Activity antidiabetic

Hydroxyhyda.ntoins. Some 5-hydroxyhydantoins such as (24) and (25) have shown antidiabetic activity (108). In some cases they are also diuretics and hypolipemics. These properties are probably related to the urea moiety found in these compounds. 

Yet another example of a so-called pharmacophoric group is the biguanide functionality, a grouping associated with oral antidiabetic activity (see the section on sulfonylureas for a fuller discussion of this activity). Condensation of 2-phenethylamine with dicyanamide affords directly the orally active hypoglycemic agent phenformin (88). ... 

Chung, S. H., Choi, C. G., and Park, S. H. (2001). Comparisons between white ginseng radix and rootlet for antidiabetic activity and mechanism in KKAy mice. Arch. Pharm. Res. 24, 214-218. 

Harris CS, Lambert J, Saleem A, et al (2008) Antidiabetic activity of extracts from needle, bark, and cone of Picea glauca organ-specific protection from glucose toxicity and glucose deprivation. Pharm Biol 46 126-134... 

Daisy P, Jasmine R, Ignacimuthu S, Murugan E. (2009) A novel Steroid from Elephantopus scaber L., an ethnomedicinal plant with antidiabetic activity. Phytomedicine 16 252-257. 

Tan MJ, Ye JM, Turner N, Hohnen-Behrens C, Ke CQ, Tang CP, Chen T, Weiss HC, Gesing ER, Rowland A, James DE, Ye Y. (2008) Antidiabetic activities of triterpenoids isolated from bitter melon associated with activation of the AMPK pathway. Chem Biol 15 263-273. 

Korec R, Sensch KH, Zoukas T. (2000) Effects of the neoflavonoid coutareagenin, one of the antidiabetic active substances of Hintonia latiflora, on streptozotocin-induced diabetes mellitus in rats. Arzneimittelforschung 50 122-128. 

Enoki T, Ohnogi H, Nagamine K, Kudo Y, Sugiyama K, Tanabe M, Kobayashi E, Sagawa H, Kato 1. (2007) Antidiabetic activities of chal-cones isolated from a Japanese Herb, Angelica keiskei. JAgric Food Chem 55 6013-6017. 

Miura T, Ichiki H, Hashimoto I, Iwamoto N, Kato M, Kubo M, Ishihara E, Komatsu Y, Okada M, Ishida T, Tanigawa K. (2001) Antidiabetic activity of a xanthone compound, mangiferin. Phytomedicine 8 85-87. 

The 3-indolylbenzoquinone fragment is a core structure in a number of biologically active natural products such as asterriquinones [49, 50]. The asterriquinones and demethylasterriquinones exhibit a wide spectrum of biological activities, including antitumor properties, and are inhibitors of HIV reverse transcriptase [51-53]. Asterriquinone Al has been shown to stop the cell cycle in G1 and promote apoptotic cell death [54, 55]. Recently, asterriquinone has been reported to be an orally active non-peptidyl mimetic of insulin with antidiabetic activity [56]. The simplest and the most straightforward approach for the synthesis of indol-... 

Antidiabetic activity. Masoprocol, a compound derived from Larrea, administered orally to streptozotocin-induced diabetic... 

Antidiabetic activity. Dietary psyllium fiber, administered to patients with type 2 diabetes at three doses of 5 g each daily be-... 

Monocyclic (3-lactams tetrasubstituted have been reported for antidiabetic activity, as they are able to control diabetic hypercholesterolemia. Induction of diabetes was confirmed by a significant rise in serum glucose and a depression in hepatic glycogen contents that control the cholesterol metabolism. 

