Conformational studies of novel antiretroviral analogs of zidovudine

Conformational properties of three novel zidovudine analogs, namely 3′-azido-3′-deoxy-5′-O-isonicotinoylthymidine (AZT-Iso, 2), (-)-trans-(5S,6S)-5-bromo-6, 5′-epoxy-5,6-dihydro-3′-azido-3′-deoxythymidine (3) and (+)-trans-(5R,6R)-5-bromo-6,5′-epoxy-5,6-dihydro-3′- azido-3′-deoxythymidine (4), have...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autor principal: Baumgartner, M.T
Otros Autores: Motura, M.I, Contreras, Rubén Horacio, Pierini, A.B, Briñón, M.C
Formato: Capítulo de libro
Lenguaje:Inglés
Publicado: 2003
Acceso en línea:Registro en Scopus
DOI
Handle
Registro en la Biblioteca Digital
Aporte de:Registro referencial: Solicitar el recurso aquí
LEADER 13669caa a22012017a 4500
001 PAPER-5003
003 AR-BaUEN
005 20250204092301.0
008 190411s2003 xx ||||fo|||| 00| 0 eng|d
024 7 |2 scopus  |a 2-s2.0-0037238689 
024 7 |2 cas  |a zidovudine, 30516-87-1; 3'-azido-3'-deoxy-5'-O-isonicotinoylthymidine; Anti-Retroviral Agents; trans-(5S,6S)-5-bromo-6, 5'-epoxy-5,6-dihydro-3'-azido-3'-deoxythymidine; Zidovudine, 30516-87-1 
030 |a NNNAF 
040 |a Scopus  |b spa  |c AR-BaUEN  |d AR-BaUEN 
100 1 |a Baumgartner, M.T. 
245 1 0 |a Conformational studies of novel antiretroviral analogs of zidovudine 
260 |c 2003 
270 1 0 |m Briñón, M.C.; Departamento de Farmacia, Ciudad Universitaria, Universidad Nacional de Cordoba, 5000 Córdoba, Argentina; email: macribri@dqo.fcq.unc.edu.ar 
504 |a Mitsuya, H., Weinhold, K.J., Furman, P.A., St. Clair, M.H., Lehrman, S.N., Gallo, R.C., Bolognesi, D., Broder, S., 3′-azido-3′-deoxythymidine (BW A509U): An antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/Lymphadenopathy-associated virus in vitro (1985) Proc. Natl. Acad. Sci. U.S.A., 82, pp. 7096-7100 
504 |a Fischl, M.A., Richman, D.D., Grieco, M.H., Gottlieb, M.S., Volberding, P.A., Laskin, O.L., Leedom, J.M., King, D., The efficacy of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A bouble-blind, placebo-controlled trial (1987) N. Engl. J. Med., 317, pp. 185-191 
504 |a De Clercq, E., Reverse transcriptase inhibitors as anti-HIV drugs (2000) Antiviral Against AIDS, pp. 107-150. , Unger, R.E., Kreuter, J., Rübsamen-Waigmann, H., Eds.; Marcel Dekker, Inc.: New York 
504 |a Sabio, M., Topiol, S., A conformational analysis of 3′-azido-3′-deoxythymidine (1992) J. Comp. Chem., 13 (4), pp. 478-491 
504 |a Saran, A., Ojha, R.P., Conformation of azidothymidine: An anti-AIDS drug (1991) J. Biosci., 16 (1), pp. 29-42 
504 |a Da Motta Neto, J.D., Zerner, M.C., Bicca de Alencastro, R., A possible mechanism of molecular recognition for the reverse transcriptase of HIV-1 (1992) Internat. J. Quantum Chem. Quantum Biology Symposium, 19, pp. 225-253 
504 |a Estévez, C.M., Graña, A.M., Rios, M.A., A semiempirical AMl conformational study of 3′-substituted deoxythymidines (1993) J. Mol. Structure (Theochem.), 288, pp. 207-214 
504 |a Birnbaum, G.I., Giziewicz, J., Gabe, E.J., Lin, T., Prusoff, W.H., Structure and conformation of 3′-azido-3′-thymidine (AZT), as inhibitor of the HIV (AIDS) virus (1987) Can. J. Chem., 65, pp. 2135-2139 
504 |a Maag, H., Nelson, J.T., Rios Steiner, J.L., Prisbe, E.J., Solid-state and solution conformations of the potent HIV inhibitor, 4′-azidothymidine (1994) J. Med. Chem., 37 (4), pp. 431-438 
504 |a Wood, D.J., Hruska, F.E., Ogilvie, K.K., Proton magnetic resonance studies of 2′-deoxythymidine, its 3′- and 5′-monophosphates and 2′-deoxythymidylyl-(3′,5′)-2′-deoxythymidine in aqueous solutions (1974) Can. J. Chem., 52, pp. 3353-3366 
504 |a Raap, J., Van Boom, J.H., Van Lieshout, H.C., Haasnoot, C.A.G., Conformations of methyl 2′-deoxy-α-D-ribofuranoside and methyl 2′-deoxy-β-D-ribofuranoside. A proton magnetic resonance spectroscopy and molecular mechanics study (1988) J. Am. Chem. Soc., 110, pp. 2736-2743 
