III International Conference

Chemistry and Biological Activity of Nitrogen-Containing Heterocycles
(in memory of Prof. A.N. Kost)

 

has been held at the Research Center in Chernogolovka, Moscow, Russia

June 20–23, 2006

 

This Conference concluded the series of international meetings on the Chemistry and Biological Activity of Synthetic and Natural Compounds dedicated to the 90th Anniversary of Honored Scientist of Russia
Prof. A.N. Kost, that started with a conference at Moscow State University in October, 2005.

 

 

The Conference was organized by InterBioScreen Ltd.
and International Charitable Foundation Scientific Partnership with the participation and support from
the Russian Academy of Sciences, Russian Mendeleev Chemical Society,
Lomonosov Moscow State University, and
Council on Science and Technology under the Moscow Government.

 

The Organizing Committee was headed by Prof. V.G. Kartsev, President of the Scientific Partnership Foundation; Chairman of Board of directors of InterBioScreen.

 

Honorary members of the International Editorial Board:

 

Prof. E.J. Corey (USA) – Nobel Prize in Chemistry, 1990

Prof. R. Noyori (Japan) – Nobel Prize in Chemistry, 2001

Prof. J.-M. Lehn (France) – Nobel Prize in Chemistry, 1987

Prof. Atta-ur-Rahman (Pakistan)

Prof. J. Bergman (Sweden)

Prof. J. Elguero (Spain)

Prof. R. Huisgen (Germany)

Prof. A.R. Katritzky (USA)

Prof. D. Spinelli (Italy)

Prof. H. van der Plas (Netherlands)

 

The scientific committee of the conference was composed of eminent Russian and CIS scientists in the field of chemistry and biological activity of synthetic and natural heterocycles:

 

 

 

 

Organizing Committee:

 

 

 

 

 

The Conference was attended by a wide circle of organic chemists active in the field of bioactive N-containing heterocyles who presented their recent achievements in the synthesis, characterization, and bioactivity of N-heterocycles.

 

Among the attendants were widely-known representatives of the international heterocyclic community Prof. H. van der Plas (University of Wageningen, the Netherlands), Prof. M. Mąkosza (Institute of Organic Chemistry, Poland), L. Fišera (Slovak University of Technology, Slovak Republic), Prof. M.N. Preobra­zhenskaya, Prof. N.S. Zefirov, and Prof. O.N. Chupakhin.

 

 

 

Prof. N.S. Zefirov, Prof. X. van der Plas, Prof. М. Mąkosza, Prof. O.N. Chupakhin

 

 

 

 

Prof. X. van der Plas, Prof. O.N. Chupakhin, Prof. М. Mąkosza

 

 

Contributions to the Conference were submitted by leading scientists of Austria, Belgium, Germany, Great Britain, Greece, Egypt, India, France, Jordan, Italy, the Netherlands, Sweden, Russia, the USA, and other countries. The conference was attended by over 250 participants from 30 countries, including 30 foreign delegates. The Russian participants represented 83 leading research institutions, and the foreign delegates, 45 research institutions and groups all over the world.

As a sponsor and organizer, InterBioScreen financially supported the participation of younger researchers and post-graduate students in the Conference.

 

 

Financial support also came from International Charitable Foundation Scientific Partnership, Council on Science and Technology under the Moscow Government, and other Russian and foreign sponsors:

 

 

 

The Opening Ceremony has begun with the introductory word by Prof. V.G. Kartsev. Prof. N.S. Zefirov read a greeting to the Conference from Prof. Jean-Marie Lehn, Nobel Laureate in chemistry; Prof. H. van der Plas, voiced the note of welcome from Prof. Elias Corey, Nobel Laureate; Prof. O.A. Kost, daughter of A.N. Kost, also warmly addressed the delegates.

 

Prof. H. van der Plas (University of Wageningen, The Netherlands)	Prof. О.А. Kost (Lomonosov Moscow State University, Moscow)

 

 

At the Conference, the first official ceremony of awarding with the Medal "In Memory of
Prof. A.N. Kost" for the year of 2006 took place.

