Аннотация:
Structural optimization of butyrylcholinesterase inhibitors, 5-bromomethyl- and 5-iodomethyl-N,N-disubstituted 2-aminothiazolines, led to a series of their annulated bicyclic analogues, obtained by intramolecular cyclization of cycloalkenylthioureas. The most active compound in this series, cyclohepta[d]thiazol-2-amine, is a mixed-type butyryl-cholinesterase inhibitor with IC50 = 130 nm, highly selective compared to acetylcholinesterase and non-toxic at 100 μm concentrations.
Образец цитирования:
E. V. Nurieva, A. A. Alexeev, N. A. Zefirov, E. R. Milaeva, N. V. Kovaleva, A. N. Proshin, G. F. Makhaeva, O. N. Zefirova, “Annulated bicyclic isothioureas: identification of active and selective butyrylcholinesterase inhibitors”, Mendeleev Commun., 33:1 (2023), 77–79
Образцы ссылок на эту страницу:
https://www.mathnet.ru/rus/mendc313
https://www.mathnet.ru/rus/mendc/v33/i1/p77
Эта публикация цитируется в следующих 5 статьяx:
N. A. Zefirov, E. V. Nurieva, I. A. Elisseev, Sh. A. Khasanov, M. A. Niukalova, V. V. Zarubaev, O. N. Zefirova, Mendeleev Commun., 35:1 (2025), 50–53
A. N. Proshin, T. P. Trofimova, A. A. Globa, E. S. Dubrovskaya, O. N. Zefirova, N. A. Zefirov, V. A. Tafeenko, T. Ya. Dutova, B. I. Ugrak, I. V. Serkov, “New 1,1-dibenzyl-3-(1-benzyl-1H-pyrazol-4-yl)-2-methylisothioureas: synthesis and evaluation of antioxidant activity”, Russ Chem Bull, 73:5 (2024), 1399
N. A. Zefirov, E. V. Khvatov, E. V. Nurieva, Ya. L. Esaulkova, A. S. Volobueva, V. V. Zarubaev, A. S. Goryashchenko, D. O. Yatsenko, V. I. Uvarova, D. I. Osolodkin, A. A. Ishmukhametov, O. N. Zefirova, “Rimantadine derivatives with antiviral activity against flaviviruses and rimantadine-resistant strain of influenza A virus”, Russ Chem Bull, 73:6 (2024), 1801
E. V. Nurieva, O. Yu. Kravtsova, A. V. Sydoriuk, E. V. Britikova, V. V. Britikov, N. A. Zefirov, E. R. Milaeva, O. N. Zefirova, “The homodimer approach to the design of a new long-acting depot prodrug of abiraterone”, Mendeleev Commun., 34:4 (2024), 502–504
I. A. Elisseev, E. V. Nurieva, N. A. Zefirov, A. Yu. Kolchanova, D. A. Skvortsov, E. R. Milaeva, O. N. Zefirova, “New C(4)-esters of podophyllotoxin and epipodophyllotoxin with heterocyclic moieties”, Russ Chem Bull, 72:9 (2023), 2191
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