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Information × Registration Number 0225U000029, (0121U107435) , R & D reports Title Synthesis and study of fused heterocyclic systems containing the 7-deazapurine fragment popup.stage_title Хімічна оптимізація структури активних сполук – конденсованих гетероциклічних систем з фрагментом 7-деазапурину. Head Smolii Oleh B., д.х.н. Registration Date 02-01-2025 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description1 Development of preparative and effective methods for the synthesis of new functionalized derivatives of 7-deazapurine and polycyclic systems containing the pyrrolo[2,3-d]pyrimidine fragment and conducting biological studies of the obtained compounds and establishing a pattern of "structure - activity". popup.description2 Approaches to the synthesis of new functionalized 7-deazapurine derivatives and fused pyrrolo[2,3-d]pyrimidines based on them have been developed. Among the tricyclic pyrimido[5',4':4,5]pyrrolo[1,2-a][1,4]diazepine derivatives, new representatives of adenosine A2A receptor antagonists have been found for the first time, which may be promising in the treatment of a number of neurodegenerative diseases. Based on methyl esters of pyrrolo[2,3-d]pyrimidine-6-carboxylic acids, preparative methods for the synthesis of new pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidines have been developed. Among the tricyclic pyrrolo[2,3-d]pyrimidine derivatives, compounds that exhibit inhibitory activity against telomerase have been found for the first time. Directed modification of the pyrrolopyrimidine ring has shown promise for the synthesis of new structural analogues of trilaciclib, in particular disubstituted derivatives of dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidine. It was found that most of the synthesized pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidines inhibit acetylcholinesterase in the micromolar concentration range. Product Description popup.authors Biletskyi Ihor І. Verves Yevhenii V. Kucher Oleksandr V. Muzychka Liubov V. Yaremchuk Iryna О. popup.nrat_date 2025-01-02 Close