 

 

The Medal "In Memory of Prof. A.N. Kost" was instituted in 2005 on the occasion of his 90th Anniversary by the International Charitable Foundation Scientific Partnership, Lomonosov Moscow State University and Russian Mendeleev Chemical Society. The Medal is awarded for outstanding achievements in the chemistry of synthetic and natural heterocyclic compounds as a sign of public recognition of the efforts of individual scientists and research groups.

 

The scientists awarded with the Medal in 2006:

 

 

 

 

 

 

 

 

The Research Centers and Groups awarded with the Medal in 2006:

 

The International Society of Heterocyclic Chemistry

Heterocycles, Japan

Department of Chemistry, Lomonosov Moscow State University, Moscow (the medal was received by Prof. N.V. Zyk, p.p. Dr. V.V. Lunin, Dean of the chemistry faculty)

Zelinskii Institute of Organic Chemistry, Moscow (the medal was received by Prof. M.P. Egorov, Director)

Journal "Chemistry of Heterocyclic Compounds", Latvia (the medal was received by A.E. Skorova,
Executive Secretary)

 

  

Medal "Badge of Honor" was awarded to the

 

Prof. A. Shelar

Institute of Pharmaceutical Education and Research, India

 

 

The International Charitable Foundation Scientific Partnership has started a new program intended to support Russian scientific libraries and extend scientific partnership by presenting the books published (in Russian and English) by the Foundation.

 

The books were donated to the following institutions and research centers:

 

Université de Rennes 1, Institut de Chimie, France (books are handed to Bazureau J.P.)

Chemical Research Center, Budapest, Hungary (books are handed to Bölcskei H.)

University of São Paulo State, Brazil (books are handed to Chung M.C.)

Università di Ferrara, Italy (books are handed to Dondoni A.)

Latvian Institute of Organic Synthesis, Riga (books are handed to Duburs G., Veinberg G.)

Slovak University of Technology, Slovak Republic (books are handed to Fišera L.)

Aristotelian University of Thessaloniki, Greece (books are handed to Geronikaki A.)

Universität Siegen, Germany (books are handed to Granzhan A.)

Chemical Research Center, Budapest, Hungary (books are handed to Hajós Gy.)

Vienna University of Technology, Austria (books are handed to Jordis U.)

Technische Universität Dresden, Germany (books are handed to Knölker H.-J.)

Institute of Organic Chemistry, PАS, Warszawa, Poland (books are handed to Mąkosza M.)

Gedeon Richter Ltd., Hungary (books are handed to Nemes A.)

Research Institute of Pharmacy and Biochemistry, Czech Republic (books are handed to Rádl S.)

Central Drug Research Institute, India (books are handed to Saxena A.K.)

Shivaji University Kolhapur, India (books are handed to Shelar A.)

University of Leuven, Belgium (books are handed to van der Eycken E.)

University of Wageningen, The Netherlands (books are handed to van der Plas H.)

Department of Chemistry, Lomonosov Moscow State University, Moscow (books are handed to
Prof. Zyk N.V., p.p. Dr. V.V. Lunin, Dean of the chemistry faculty)

Zelinskii Institute of Organic Chemistry, Moscow (books are handed to Prof. Egorov M.P., Director)

Journal "Chemistry of Heterocyclic Compounds", Latvia (books are handed to Prof. Skorova A.E., Ececutive Secretary)

 

The books are handed to Rrof. H.-J. Knölker for Technische Universität Dresden, Germany	The books are handed to Rrof. H. Bölcskei for Chemical Research Center, Budapest, Hungary
The books are handed to Rrof. S. Rádl for Research Institute of Pharmacy and Biochemistry, Czech Republic	The books are handed to Rrof. M.C. Chung for University of São Paulo State, Brazil

 

 

The Scientific Program was opened with the keynote lectures delivered by the leading experts in the organic chemistry and chemistry of natural compounds:

Mąkosza M. (Польша)
Synthesis of indoles via nucleophilic substitution of hydrogen in nitroarenes

Van der Plas H.C. (Нидерланды)

The ring transformation as methodology for the synthesis of azaheterocycles

 

The lecture is presented by Prof. M. Mąkosza (Institute of Organic Chemistry, Poland)	The lecture is presented by Prof. Х. van der Plas (University of Wageningen, The Netherlands)

 

Oral and poster presentations reflected recent achievements in the synthesis, chemical transformations, and bioactivity of various nitrogeneous heterocycles.

