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Synthesis and structure—activity relationships of cyclopropane-containing analogs of pharmacologically active compounds

Novakov I. A., Babushkin A. S., Yablokov A. S., Nawrozkij M. B., Vostrikova O. V., Shejkin D. S., Mkrtchyan A. S., Balakin K. V.
Russian Chemical Bulletin
Vol.67, Issue3, P. 395-418
Опубликовано: 2018
Тип ресурса: Обзор

DOI:10.1007/s11172-018-2087-6

Аннотация:
The review summarizes information on cyclopropane as an independent pharmacophore group and as a fragment for modification of pharmacological activity level of medicines used in practice. The advantages of a cyclopropane fragment over its bioisosteres are that, on the one hand, this fragment imposes conformational rigidity on the molecules of physiologically active compounds and, on the other hand, the replacement of acyclic terminal and “linker” groups with a cyclopropane fragment increases the metabolic stability of the target structures and extends the scope of their therapeutic action. © 2018, Springer Science+Business Media, LLC, part of Springer Nature.
Ключевые слова:
cycloaddition; cyclopropanes; heterocyclization; pyrimidines
Язык текста: Английский
ISSN: 1573-9171
Novakov I. A.
Babushkin A. S.
Yablokov A. S.
Nawrozkij M. B.
Vostrikova O. V.
Shejkin D. S.
Mkrtchyan A. S.
Balakin K. V. Konstantin Valeryevich 1970-
Новаков И. А.
Бабушкин А. С.
Яблоков А. С.
Наwрозкij М. Б.
Вострикова О. В.
Шейкин Д. С.
Мкртчян А. С.
Балакин К. В. Константин Валерьевич 1970-
Synthesis and structure—activity relationships of cyclopropane-containing analogs of pharmacologically active compounds
Текст визуальный непосредственный
Russian Chemical Bulletin
Springer-Verlag GmbH
Vol.67, Issue3 P. 395-418
2018
Обзор
cycloaddition cyclopropanes heterocyclization pyrimidines
The review summarizes information on cyclopropane as an independent pharmacophore group and as a fragment for modification of pharmacological activity level of medicines used in practice. The advantages of a cyclopropane fragment over its bioisosteres are that, on the one hand, this fragment imposes conformational rigidity on the molecules of physiologically active compounds and, on the other hand, the replacement of acyclic terminal and “linker” groups with a cyclopropane fragment increases the metabolic stability of the target structures and extends the scope of their therapeutic action. © 2018, Springer Science+Business Media, LLC, part of Springer Nature.