Hypoglycemic activity

A number of 4-pyrazolylpyridinium salts (687) have been found to have hypoglycemic activity in several animal models (68JMC981). The possibility that the corresponding 4-pyrazolylpyridine I-oxides might also exhibit this type of activity was investigated without success (69JMC945). 

Azaquinolizinium tetrafluoroborate, 2-ethoxy-synthesis, 2, 573 1 -Azaquinolizin-2-one dipolar character, 2, 572 synthesis, 2, 575 UV spectra, 2, 572 1 - Azaquinolizin-4-one hypoglycemic activity, 2, 575 reactions, 2, 574 synthesis, 2, 575 UV spectra, 2, 572... 

Meguro and co-workers described the synthesis and hypoglycemic activity of 4-oxazoleacetic acid derivatives." For example, cyclization of 18 was performed by using phosphorus oxychloride in refluxing toluene to provide 5-methyI-2-(l-methylcyclohexyl)-4-oxazoleacetate in 73% yield and the subsequent hydrolysis gave 19. 

Systematic modification of the sulfanilamide molecule in order to maximize the hypoglycemic activity led to the observation that the sulfonamide is best replaced by a sulfonylurea function. Modification on both the aromatic ring and the substituent on the terminal nitrogen modulates the activity of the products. ... 

It is of note that hypoglycemic activity is maintained even when the aromatic ring is fused onto a carbocyclic ring. Chlor-sulfonation of hydrindan gives chloride, 206. Reaction of the sulfonamide (207) obtained from that intermediate with cyclohexyl isocyanate leads to glyhexamide (208). ... 

Rice bran hemicelluloses reduce thymus atrophy in rats (Takenaka, 1992). Hikino et al. (1988) isolated and purified four glycan fractions from rice bran hemicelluloses and named them as Oryzabrans A, B, C, and D. All these glycans were shown to improve the peripheral utilization of insulin, resulting in significant hypoglycemic activity (Hikino et al., 1988 Hikino and Hayashi, 1989). Several investigations into rice bran polysaccharides and hemicelluloses (Masayoshi et al., 1987) have indicated a strong improvement in the immune... 

HIKING H, TAKAHASHi M, osHiMA Y, KONNO c (1988) Isolation and hypoglycemic activity of oryzabrans A, B, C, and D, glycans of oryza sativa bran. Planta Med, 54(1) 1-3. 

Anti-nephritis activity and anti-nephrosis activity Hypoglycemic activity Cholesterol decreasing effect... 

NONCYCLIC ALIPHATICS Many of the biguanides have oral hypoglycemic activity, and metformin (87) is such an antidiabetic agent. Cyanamide has a highly reactive nitrile function because of the electropositive NH2 group... 

Isolated from seeds of Billia 2-(Methylenecyclopropyl)glycine -hippocastanum and fruits of hypoglycemic activity and... 

Perez Gntierrez RM, Vargas SoUs R, Garcia Baez E, Navarro YG (2009) Hypoglycemic activity of constituents from Astianthus viminalis in normal and streptozotocin-induced diabetic mice. Nat Med (Tokyo) 63 393-401. 

Yoshikawa M, Murakami T, Ueno T, Kadoya M, Matsuda H, Yamahara J, Murakami N. (1995) Bioactive saponins and glycosides, i. senegae radix. (1) E-senegasaponins a and b and z-senegasaponins a and b, their inhibitory effect on alcohol absorption and hypoglycemic activity. Chem Pharm Bull 43 2115-2122. 

Hukeri GA, Kalyani HK. (1988) Hypoglycemic activity of flavonoids of Phyllanthus frametus in rats. Fitoterapia 59 68-70. 

Contreras C, Rom i R, Perez C, Alarcon F, Zavala M, Perez S. (2005) Hypoglycemic activity of a new carbohydrate isolated from the roots of Psacalium peltatum. Chem Pharm Bull 53 1408-1410. 

A series of esters of nuclear halogenated 3-carboxy-1,2,3-benzotriazin-4(3//)-ones show depressant activity, while the benzoate esters of substituted 3-(2-hydroxyethyl)-l,2,3-benzotriazin-4(3f0-one are reported to function as coronary dUating agents," as do certain other compounds of this type." 3-(o-Haloaryl)-l,2,3-benzotriazin-4(3i/> ones are claimed to have antisecretory," anoretic, anticonvulsant, and hypoglycemic activity, and a variety of other 3-aryl derivatives are stated to be relaxants, tranquilizers, sedatives, hypnotics, or cramp inhibitors. A number of derivatives of 10, R = H, in which the 3-substituent is a long alkyl chain containing a terminal sulfonamide group have been claimed to act. as antidiabetics. ... 

Tolazamide is slowly absorbed and its hypoglycemic action only becomes manifest after several hours. Its is metabolized in the liver with an elimination half-life of about 7 hours. However several of its metabolites retain hypoglycemic activity. Its duration of action is shorter than that of chlorpropamide. 

Glibenclamide has an intermediate duration of action. It is well absorbed with peak levels 4 hours after oral dosing. Its protein binding is about 90%. Glibenclamide is metabolized in the liver with an elimination half-life of 10 hours. However some of the metabolites which are excreted in the urine have hypoglycemic activity which makes glibenclamide... 

Glimepiride is more rapidly absorbed than glicazide with peak plasma concentrations after 2-3 hours. It has very high protein binding of over 99%. Glimepiride is metabolized in the liver with and elimination half-life of 3-6 hours. Its active hydroxy metabolite has an elimination half-life of 5-8 hours and is responsible for part of the hypoglycemic activity of glimepiride. 

Hypoglycemic activity. Ethanol extract of the leaf, administered orally to rats at a dose of 250 mg/kg, produced less than a 30% drop in blood sugar level " . Fruit juice, administered intravenously by infusion to dogs at a dose of 3 mL/min for 100 min, was active " ". Hot water extract of the dried shell, administered hy gastric intubation to dogs at a dose of 200 mL/animal (20 g of... 

Hypoglycemic activity. Dried leaf, in tbe ration of male mice at a concentration of 6.25% of the diet for 28 days, was inactive vs streptozotoc in-induced hyperglycemia° . Ether extract of the fresh root, administered subcutaneously to dogs, rabbits, and human adults, was active ... 

DC 103 Neef, H., P. De Clercq, and G. Laeke-man. Hypoglycemic activity of selected European plants. Pharm World Sci 1993 15(6) HI 1-. DC116... 

Hypoglycemic activity. Water extract of the fermented root, administered intravenously to rabbits, was active "" The dried seed, administered orally to eight healthy volunteers at a dose of 50 g/person, was active. A single dose resulted in a glycemic index of 68.7 and an insulinemic index of... 

OE124 Gonzalez, M., A. Zarzuelo, M. J. Gamez, M. P. Utrilla, J. Jimenez, and I. Osuna. Hypoglycemic activity of olive leaf. 

Hypoglycemic activity. Dried grain, taken orally by human adults at a dose of 162 g/ person, was active, results were significant at p less than 0.001 level . Water extract of the dried seed coat of cultivar Fukuyuki, administered intraperitoneally to mice at a dose of 100 mg/kg, was active k Hypotensive activity. Ethanol (50%) extract of the grain, administered intravenously to dogs at a dose of 50 mg/kg, was active . 

---