 

The scale and a high level of the Conference were ensured by the excellent quality of plenary lectures delivered by leading experts in the field.

 

 

The lectures of the plenary session were delivered by:

 

Dondoni A., Massi A. (Italy)

Multicomponent synthetic approach to reengineered N-heterocycle pharmacophores by glycoside decoration

Fišera L. (Slovak Republic)

Control of regio- and stereoselectivity in nitrone cycloadditions and their utilization in synthesis

Hajós Gy. (Hungary)

Zwitter-ionic heterocycles: A pool of novel polyfused ring systems

Jordis U. (Austria)

How to use software and integrate databases in the daily practice of heterocyclic chemist

Saxena А. (India)

Substituted arylpiperazines in rational drug design

Granik V.G. (Russia)

Biotransformations of heterocyclic nitrogen-containing drugs

Kartsev V.G. (Russia)

New horizons for use of T-reactions in the synthesis of heterocycles

Kostyanovsky R.G. (Russia)

Nitrogen chirality in heterocyclic chemistry

Akhrem A.A., Gulyakevich O.V., Mikhal'chuk A.L. (Belarus)

[2+4]-Cyclocondensation of monocyclic azomethines with b-di- and
b,b'-tricarbonyl compounds in synthesis of azangular heterocycles

Poroikov V.V., Filimonov D.A., Gloriozova T.A., Lagunin A.A. (Russia)

Computer-aided prediction of biological activity for nitrogen-containing organic compounds

Preobrazhenskaya M.N. (Russia)

Chemistry and biology of ascorbigen

Chupakhin O.N., Rusinov V.L., Charushin V.N. (Russia)

Abnormal nucleosides from isosteres of purine

Sagitullina G.P., Sagitullin R.S. (Russia)

Recyclization of pyridinium salts: New horizons

Saloutin V.I., Burgart Ya.V., Chupakhin O.N. (Russia)

Design of azaheterocycles based on fluorine-containing 2,4-dioxobutanoates and their derivatives

Shestopalov A.M., Rodinovskaya L.A., Shestopalov A.A. (Russia)

Recyclization reactions of degenerate carbo- and heterocycles: Practical retrosynthetic approach to new multicomponent methods for synthesis of N-containing five- and six-membered heterocycles

Vasilevsky S.F., Balova I.A. (Russia)

New one-pot synthesis and heterocyclization of vic-functionalized aryl(hetaryl)alkadiynes-1,3

Zefirov N.S. (Russia)

Organic chemistry and mathematics: Design and modeling

Zefirov N. (Russia)

The use of QSAR in the search of biologically active compounds

 

 

Oral presentations were made by 51 scientists from Russia and abroad:

 

An oral lecture is delivered by Dr. R.B. Lesyk (Danylo Halytsky National Medical University, L'vov)	An oral lecture is delivered by Prof. A.V. Velikorodov (Astrakhan' State University, Astrakhan')	An oral lecture is delivered by Prof. А.А. Gidaspov (State Technical University, Samara)

 

Bazureau J.P., Legeay J.C., Fraga-Dubreuil J., Hakkou H. (France)

Ionic liquid-phase technology: A new tool for combinatorial chemistry. Applications in heterocyclic chemistry mediated by microwave dielectric heating

Belous A.R. (USA)

Endogenous indole compounds: biological significance of 5-hydroxytriptamine and its metabolites