Comparison of V(IV,V) hydroxamic acid complexes showed the V(V) complex induced a stronger insulin-enhancing effect than the V(IV) complex, and both complexes were better than either of the salts, vanadyl sulfate or sodium vanadate, in relieving the symptoms of mice with STZ-induced diabetes. The distribution of vanadium in tissues was the same irrespective of the complex administered however, the tissue distribution of vanadium when the salts were administered was different from that seen after vanadium complex administration [146], These results suggest that the difference in the antidiabetic activity of the hydroxaminic acid V complexes is related to the different oxidation state, although there was no difference in the final tissue distribution of these complexes. 

Some 2-deoxy-analogues of rubrosterone have been reported.73 The synthesis commenced with a Bamford-Stevens reaction upon 3/3,17/3-diacetoxyandrost-5-en-7-one tosylhydrazone to yield the corresponding 5,7-diene. Successive chromic acid and selenium dioxide oxidation of this diene furnished the 2-deoxyrubrosterones (177 R1 = OAc, R2 = H, R3 = OH, X= 17/3-0Ac,H 5a-H) and (177 R = OAc, R2 = R3 = H, X = 17/3-OAc,H 5a-H) respectively. Alkaline hydrolysis of the latter derivative afforded an A-homo-B-nor-steroid (178). The rubrosterone (177 R1 = R2 = R3 = OH, X = O 5/3-H), which possesses antidiabetic activity, has been prepared by oxidative degradation of the cholestene (179), itself obtained from ecdy-sterone.74... 

More recent studies have confirmed that dual activation of PPARy and PPARo subtypes would be beneficial for treating type-2 diabetes [ 139]. In this connection KRP-297, a TZD derivative has been found to express in vitro as well as in vivo affinity for both the PPARo and PPARy subtypes [152], In light of this, Desai and co-workers have investigated the PPARoj/y dual agonistic activity of a series of TZD and oxazolidinedione derivatives (comp, a. Fig. 22, Table 14) to assess their antidiabetic activity [153,154],... 

Discovery of a small molecule insulin mimetic with antidiabetic activity in mice. Science 1999 284 974-977. 62. 

The simple dioxolanone 309 has been prepared and has antidiabetic activity <2003W02550>, and the dioxolone structure 310 has been used as a pro-drug for pharmaceutically active amines R 2NH to which it is degraded in vivo <1995USP5466811>. Dioxolanone-containing compounds such as 311 have squalene synthetase and cholesterol synthetase inhibitory activity and can be used to treat hypercholesterolemia <2001JPP187789>. 

In an effort to obtain LA derivatives with improved antidiabetic activity <2006JME4072>, a class of hybrid LA derivatives was prepared, including 366 and water-soluble analogue 367, containing l,3-thiazolidine-2,4-dione moiety covalently bonded via C-5 to an amide linker. 

Pyrazinamide is one of the most powerful drugs available for the inhibition of urate excretion in man, consistently providing a 80-90% reduction in the renal clearance of uric acid (1401, 1403). 2-Morpholinocarbonylpyrazine and its 6-methoxy derivative are claimed to have antidiabetic activity (948, 949, 1351, 1387, 1404), and some 2-(p-ureidosulfonylphenethylcarbamoyl)pyrazines have been shown to have hypoglycemic activity in mice (1405). The effect of 2-amino-3-hydroxy-carbamoylpyrazine on DNA synthesis by Erlich ascites tumor cells in vitro has been investigated (1406) as well as the inhibition by 2-amino-3-hydroxycarbamoylpyrazine on L-histidine carboxylyase (1407) many 2-hydroxyimidazo[4,5-6]pyrazines (prepared from 2-amino-3-hydrazinocarbonylpyrazines with nitrous acid) are potent hypotensive agents in animals (880,891,963,1181). 

This section describes compounds developed as CNS agents for the treatment of obesity or depression for which independent hypoglycaemic activity has been observed. Whether or not this secondary effect is also centrally mediated is unclear. The first of these agents to be identified was fenfluramine (87), a serotonin agonist anorectic agent developed in the early 1960s. Its antidiabetic activity has been studied in animals and man and has been recently reviewed [384, 385]. 

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