Sulfonylurea derivatives

Sulfonates, aliphatic la 388, 389 Sulfones lb 321,360 Sulfonic acids la 91 Sulfonylurea derivatives lb 204 Sulfoxides lb 321,358,360,372,373,374 Sulfur compounds lb 338 Sulfur-containing compounds lb 301,339 Sulfur dioxide vapor la 86 -, dipole moment la 97 Sulfur, divalent lb 302 Sulfuric acid la 87,195,333,411,426 Sulfur ions lb 302 Sulfutyl chloride vapor la 86 Sulpyrid lb 268 Sunflower seed oil lb 286 Surfactant-TLC plates la 89 Sweeteners la 44, 388-390 Swep la 108... 

Various substituted sulfonylurea derivatives, partly in use as diabetes drugs, have been coordinated to Cd and Hg. Besides the IR and [H NMR spectra of several species, the structures of one each of the Cd and Hg compounds have been solved.155 In the Cd complex three ligands act as... 

The combination of metformin with various sulfonylurea derivatives has been extensively reviewed (15). When metformin or pioglitazone were added to sulfonylureas in patients with type 2 diabetes who were poorly controlled, those with reduced pancreatic beta cell function responded better to metformin, while those with greater insulin resistance responded better to pioglitazone (23). 

Sulfonylurea derivatives such as tolbutamide (Figure 5.14) bind to the sulfonylurea receptor and thereby promote the closing of the Kj, channel. This amplifies the secretion of insulin - a desirable effect in type II diabetics, who suffer not from an absolute lack of insulin (as type I diabetics do) but from an inadequate response to it. Sulfonylurea drugs can be used orally, which is more convenient than insulin therapy. It is also less prone to result in excessive insulin action (hypoglycemia), since the physiological signal is amplified but not substituted. However, commonly the (3-cells wear out eventually, and insulin therapy has to be instituted anyway. 

Another, as yet experimental use of sulfonylurea derivatives targets the Kj, channels in the heart in certain forms of arrhythmias. The sulfonylurea receptors in the heart are somewhat different from those in the (3-cells, which makes selective drug action possible. Closing potassium channels should increase the excitability of heart muscle cells - in contrast to the effect of sodium (and calcium) channel blockers Don t worry, though - the cardiologists will find a way to show us why this is a good thing, like old farm-... 

Schulz E, Koch K, Schmidt FH. [Potentiation of the hypoglycemic effect of sulfonylurea derivatives by drugs. II. Pharmacokinetics and metabolism of glibenclamide (HB 419) in presence of phenylbutazone.] Eur J Clin Pharmacol 1971 4(l) 32-7. 

Blood sugar lowering compounds sulfonylurea derivatives Standards for the assessment of combination products 1992-04... 

Toradol " ketorolac trometamol. toramazoline hydrochloride tramazoline. torasemide [ban. inn) (torsemide [usan] Oemadex ) is a sulfonylurea derivative, which acts as a (loop) DIURETIC. It can be used as an anthiypertensive and to treat oedema, especially in renal failure, torbugesic butorphanol. 

Structural chemists and kidney physiologists responsible for chlorothiazide development for the control of high blood pressure and of edema associated with cardiac failure. Thiazidic compounds and furosemide, another sulfonylurea-derived diuretic, are now universally accepted as a primary treatment for hypertension. 

Vicentini, C. B., Guarneri, M., Sarto, G. Hypoglycemic compounds. Sulfonylurea derivatives containing amino acids and dipeptides. Farmaco, Ed. Sci. 1983, 38, 595-608. 

Legtenberg RJ, Houston RJ, Oesebuig B, et al Effects of sulfonylurea derivatives on ischemia-induced... 

Sulfonylureas derived from pyrimidine (and 1,2,4-triazine) are of considerable importance among the more recently introduced growth regulators for herbicides, e.g. bensulfuronmethyl 43. 

Chrysoidine, which was a deep-red dye, had to be grafted to a sulfonylurea derivative (sulfamidochrysoidine) in order to be active. In 1932, it was studied by two chemists, Fritz Mietzsch and Josef Klarer. Testing the new dye on laboratory rats and rabbits infected with streptococci bacteria, Domagk found that it was highly antibacterial but not toxic. It was called Streptozan , but its name soon changed to Prontosil . 

Acetohexamide is used as an oral antidiabetic agent for the treatment of ketoacidosis-resistant diabetes. It is an intermediate acting sulfonylurea derivative. The clinical effects of lowering elevated blood glucose levels Is similar for all of the sulfonylurea derivatives. Acetohexamide, however. Is the only one to also possess uricosuric activity and therefore Is a preferable agent to treat diabetic patients with gout. 

Acetohexamide Is a sulfonylurea derivative, that produces Its hypoglycemic effect by stimulating the Islet tissue to synthesize and release endogenous Insulin (40). The hypoglycemic effects are also attributed to an Increased sensitivity of Insulin receptors as well as Improved peripheral utilization of Insulin (37). 

A mixture of 2-p-dilorobenzenesulfonylimino-l,3-oxathiolane and piperidine in acetonitrile allowed to stand 16 hrs. at room temp. sulfonylurea deriv. Y ... 

Reaction with Amino Derivatives. Methyl A (jO-toluenesul-fonyl)carbamate serves as an electrophilic partner in the suhstitu-tion reaction with amines and afforded a good yield of sulfonylurea derivatives. The sulfonylurea derivatives so obtained were converted into carboxamidine derivatives in moderate yields via the imidoyl chloride intermediates, which are prepared by chlorination using phosphorus pentachloride in chlorobenzene and showed high reactivity with a broad range of amines (eq 4). 

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