Bölcskei H., Gács-Baitz E., Szántay Cs. Jr., Kalaus Gy., Szántay Cs. (Hungary)

Synthesis of indoloazepines and indoloazocines

Chung M.C. (Brazil)

Prodrug design: Improving drug activity

Duburs G., Bisenieks E., Krauze A., Plotniece A., Sobolevs A., Tirzitis G., Vigante B. (Latvia)

Dihydropyridine derivatives as biomimetics and bioprotectors

Geronikaki A., Incerti M., Zani F., Vicini P. (Greece)

2-Benzo[d]isothiazolylimino-5-arylidene-4-thiazolidinones: Synthesis and antimicrobial activity

Granzhan A., Ihmels H., Viola G. (Germany)

Rearrangements in diazoniapentaphenes and DNA-binding properties of diazoniapolycycles

Agarwal S., Filali S., Fröhner W., Knöll J., Krahl M.P., Reddy K.R., Knölker H.-J. (Germany)

Application of oxidative cyclizations to the synthesis of bioactive nitrogen-containing heterocycles

Nemes A. (Hungary)

Synthetic studies related to cis- and trans-apovincamine derivatives and metabolites

Rádl S., Klecán O. (Czech Republic)

New approaches to the synthesis of triptans

Mali A., Shelar M., Shelar A. (India)

Antibiotic resistance: A search for new b-lactam antibiotics

Van der Eycken E. (Belgium)

Microwave irradiation: A 'green tool' in 2(1H)-pyrazinone chemistry

Veinberg G., Vorona M., Shestakova I., Kanepe I., Lukevics E. (Latvia)

Antitumor 3a-chloro- and 3-alkylideneazetidinone-2 derivatives

Adekenov S.М. (Kazakhstan)

Nitrogen-containing derivatives of natural sesquiterpene lactones

Akhmetova V.R., Nadyrgulova G.R., Khairullina R.R., Khafizova S.R., Kunakova R.V., Dzhemilev U.M. (Russia)

One-pot synthesis of novel N,S-containing heterocycles

Berestovitskaya V.M., Anisimova N.A., Makarova N.G. (Russia)

Synthesis of nitrogen-containing heterocycles from b-nitroethenylphosphonates and -carboxylates

Burgart Ya.V., Pryadeina M.V., Khudina O.G., Saloutin V.I., Chupakhin O.N. (Russia)

Synthesis of fluoroalkyl-containing pyrimidines

Drach B.S., Sviripa V.N., Pil'o S.G., Popil'nichenko S.V., Golovchenko A.V., Brovarets V.S. (Ukraine)

Synthesis of functionalized condensed heterocycles from 2-acylamino-3,3-dichloroacrylonitriles

Eremkin A.V., Mol'kov S.N., Ershov O.V. (Russia)

Hydrolysis of cyano groups in 2-halo-6-hydroxy-5,5-dialkyl-5,6-dihydropyridine-3,4,4(1H)-tricarbonitriles

Ershov A.Yu., Lagoda I.V., Koshmina N.V., Dobrodumov A.V. (Russia)

Recyclization of isoxazole derivatives

Gidaspov A.A. (Russia)

bis-Trinitromethylation of 2,4,6-trichloro-1,3,5-triazine

Gornostaev L.M., Arnold E.V., Beresnev V.A., Dolgushina L.V., Lavrikova T.I., Sokolova M.S. (Russia)

Anthraquinone derivatives condensed with pyrrole and triazole rings: Synthesis and properties

Gorobets N.Yu., Ermolaev C.A., Dzhavakhishvili S.G., Sirko S.N., Chernenko V.N., Desenko S.M. (Ukraine)

2-Dimethylaminomethylene-1,3-cyclohexanedione derivatives in reaction with methylene-active nitriles

Isak A.D., Pogorelova I.P., Tyupalo N.F., Isak V.A. (Ukraine)

Pyrimidine sulfone amides and their derivatives: Synthesis and biological activity

