85676-33-1Relevant academic research and scientific papers
Studies on analgesic oligopeptides. II. Structure-activity relationship among thirty analogs of a cyclic dipeptide, cyclo(-Tyr-Arg-)
Sasaki,Akutsu,Matsui,Suzuki,Sakurada,Sato,Kisara
, p. 4435 - 4443 (2007/10/02)
Thirty diketopiperazines were synthesized as analogs of cyclo(-Tyr-Arg-). The analgesic activities of these analogs were evaluated after intracerebral administration in mice. In the cyclo(-X-Arg-) series of analogs, cyclo[-Tyr(Et)-Arg-] showed the most po
Further Studies on the Use of Multi-substituted Benzenesulfonyl Groups for Protection of the Guanidino Function of Arginine
Fujino, Masahiko,Wakimasu, Mitsuhiro,Kitada, Chieko
, p. 2825 - 2831 (2007/10/02)
Various multi-substituted benzenesulfonyl protecting groups for the guanidino function of arginine, removable under mild conditions such as with trifluoroacetic acid (TFA)-thioanisole, were studied.Among them, the 4-methoxy-2,6-dimethylbenzenesulfonyl (Mds) group, the 2,3,4,5,6-pentamethylbenzenesulfonyl (Pme) group, and the 4-methoxy-2,3,6-trimethylbenzenesulfonyl (Mtr) group were found to be useful.Both Mds and Pme show considerable resistance to TFA and, therefore, are suitable for procedures in which the intermediates are deprotected by TFA treatment, while Mtr is the most useful protecting group when TFA treatment is not necessary.Keywords---4-methoxy-2,6-dimethylbenzenesulfonyl (Mds); 2,4,6-trimethoxybenzenesulfonyl (Mtb); 2,3,4,5,6-pentamethylbenzenesulfonyl (Pme); 4-methoxy-2,3,6-trimethylbenzenesulfonyl (Mtr); trifluoroacetic acid-thioanisole deprotection
