase. In this interest, several α-glucosidase inhibitors are being administered in the treatment of type-2 diabetes such as acarbose (valienamine), voglibose (valiolamine) and miglitol (desoxynojirimycin). However, the prolonged use of these agents could result in various side effects such as vomiting, pomposity, diarrhoea and flatulence. Therefore, the discovery and development of new and potent α-glucosidase inhibitors have gained immense attention in pharmaceutical chemistry8–10. In this regard, a new derivative from a series of sulphonamide containing diarylpentadienones was found to be a promising inhibitor of α-glucosidase (IC50 5.69 ± 0.5 µM) with the competitive mode of inhibition11, some new benzamide derivatives of thiourea (IC50 range 20.44 − 333.41 µM) were evaluated as good candidates for targeting α-glucosidase enzyme12. The literature also suggested that the derivatives of triazole thiones were found to be effective inhibitors of α-glucosidase (IC50 value 36.11 μg/mL)13. The recent research has suggested that polyphenols are excellent anti-diabetic agents, recently in this interest; the α-glucosidase inhibitory potential of flavonoids was compared with acarbose with the sequence of inhibitory potential as scutellarein > nepetin > apigenin > hispidulin > acarbose14. Dihydropyridine derivatives (IC50 range 2.21 ± 0.06 − 9.97 ± 0.08 μM)15 have been reported as potential α-glucosidase inhibitors.