Kalinin V.N., Shishkov I.V., Moiseev S.K., Shults E.E., Tolstikov G.A. (Russia)

Synthesis of new dienes and trienes of the morphinan series

Kofanov E.R., Sosnina V.V. (Russia)

Multifunctional heterocyclic compounds from nitriles of aromatic carboxylic acids

Korotkikh N.I., Raenko G.F., Kiselev А.V., Knishevitsky А.V., Shvaika О.P., Glinyanaya N.V., Panov I.S., Cowley А.H., Jones J.N., Moore J.A. (Ukraine)

Stable carbenes. Insertion into С–Н bonds and reaction with ester function. New cleavage and thermal transformation of 1,2,4-triazol-5-ylidenes

Kravchenko A.N., Sigachev A.S., Chikunov I.E., Lozhkin B.V., Baranov V.V., Gazieva G.A., Trunova N.S., Lysenko K.A., Belyakov P.A., Makhova N.N. (Russia)

New horizons in a-ureidoalkylation

Lesyk R.B., Zimenkovsky B.S., Atamanyuk D.V. (Ukraine)

Thiopyrano[2,3-d]thiazoles and their derivatives: Synthesis and biological activity

Levinson F.S., Ermolaeva E.A., Efimov S.I., Evgen'ev M.I., Varganov R.V., Vasyutina E.A., Shakirova I.M. (Russia)

4,6-Dichloro-5,7-dinitro- and 4-methoxy-6-chloro-5,7-dinitrobenzofurazans as new two-position electrophiles

Levkovskaya G.G., Bozhenkov G.V., Savosik V.A., Mirskova A.N. (Russia)

Derivatives of 4- and 5-halopyrazoles: Targeted synthesis, structure, and properties

Makarenko S.V., Berestovitskaya V.M., Sadikov K.D., Tafeenko V.A., Chernyshev I.V. (Russia)

Potentially bioactive 1,4-benzodiazinones and their heteroanalogs: Synthesis and structure

Makhova N.N., Shevtsov A.V., Petukhova V.Yu., Kuznetsov V.V., Kislukhin A.A. (Russia)

Transformation of diaziridine ring under the action of ketenes as a new synthetic approach to nitrogen-containing heterocyclic systems

Mareev A.V., Pavlov D.V., Khatashkeev A.V., Medvedeva A.S., Afonin A.V., Ushakov I.A. (Russia)

Cascade assembling of polyfunctional 1,2-dihydropyridine and related compounds from 3-trimethylsilyl-
2-propynal and 2-aminopyridine under microwave activation

Medvedeva A.S., Demina M.M., Novokshonov V.V., Safronova L.P., Rulev A.Yu., Pavlov D.V., Mareev A.V., Afonin A.V. (Russia)

Synthesis of azidomethyl-1Н-1,2,3-triazoles

Polygalova N.N., Mikhailovskii A.G., Vakhrin M.I. (Russia)

Carbonyl derivatives of condensed isoquinolines: Synthesis and reactivity

Mikhalev O.V., Tarasevich B.N., Fedyanin I.V., Il'ina I.G. (Russia)

Autocomplexes of nitroaryls with heterocycles: Synthesis and characterization

Gulyakevich O.V., Mikhal'chuk A.L. (Belarus)

Construction of azinone framework by [3+3]-cyclocondensation of b-enaminones with b-ketoesters

Nekrasov D.D., Obukhova A.S. (Russia)

2-Amino-substituted 6-aryl-1,3-oxazin-4-ones: Synthesis and biological activity

Ol'shevskaya V.A., Zaitsev A.V., Savchenko A.N., Luzgina V.N., Shtil' A.A., Kalinin V.N. (Russia)

Carboranylporphyrins: Synthesis and bioactivity

Plaskon' A.S., Ryabukhin S.V., Volochnyuk D.M., Tolmachev A.A. (Ukraine)

3-Formylchromones in recyclization with 1,3-CCN- and 1,3-ССС-binucleophiles

Popkov S.V., Kovalenko L.V. (Russia)

1-Azolylmethyl-6-benzylidene-2-alkoxy-2-methyl- and 2,2-dimethylcyclohexanols: Synthesis and bioactivity

Przheval'skii N.M. (Russia)

Heterohexadiens in synthesis of heterocycles

Semenov V.E., Nikolaev A.E., Giniyatullin R.Kh., Lodochnikova O.A., Voloshina A.D., Galiullina L.F.,
Latypov Sh.K., Reznik V.S. (Russia)

Pyrimidinophanes with nitrogen atoms in bridging groups: Synthesis and properties

Zobov V.V., Semenov V.E., Kataev V.E., Akamsin V.D., Reznik V.S. (Russia)

Tetraalkylammonium derivatives of uracil and their macrocyclic analogs as potential neuromuscular transmission modulators

Shestakov A.S., Gusakova N.V., Shikhaliev Kh.S. (Russia)

Cyanamides and their derivatives in reactions of heterocyclyzation

Shikhaliev Kh.S., Kryl'skii D.V., Falaleev A.V., Kovygin Yu.A., Potapov A.Yu. (Russia)

Construction of heterocyclic systems from guanidines and carbonyls

Shklyaev Yu.V., Glushkov V.A., Stryapunina O.G., Rozhkova Yu.S., El'tsov M.A. (Russia)

The synthesis of partially hydrohenization azine and azole: Dihydroisoquinolines, spiropyrrolines, polyhydroindolines

Stroganova T.A., Vasilin V.K., Krapivin G.D. (Russia)

Amino acids of the thieno[2,3-b]pyridine series in reactions of intramolecular cyclization

Velikorodov А.V. (Russia)

Quinones and quinoids in synthesis and modification of indoles

Volochnyuk D.M., Pushechnikov A.O., Pinchuk A.M., Tolmachev A.A. (Ukraine)

Fused 1,5,2-diaza- and 1,5,2-oxazaphosphinines: Synthesis and properties

Voskressensky L.G., Vorob'ev I.V., Varlamov A.V. (Russia)

Unusual reactions of tetrahydrobenzo[b][1,6]naphthyridines with activated alkynes

 

 

The poster session presented over 150 contributions.

 

 

A high quality edition of the 2-volume proceedings of the Conference entitled as Nitrogen-Containing Heterocycles in Russian and English continues our series of monographs Chemistry and Biological Activity of Synthetic and Natural Compounds. Volume 1 is a collection of the plenary and oral lectures reviewing recent achievements in the field. Volume 2 contains the abstracts of 223 poster presentations and 94 most interesting (nominal) synthetic protocols for the synthesis and modification of complex heterocyclic compounds worked out in the last few years by chemists from Russia, Ukraine, Belarus, and other countries, mostly inspired and supported by InterBioScreen.

 

 

Editorial Board of the Proceedings

 

Editor-in-chief  Kartsev V.G.

 

International Editorial Board

 

 

 

 

 

 

 

Editorial Board

 

 

 

Regional Editors

 

 

Executive secretary Semenova L.F.

 

 

 

 

To the attention of the Conference attendants were offered two-volume Proceedings of three Conferences in the series: Nitrogen-Containing Heterocyles and Alkaloids (СВС2001), Oxygen- and Sulfur-Containing Heterocycles (СВС2003), Nitrogen-Containing Heterocycles (СВС2006), as well as four volumes (both in Russian and English) of the monograph series Selected Methods for Synthesis and Modification of Heterocycles (vol. 1: Nitrogen-Containing Heterocyles, vol. 2: Oxygen- and Sulfur-Containing Heterocyles, vol. 3: Chemistry of Synthetic Indole Systems, vol. 4: Chemistry and Biological Activity of Natural Indole Systems). Electronic versions of some books were offered on CDs, including in the ISIS_Base 2.X format.

 

 

The next Conference will be devoted to heterocycles in medicinal chemistry
and is to be held in St. Petersburg in 2010.