Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 3: 8-Thiocarboxamido and 8-thioformamido derivatives of cyclazocine.
8-Position variants of cyclazocine have been made where the phenolic 8-OH was replaced by thioamide, amidine, guanidine, urea and thiourea groups. High affinity for opioid receptors was observed for the 8-CSNH2 and 8-NHCHS analogues indicating that these groups are isosteric with not only the 8-OH but with the previously synthesized 8-CONH2 and 8-NHCHO cyclazocine derivatives.
Wentland
Mark P
MP
Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, Troy, NY 12180, USA. wentmp@rpi.edu
Sun
Xufeng
X
Bu
Yigong
Y
Lou
Rongliang
R
Cohen
Dana J
DJ
Bidlack
Jean M
JM
D003496:Cyclazocine / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D003496:Cyclazocine