504 |a Plavec, J., Koole, L.H., Sandström, A., Chattopadhyaya, J., Structural studies of Anti-HIV 3′-α-fluorothymidine and 3′-α-azidothymidine by 500 MHz 1H-NMR spectroscopy & molecular mechanics (MM2) Calculations (1991) Tetrahedron, 47 (35), pp. 7363-7376 
504 |a Altona, C., Sundaralingam, M., Conformational analysis of the sugar ring in nucleosides and nucleotides. A new description using the concept of pseudorotation (1972) J. Am. Chem. Soc., 94 (23), pp. 8205-8212 
504 |a Altona, C., Sundaralingam, M., Conformational analysis of the sugar ring in nucleosides and nucleotides. Improved method for the interpretation of proton magnetic resonance coupling constants (1973) J. Am. Chem. Soc., 95 (7), pp. 2333-2344 
504 |a Guschlbauer, W., Conformational analysis of ribonucleosides from proton-proton coupling constants (1980) Biochim. Biophys. Acta, 610, pp. 47-55 
504 |a Motura, M.I., Salomón, H., Moroni, G.N., Wainberg, M., Briñón, M.C., Synthesis, lipophilicity and anti-HIV activity of a new brominated analog of zidovudine (1999) Nucleos. Nucleot., 18 (3), pp. 337-351 
504 |a Teijeiro, S.A., Moroni, G.N., Motura, M.I., Briñón, M.C., Lipophilic character of pyrimidinic nucleoside derivatives. Correlation between shake flask, chromatographic (RP-TLC and RP-HPLC) and theoretical methods (2000) J. Liq. Chrom. & Rel. Technol., 23 (6), pp. 855-872 
504 |a Motura, M.I., Moroni, G.N., Teijeiro, S.A., Salomón, H., Briñón, M.C., 3′-Azido-3′-deoxy-5′-O-isonicotinoylthymidine, a new prodrug of zidovudine., synthesis, solid state characterization and anti HIV-1 activity (2002) Nucleos. Nucleot. & Nucleic Acids, 21 (3), pp. 231-241 
504 |a Bothner-By, A.A., Castellano, S.M., (1968) Computer Programs for Chemistry, 1, pp. 68-19706. , DeTar D.F. Ed.; W.A. Benjamin Inc.: New York, Library of Congress Catalog number 
504 |a De Leeuw, F.A.A.M., Altona, C., Computer-assisted pseudorotation analysis of five-membered rings by means of proton spin-spin coupling constants: Program PSEUROT (1983) J. Comp. Chem., 4 (3), pp. 428-437 
504 |a Dyer, I., Low, J.N., Tollin, P., Wilson, H.R., Alan Howie, R., Structure of 3′-azido-3′-deoxythymidine, AZT (1988) Acta Cryst., C44, pp. 767-769 
504 |a (1998) Hyperchem 5.0, , Hyper cube, Inc 
504 |a Liotard, D.A., Healy, E.F., Ruiz, J.H., Dewar, M.J.S., AMPAC version 2.10. Quantum chemistry program exchange, Program 506 (1989) QCPE Bull., 9, p. 123 
504 |a (1996) PCMODEL for Windows 6.0. Serena Software 
504 |a Buchanan, G.W., Bourque, K., 13C NMR spectra of antiviral nucleosides 3′-azido-3′-deoxythymidine, 2′,3′-dideoxyadenosine, 2′,3′-dideoxycytidine and 2′,3′-dideoxyinosine (1989) Magn. Reson. Chem., 27, pp. 200-201 
504 |a Swapna, G.V.T., Jagannadh, B., Gurjar, M.K., Kunwar, A.C., NMR Investigation on the structure and conformation of 3′-azido-2′,3′-dideoxyribosylthymine (AZT), an inhibitor of the HIV (AIDS Virus) (1989) Biochem. Biophys. Res. Commun., 164 (3), pp. 1086-1092 
504 |a Cadet, J., Ducolomb, R., Hruska, F.E., Proton magnetic resonance studies of 5,6-saturated thymidine derivatives produced by ionizing radiation. Conformational analysis of 6-hydroxylated diastereoisomers (1979) Biochim. Biophys. Acta, 563, pp. 206-215 
504 |a Teoule, R., Fouque, B., Cadet, J., Synthesis and spectroscopic properties of two classes of 5,6-dihydrothymidine derivatives. Action on the Ehrlich's Ascites cells thymidine kinase (1975) Nucleic Acids Res., 2 (4), pp. 487-499 
504 |a Kumar, R., Wang, L., Wiebe, L.I., Knaus, E.E., Synthesis, antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy (or azido)-5,6-dihydro-3′-fluoro-3′-deoxythymidine diastereomers. Potential prodrugs to 3′-fluoro-3′-deoxythymidine (1994) J. Med. Chem., 37, pp. 3554-3560 
504 |a (1997) Advanced Chemistry Development Inc. Version 2.51 
504 |a Kumar, R., Wang, L., Wiebe, L.I., Knaus, E.E., Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3′-azido-3′-deoxythymidine diastereomers as potential prodrugs to 3′-azido-3′-deoxythymidine (AZT) (1994) J. Med. Chem., 37, pp. 4297-4306 
504 |a Haasnoot, C.A.G., De Leeuw, F.A.A.M., Altona, C., The relationship between proton-proton NMR coupling constants and substituent electronegativities. I. An empirical generalization of the Karplus equations (1980) Tetrahedron, 36, pp. 2783-2792 
504 |a Altona, C., (1996) Encyclopedia of Nuclear Magnetic Resonance, p. 4909. , Editors-in-Chief Grant, D.M., Harris, R.K., Wiley: Chichester 
504 |a Olson, W.K., Sussman, J.L., How flexible is the furanose ring? 1. A comparison of experimental and theoretical studies (1982) J. Am. Chem. Soc., 104, pp. 270-278 
504 |a Olson, W.K., How flexible is the furanose ring? 2. An updated potential energy estimate (1982) J. Am. Chem. Soc., 104, pp. 278-286 
504 |a De Leeuw, F.A.A.M., Altona, C., Conformational analysis of β-D-Ribo-, β-D-Deoxyribo, β-D-arabino-, β-D-xylo-, and β-D-lyxo-nucleosides from proton-proton coupling constants (1982) J. Chem. Soc. Perkin II, pp. 375-384 
504 |a note 
506 |2 openaire  |e Política editorial 
520 3 |a Conformational properties of three novel zidovudine analogs, namely 3′-azido-3′-deoxy-5′-O-isonicotinoylthymidine (AZT-Iso, 2), (-)-trans-(5S,6S)-5-bromo-6, 5′-epoxy-5,6-dihydro-3′-azido-3′-deoxythymidine (3) and (+)-trans-(5R,6R)-5-bromo-6,5′-epoxy-5,6-dihydro-3′- azido-3′-deoxythymidine (4), have been investigated by AM1 calculations and NMR studies, and compared with those of the parent nucleoside (AZT, 1). Based on the results obtained the following correlation may be established, a) AZT and AZT-Iso exhibit a conformational behavior analog to other pyrimidinic nucleosides, displaying a dynamic equilibrium in solution where the two conformers (North and South) undergo a constant transformation. b) Compounds 3 and 4 show a different conformational profile. The estimate of the pseudorotation phase angle reveals the rigid structures of the latter compounds, which do not evidence conformational equilibrium in solution; the azide group being the only group free to rotate. c) Diastereoisomers 3 and 4 exhibit an extra conformational parameter compared with other pyrimidinic nucleosides: the chair or boat conformation in the third ring formed between the sugar and the base. In all cases, a reasonable correlation was obtained between theoretical and NMR spectroscopic data.  |l eng 
536 |a Detalles de la financiación: Agencia Córdoba Ciencia 
536 |a Detalles de la financiación: Secretaria de Ciencia y Tecnología - Universidad Nacional de Córdoba 
536 |a Detalles de la financiación: Fundación Antorchas 
536 |a Detalles de la financiación: Agencia Nacional de Promoción Científica y Tecnológica 
536 |a Detalles de la financiación: Consejo Nacional de Investigaciones Científicas y Técnicas 
536 |a Detalles de la financiación: Fondo para la Investigación Científica y Tecnológica 
536 |a Detalles de la financiación: The authors thank the Agencia Córdoba Ciencia, the Agencia Nacional de Pro-moción Científica y Tecnológica (FONCyT), the Secretaria de Ciencia y Técnica de la Universidad Nacional de Córdoba (SECyT-UNC), the Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Argentina, and Fundación Antorchas for financial support. The authors also wish to express their sincere thanks to Dra. L. Alassia (FILAXIS Laboratories, Buenos Aires, Argentina) for supplying zidovudine, Dr. C. Altona (State University Leiden, Gorlaeus Laboratories, The Netherlands) for PSEUROT calculations, and Dr. V. J. Kowalesky for recording NMR spectra in a 500 MHz apparatus (LANAIS RMN500). 
