Synthesis and structure—activity relationships of cyclopropane-containing analogs of pharmacologically active compounds
- Authors: Novakov I.A.1, Babushkin A.S.1, Yablokov A.S.1, Nawrozkij M.B.1, Vostrikova O.V.1, Shejkin D.S.1, Mkrtchyan A.S.1, Balakin K.V.2,3
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Affiliations:
- Volgograd State Technical University
- Kazan Federal University, Education and Research Center of Pharmacy
- I. M. Sechenov First Moscow State Medical University of the Ministry of Healthcare of the Russian Federation (Sechenov University)
- Issue: Vol 67, No 3 (2018)
- Pages: 395-418
- Section: Reviews
- URL: https://journals.rcsi.science/1066-5285/article/view/242275
- DOI: https://doi.org/10.1007/s11172-018-2087-6
- ID: 242275
Cite item
Abstract
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.
About the authors
I. A. Novakov
Volgograd State Technical University
Email: maxim.nawrozkij@gmail.com
Russian Federation, 28 prosp. im. Lenina, Volgograd, 400131
A. S. Babushkin
Volgograd State Technical University
Email: maxim.nawrozkij@gmail.com
Russian Federation, 28 prosp. im. Lenina, Volgograd, 400131
A. S. Yablokov
Volgograd State Technical University
Email: maxim.nawrozkij@gmail.com
Russian Federation, 28 prosp. im. Lenina, Volgograd, 400131
M. B. Nawrozkij
Volgograd State Technical University
Author for correspondence.
Email: maxim.nawrozkij@gmail.com
Russian Federation, 28 prosp. im. Lenina, Volgograd, 400131
O. V. Vostrikova
Volgograd State Technical University
Email: maxim.nawrozkij@gmail.com
Russian Federation, 28 prosp. im. Lenina, Volgograd, 400131
D. S. Shejkin
Volgograd State Technical University
Email: maxim.nawrozkij@gmail.com
Russian Federation, 28 prosp. im. Lenina, Volgograd, 400131
A. S. Mkrtchyan
Volgograd State Technical University
Email: maxim.nawrozkij@gmail.com
Russian Federation, 28 prosp. im. Lenina, Volgograd, 400131
K. V. Balakin
Kazan Federal University, Education and Research Center of Pharmacy; I. M. Sechenov First Moscow State Medical University of the Ministry of Healthcare of the Russian Federation (Sechenov University)
Email: maxim.nawrozkij@gmail.com
Russian Federation, 18 ul. Kremlevskaya, Kazan, 420008; Build. 2, 8 ul. Trubetskaya, Moscow, 119991