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aminoguanidine bicarbonate(cas2582-30-1) Protective effect​

Protective effect of aminoguanidine bicarbonate(cas2582-30-1) in a murine model of pulmonary fibrosis induced by bleomycin.


aminoguanidine bicarbonate(cas2582-30-1) is a drug known for more than a century, which has been attracting increasing interest in recent years due to the discovery of new pharmacological properties. This study investigated the effects of aminoguanidine bicarbonate(cas2582-30-1) on the fibrotic response induced by intratracheal administration of bleomycin to rats. Three groups of animals were studied: Group A (n = 19) corresponded to the control group. Group B (n = 20) received 10 IU/kg bleomycin intratracheal, and Group C (n = 12) received the same amount of bleomycin as Group B followed by 50 mg/kg/day aminoguanidine bicarbonate(cas2582-30-1) bicarbonate for 4 weeks. aminoguanidine bicarbonate(cas2582-30-1) led to significant reductions in total hydroxyproline content of the lungs in Group C compared to Group B (Group A: 1.83+/-0.14 mg x Group B: 3.46+/-0.36 mg x Group C: 2.09+/-0.22 mg). Morphometric collagen studies carried out on histological sections stained with Sirius red F3BA showed that aminoguanidine bicarbonate(cas2582-30-1) promoted a significant reduction of the area occupied by collagen in the axial and septal zones of the lungs (Axial region = Group A: 4.29+/-1.31% x Group B: 19.30+/-4.86% x Group C: 8.52+/-1.96%; Septal region = Group A: 0.15+/-0.06% x Group B: 0.61+/-0.21% x Group C: 0.15+/-0.06%). These results suggest that aminoguanidine bicarbonate(cas2582-30-1) is a potential therapeutic agent for the treatment and prevention of pulmonary fibrosis which is associated with different clinical conditions.


SYNTHESIS AND SCREENING OF CERTAIN ARYLOXYACETYLAMINOGUANIDINES AS POTENTIAL ANTIHYPERTENSIVE AGENTS


Ethyl aryloxyacetates (2a-k) have been synthesized either by the esterification of aryloxyacetic acids (1a-j) with ethanol in the presence of concentrated sulphuric acid or by reacting potassium naphthoxides with ethyl chloroacetate in dimethylformamide. Hydrazinolysis of either 1a, b, d, f, j or 2a-k furnishes the corresponding hydrazides (3). On the other hand, the acid chlorides (4f-h) have been prepared via the reaction of 1a-f with thionyl chloride in dry benzene, which on refluxing with aminoguanidine bicarbonate in dry benzene give the target aminoguanidine hydrochlorides (5a-h). Meanwhile, the desired aminoguanidine sulphates (5a-e) have been obtained by condensing 2a-e with S-methylisothiourea sulphate in aqueous ethanol. Additionally, the new aminotriazole sulphates (6a-h) are obtained either by refluxing 2a-h with S-methylisothiourea sulphate or by fusion of 1a,b, h, j with aminoguanidine sulphate. Structures of the new compounds are based on elemental analyses and IR, (1)HNMR and mass spectral data. Pharmacological screening, indicates that some of the newly synthesized compounds exhibit significant antihypertensive activity in both normal and renal hypertensive rats. Compound 5b produces significant decrease in the heart rate of normal rats. Compounds 5f and 5g have no significant effect. Compounds 5f,g, h have inhibition effect on the isolated rabbit intestine.


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