593 |a Depto. de Quimica Organica-INFIQC, Ciudad Universitaria, Universidad Nacional de Cordoba, Córdoba, Argentina 
593 |a Departamento de Farmacia, Ciudad Universitaria, Universidad Nacional de Cordoba, 5000 Córdoba, Argentina 
593 |a Departamento de Física, Fac. de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Buenos Aires, Argentina 
690 1 0 |a AM1 CALCULATIONS 
690 1 0 |a ANTIRETROVIRAL ANALOGS 
690 1 0 |a CONFORMATIONAL ANALYSIS 
690 1 0 |a NMR STUDIES 
690 1 0 |a NOVEL AZT DERIVATIVES 
690 1 0 |a 3' AZIDO 3' DEOXY 5' O ISONICOTINOYLTHYMIDINE 
690 1 0 |a 5 BROMO 6,5' EPOXY 5,6 DIHYDRO 3' AZIDO 3' DEOXYTHYMIDINE 
690 1 0 |a NUCLEOSIDE 
690 1 0 |a UNCLASSIFIED DRUG 
690 1 0 |a ZIDOVUDINE 
690 1 0 |a ZIDOVUDINE DERIVATIVE 
690 1 0 |a ANALYTIC METHOD 
690 1 0 |a ARTICLE 
690 1 0 |a CALCULATION 
690 1 0 |a CORRELATION ANALYSIS 
690 1 0 |a DIASTEREOISOMER 
690 1 0 |a DRUG CONFORMATION 
690 1 0 |a NUCLEAR MAGNETIC RESONANCE 
690 1 0 |a NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY 
690 1 0 |a ROTATION 
690 1 0 |a STRUCTURE ANALYSIS 
690 1 0 |a ANTI-RETROVIRAL AGENTS 
690 1 0 |a MAGNETIC RESONANCE SPECTROSCOPY 
690 1 0 |a MOLECULAR CONFORMATION 
690 1 0 |a ZIDOVUDINE 
700 1 |a Motura, M.I. 
700 1 |a Contreras, Rubén Horacio 
700 1 |a Pierini, A.B. 
700 1 |a Briñón, M.C. 
773 0 |d 2003  |g v. 22  |h pp. 45-62  |k n. 1  |p Nucleosides Nucleotides Nucleic Acids  |x 15257770  |w (AR-BaUEN)CENRE-6328  |t Nucleosides, Nucleotides and Nucleic Acids 
856 4 1 |u https://www.scopus.com/inward/record.uri?eid=2-s2.0-0037238689&doi=10.1081%2fNCN-120018622&partnerID=40&md5=646d85b83a0b2d5c8b9b669da51856d0  |y Registro en Scopus 
856 4 0 |u https://doi.org/10.1081/NCN-120018622  |y DOI 
856 4 0 |u https://hdl.handle.net/20.500.12110/paper_15257770_v22_n1_p45_Baumgartner  |y Handle 
856 4 0 |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_15257770_v22_n1_p45_Baumgartner  |y Registro en la Biblioteca Digital 
961 |a paper_15257770_v22_n1_p45_Baumgartner  |b paper  |c PE 
962 |a info:eu-repo/semantics/article  |a info:ar-repo/semantics/artículo  |b info:eu-repo/semantics/publishedVersion 
999 |c 65956