Guanidine, amidino-

More recently, ammonium sulphonates have proved excellent reagents for converting cyano- into amidino-groups (488). Applied to the present case, the use of ammonium sulphonates at 140—160° is particularly useful in the production of 1-arylbiguanides (44, 488, 613, 614). As expected, action of two moles of ammonium sulphonates results in guanidines. 

Guanidine and amidino phenyfesters of substituted benzoic adds act as temporary inhibitors of serine proteases and may serve for the preparation of stable... 

Methyl-6-R-4//-pyrazino-(2,3-d] 11,3 ]oxazin-4-ones (where R = MeS, MeSO, PhCH,S,Me,N,MeO, Piperidino, Pi NH, PhCHjNH) Guanidine 2-Acetamido-3-amidino- carbamoyl-5-R 432... 

The functions of the guanidine-modifying enzymes further subdivide the family into three distinct groups hydrolases, dihydrolases, and amidinotransferases. Hydrolases catalyze the hydrolysis of guanidine derivatives to form ureido compounds, whereas dihydrolases catalyze a hydrolysis reaction to yield a primary amine, ammonia, and bicarbonate (or carbon dioxide). The amidinotransferases transfer an amidino group from one substrate to an amine. Although these are distinct reactions, they are characterized by common structural and mechanistic themes. 

Bisacchi G, Slusarchyk WA, Treuner U, et al. Preparation of amidino and guanidine azetidinone compounds as hyptase inhibitors. WO 9967215, 1999. 

Purified transamidinase preparations from S. griseus and 5. hikiniensis and a crude preparation from S. hluensis catalyzed, when incubated in the presence of L-arginine, the formation of phosphate esters of N-amidino-scyZ/o-inosamine, N-amidino-streptamine and N-amidino-2-deoxy-streptamine from phosphate esters of scy/Zo-inosamine, streptamine and 2-deoxy-streptamine, respectively. None of the enzyme preparations, however, catalyzed the addition of a second amidine group to these monoguanidinated molecules. It is not known whether this second guanidine group is derived via another transamidination reaction or by a different mechanism. 

Type C Syntheses [N—C—N—C—S]. From amidino-thiono-compounds. The general synthesis of 1,2,4-thiadiazoles by the oxidative cyclization of compounds incorporating the amidino-thiono-grouping [—C(=NH)NHCS—] has been extended by the synthesis of l-acyl(and -sulphonyl)-3-thioacyl-guanidines (41) from acyl- or sulphonyl-guanidines (40) with thioacid O-esters in the presence of sodium hydride, followed by their oxidation with hydrogen peroxide in pyridine. 

BS 110—141, N-amidino-2-(2,6-dichlo-rophenyljacetamide HCl is a guanidine derivative, but its pharmacological action resembles that of clonidine it possesses a central os-adrenoreceptor stimulant activity and causes a centrally induced fall in blood pressure, due probably to lowering of sympathetic activity and reduction of circulatory pressor reflexes. Apparently because of this, postural hypotension seems to be rare. In a series of 15 patients some general side effects were recorded and (surprisingly) the development of a tremor in 5 on a 3—6 mg daily dose (22 =). 

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