62932-78-9

Upstream product

• 63901-90-6 8-bromo-7-(3-chloro-2-hydroxypropyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione 
• 100-46-9 benzylamine 

Relevant academic research and scientific papers

Structure-cardiovascular activity relationships in a group of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3-aminopropyl)-3,7-dihydro-1H-purine-2, 6-diones

On the basis of our earlier studies in a group of 7,8-disubstituted derivatives of 1,3-dimetyl-3,7-dihydropurine-2,6-dione, a series of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3-aminopropyl)-3,7-dihydropurine-2, 6-diones (8-15) were synthesized and tested for their electrocardiographic, antiarrhythmic and hypotensive activity and for 1- and 2-adrenoreceptor affinities. Among the new derivatives, compounds with the 7-[2-hydroxy-3-(4-phenylpiperazine)-propyl] substituent (9-11) displayed prophylactic antiarrhythmic activity in epinephrine-induced arrhythmia. Analogue 10 with the 8-(2-morpholin-4-yl)-ethylamino group was the most active (ED 50 = 3.9 mg/kg and TI = 59.8), which may indicate that this substituent is preferably important for the antiarrhythmic effect. Only compound 11 with the 8-(2-diethylamino)-ethylamino group significantly decreased the systolic (20.4-28.1%) and diastolic (23.4-33.2%) pressure, but this effect lasted for only 1-5 min. The pharmacologically active compounds 9-11 with the phenylpiperazine moiety showed affinity for 1-receptors (Ki = 0.143-0.383 μM), but the other compounds were almost (12-15) or completely (8) inactive at this site. Compounds 9-11 and 13-15 displayed moderate to low affinity for 2-receptors (Ki = 0.36-2.7 μM). Copyright

Synthesis of bronchospasmolytically effective β phenylethyl aminoalkyl xanthines

New theophylline and theobromine derivatives are synthesized from the β phenylethylaminoalkyl xanthines, whose phenyl substituent is substituted by one or two hydroxyl groups and partially also by other substituents. Different methods of synthesis are described, among them the production of the bronchospasmolytic 7 (3 [2 (3,5 dihydroxyphenyl) 2 hydroxy ethylamino] propyl) theophylline (reproterol . HCl).