Ontology highlight
ABSTRACT:
SUBMITTER: Schunk S
PROVIDER: S-EPMC4137374 | biostudies-literature | 2014 Aug
REPOSITORIES: biostudies-literature
Schunk Stefan S Linz Klaus K Hinze Claudia C Frormann Sven S Oberbörsch Stefan S Sundermann Bernd B Zemolka Saskia S Englberger Werner W Germann Tieno T Christoph Thomas T Kögel Babette-Y BY Schröder Wolfgang W Harlfinger Stephanie S Saunders Derek D Kless Achim A Schick Hans H Sonnenschein Helmut H
ACS medicinal chemistry letters 20140624 8
In a previous communication, our efforts leading from 1 to the identification of spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amine 2a as analgesic NOP and opioid receptor agonist were disclosed and their favorable in vitro and in vivo pharmacological properties revealed. We herein report our efforts to further optimize lead 2a, toward trans-6'-fluoro-4',9'-dihydro-N,N-dimethyl-4-phenyl-spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-b]indol]-4-amine (cebranopadol, 3a), which is currently in clinical de ...[more]