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

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...

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Bibliographic Details
Published inRussian chemical bulletin Vol. 67; no. 3; pp. 395 - 418
Main Authors Novakov, I. A., Babushkin, A. S., Yablokov, A. S., Nawrozkij, M. B., Vostrikova, O. V., Shejkin, D. S., Mkrtchyan, A. S., Balakin, K. V.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.03.2018
Springer Nature B.V
Subjects
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
Cyclopropane
Fragmentation
Inorganic Chemistry
Molecular chains
Organic Chemistry
Pharmacology
Reviews
Structural stability
cyclopropanes
heterocyclization
cycloaddition
pyrimidines
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Summary: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.
ISSN:1066-5285
1573-9171
DOI:10.1007/s11172-018-2087-6