Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer

• Main Authors: Jonathan Elie (Author), Johnny Vercouillie (Author), Nicolas Arlicot (Author), Lucas Lemaire (Author), Rudy Bidault (Author), Sylvie Bodard (Author), Christel Hosselet (Author), Jean-Bernard Deloye (Author), Sylvie Chalon (Author), Patrick Emond (Author), Denis Guilloteau (Author), Frédéric Buron (Author), Sylvain Routier (Author)
• Format: Book
• Published: Taylor & Francis Group, 2019-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

A series of novel derivatives exhibiting high affinity and selectivity towards the COX-2 enzyme in the (aza) indazole series was developed. A short synthetic route involving a bromination/arylation sequence under microwave irradiation and direct C-H activation were established in the indazole and az...