A new class of pyrazolo[5,1-a]isoquinolines, pyrazolo[5,1-f][1,6]naphthyridines, pyrazolo[5,1-a][2,6]naphthyridines, pyrazolo[5,1-a][2,7]naphthyridines and pyrazolo[1,5-h][1,7]naphthyridines were designed as bioisosteres of pyrazolo[1,5-c]quinazolines, described as potent inhibitors of PDE10A enzyme. In fact, bioisosteric modifications of the tricyclic core of the above known molecules might offer new templates that could provide optimized interactions with the PDE10A enzyme and desiderable pharmacokinetic properties. This work allowed to synthesize a small library of compounds incorporating a bi-substituted tricyclic pyrazole-based platform. A reproducible and efficientone-potsynthesis was achieved for the above-mentioned compounds.

Sintesi e studiSARdi nuove piattaforme tricicliche a struttura pirazolo-isochinolinica e pirazolo-naftiridinica come inibitori dell’enzima fosfodiesterasi 10A (PDE10A) / Dore, Antonio. - (2013 Feb 18).

Sintesi e studiSARdi nuove piattaforme tricicliche a struttura pirazolo-isochinolinica e pirazolo-naftiridinica come inibitori dell’enzima fosfodiesterasi 10A (PDE10A)

DORE, Antonio
2013

Abstract

A new class of pyrazolo[5,1-a]isoquinolines, pyrazolo[5,1-f][1,6]naphthyridines, pyrazolo[5,1-a][2,6]naphthyridines, pyrazolo[5,1-a][2,7]naphthyridines and pyrazolo[1,5-h][1,7]naphthyridines were designed as bioisosteres of pyrazolo[1,5-c]quinazolines, described as potent inhibitors of PDE10A enzyme. In fact, bioisosteric modifications of the tricyclic core of the above known molecules might offer new templates that could provide optimized interactions with the PDE10A enzyme and desiderable pharmacokinetic properties. This work allowed to synthesize a small library of compounds incorporating a bi-substituted tricyclic pyrazole-based platform. A reproducible and efficientone-potsynthesis was achieved for the above-mentioned compounds.
Pirazolo-isochinolina; pirazolo-naftiridina; argento triflato; Sonogashira
Sintesi e studiSARdi nuove piattaforme tricicliche a struttura pirazolo-isochinolinica e pirazolo-naftiridinica come inibitori dell’enzima fosfodiesterasi 10A (PDE10A) / Dore, Antonio. - (2013 Feb 18).
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11388/250801
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