А series of the work "Directed synthesis of biologically important oxazaheterocycles and opened heteroatomic structures on the basis of epoxy compounds"

Work number - M 61 AWARDED

Author: Palchikov V.A.

Submitted by Oles Honchar Dnipropetrovsk National University of theMinistry of Education and Science of Ukraine

Series of scientific works contains10 separate chapters, published mainly in 1 monograph and 45 scientific articles published by the periodof10 years (2004-2013).

Aimofthework–development of methods forthe synthesis of building-blocks and targetcombinatorial libraries (amines, aminoalcohols,sulfon- and carboxamides, imides, cage-likelactones and lactams, aza-and oxabrendanesetc.) on the basisofavailable epoxy compounds for the needs of the combinatorial chemistry and high-throughputbioscreening technology.

Thescientific bases and methodology directed synthesis of new oxazaheterocyclesand openedheteroatomicderivativeswas developed based on epoxides and their primary aminolysis products (described more than 370 compounds),revealed regularities in the cleavageand closure ringsin reactions of these compounds with a wide range of nucleophilic and electrophilic reagents using modern spectroscopic and quantum chemical methods, evaluated the profile of biological activity of the synthesized compounds in a series of in vivo / in vitro studies,identified and patented 14lead-compounds.

Obtained anumber of fundamental results concerning the mechanism first proposed strategy of "domino aminolysisofdiepoxides" and stereochemistry of vinylicnucleophilic substitution in the bicyclic methyleneaziridines.

Proposed new substances that biological activity is at the level, and in some cases exceed the relevant comparators: analgesic Analgin, anti-inflammatory drug Diclofenac, plant growth regulators Ivin and Ethrel, anti-HIV drug Azidothymidine.

Series of scientific works contains priority results in the field of organic, medicinal and pharmaceutical chemistry.

The results of the researchare important for agriculture, since the application developed and patented new growth regulators can more fully realize the potential of plants, inherent by the nature and selection.

Based on materials of the researchauthor published 100 scientific papers, including 1 monograph (2012, 644 p.), 45 articles in professional journals, 21 of them published in international peer-reviewed journals with non-zero impact factor and included in the Scopus (they have 75 links in 41 articles, the Hirsch index of the author h = 5), 16 patents of Ukraine for inventions and utility models, 38 abstracts ofnational and international conferences, received 3 reports of implementation of research results into the learning process of the Oles Honchar DNU.

Total number of scientific publications of the author – 213 (1 monograph, 51 articles, 20 patents, 141 abstracts).