Category: 1125-56-0

Jones, James Holden published the artcilePyrazine diuretics. IV. N-Amidino-3-amino-6-substituted pyrazinecarboxamides, Related Products of pyrazines, the main research area is PYRAZINECARBOXAMIDES; DIURETICS; SALURETICS.

cf. CA 67: 100105q. The synthesis of a series of N-amidino-3-amino-6-substituted pyrazinecarboxamides (I) (R = MeS, MeSO2, PhCH2S, and Me2N) is described. Since more direct synthetic routes were unsuccessful, the intermediate 3-amino-6-substituted pyrazinecarboxylic acids were synthesized by nucleophilic displacement of the Cl from 6-chloro-4(3H)-pteridinones or their 3-methyl derivatives, followed by alk. hydrolysis. These were cyclized to the 2-methyl-6-substituted 4H-pyrazino[2,3-d][1,3]oxazin-4-ones, which upon reaction with a guanidine followed by hydrolysis, afforded the desired compounds When the N-amidino-3-amino-6-substituted pyrazinecarboxamides were assayed for saluretic and diuretic activity in normal rats, the 6-methylthio and the 6-benzylthio derivatives proved to be the most potent, while in the corresponding 3-acetamido series, the outstanding members were the 6-methylthio and the 6-methoxy derivatives

Journal of Medicinal Chemistry published new progress about Diuretics. 1125-56-0 belongs to class pyrazines, name is 3-Amino-6-chloropyrazine-2-carboxamide, and the molecular formula is C5H5ClN4O, Related Products of pyrazines.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Jones, James Holden published the artcilePyrazine diuretics. V. N-Amidino-3-aminopyrazinecarboxamidines and analogous 2,4-diaminopteridines, Recommanded Product: 3-Amino-6-chloropyrazine-2-carboxamide, the main research area is PYRAZINES DIURETICS; AMIDINOPYRAZINECARBOXAMIDINES; DIAMINOPTERIDINES DIURETICS; DIURETICS PYRAZINES; PTERIDINES DIAMINO.

The synthesis of a series of N-amidino-3-aminopyrazinecarboxamidines (I), principally by the reaction of a 3-aminopyrazinecarbonitrile with an appropriate guanidine, is described. Cyclization of selected members of this series afforded the analogous 2,4-diaminopteridines (II). The required 3-aminopyrazinecarbonitriles were prepared from the corresponding carboxamides; 3-amino-5,6-dichloropyrazinecarbonitrile yielded a variety of 5-substituted derivatives by nucleophilic displacement of the 5-chloro group. I exhibited diuretic activity as measured by several assay methods in rats and dogs. These compounds were generally less active than the corresponding 2,4-diaminopteridines which, in turn, were less potent than the corresponding N-amidino-3-aminopyrazine-carboxamides. 16 references.

Journal of Medicinal Chemistry published new progress about Diuretics. 1125-56-0 belongs to class pyrazines, name is 3-Amino-6-chloropyrazine-2-carboxamide, and the molecular formula is C5H5ClN4O, Recommanded Product: 3-Amino-6-chloropyrazine-2-carboxamide.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Lin, Songnian published the artcileNovel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2), Product Details of C5H5ClN4O, the main research area is aminopyrazine amine isothiocyanate condensation; aminopyrazinylmethyl thiourea preparation antiinflammatory antiarthritis; protein kinase 2 inhibition structure activity.

Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas, i.e. I, are described as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). These compounds demonstrate potent in vitro activity against the enzyme with IC50 values as low as 15 nM, and suppress expression of TNFα in THP-1 cells and in vivo in an acute inflammation model in mice. The synthesis, structure-activity relationship (SAR), and biol. evaluation of these compounds are discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 1125-56-0 belongs to class pyrazines, name is 3-Amino-6-chloropyrazine-2-carboxamide, and the molecular formula is C5H5ClN4O, Product Details of C5H5ClN4O.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem