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Information × Registration Number 0222U003619, 0115U003873 , R & D reports Title Synthesis, physical, chemical and biological properties of 1,3,7,8-tetrasubstituted xanthines and their condensed derivatives popup.stage_title Head Romanenko Mykola Ivanovych, Доктор фармацевтичних наук Registration Date 07-05-2022 Organization Zaporizhzhya State Medical University popup.description2  The object of study is 1,3,7,8-tetrasubstituted of xanthine and their fused derivatives. The aim of the study - synthesis of new and low-toxic compounds - 1,3,7,8-tetrasubstituted and condensed xanthine derivatives with diuretic, analgesic, antioxidant, anti-inflammatory, hypoglycemic, antimicrobial activity, which may be the basis for the creation of new medications, establishment of regularities between chemical structure and biological action. Research Methods - Preparative organic synthesis of 1,3,7,8-tetra¬substituted of xanthine and their fused derivatives. The use of IR-, NMR- spectroscopy to confirm the structure of the synthesized compounds. Biological activity on in vitro and in vivo models. Results and novelty - For the first time, by varying the pharmacophore substituents at positions 1, 7 and 8 of the xanthine molecule, the possibility of purposeful synthesis of new biologically active compounds with a predetermined pharmacological action is demonstrated. For the first time, a number of 1- and 7- substituted of 8-bromo-3-methylxanthine (1,3-dimethylxanthine) were obtained by reacting the corresponding bromoxanthines with alkyl, aralkyl halides, halogen alcohols, ethers, halogen ketones, nitriles, amides and esters of chloroethanes. The reactions of the starting bromoxanthines with various primary and secondary amines, amino alcohols, amino ethers, diamines, and secondary amines of the heterocyclic structure have been studied, which significantly expands the chemical library of bioactive xanthine derivatives. The reactions of 8-brom-7- (2-hydroxy-2- m-ethylphenoxypropyl-1-) theophylline with primary and secondary heterocyclic amines were studied, which made it possible to offer available methods for the synthesis of 8-amino substituted of 7- (2-hydroxy-2-m- ethylphenoxypropyl-1-) theophylline and 6,8-dimethyl-2-m-ethylphenoxymethyl-2,3-dihydro-1,3-oxazolo [2,3-f] theophylline. It is the first time 7-substituted xanthinyl-8-aminoalkanoic acids and their Product Description popup.authors Ivanchenko Dmytro Hryhorovych popup.nrat_date 2022-05-07 Close