Synthesis and antiviral evaluation of nucleic acid based...

C - Chemistry – Metallurgy – 07 – B

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C07B 61/00 (2006.01) A61K 31/7052 (2006.01) A61P 31/12 (2006.01) C07H 19/06 (2006.01) C07H 19/16 (2006.01) C07H 21/00 (2006.01)

Patent

CA 2415368

The present invention provides for compositions and methods to generate a library of small molecules that mimic the repertoire of interactions that exist amongst nucleic acids, and proteins, as well as, that which exist between proteins and nucleic acids. The designed library of nucleoside analogs are for use as competitive and non-competitive viral replication inhibitors or serve as pro-drugs of inhibitors in anti-viral drug discovery. A facile parallel solution-phase chemistry has been developed to carry out the combinatorial synthesis of nucleoside analogs as a source of pharmacore-based chemical diversity.

La présente invention concerne des compositions et des procédés de création d'une bibliothèque de petites molécules imitant le répertoire immunologique des interactions existant parmi des acides nucléiques, et des protéines, ainsi que celles existant entre des protéines et des acide nucléiques. Selon l'invention, la bibliothèque d'analogues de nucléosides sont utiles en tant qu'inhibiteurs compétitifs et non compétitifs de la réplication virale ou agissent comme prodrogues d'inhibiteurs dans la découverte des médicaments antiviraux. On a développé une chimie parallèle en phase de solution en vue d'effectuer la synthèse d'analogues de nucléosides en tant que source de diversité chimique sur la base d'évaluation pharmacologique.

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