212204-36-9Relevant academic research and scientific papers
Efficient synthesis of protected sulfonopeptides from N-protected 2-aminoalkyl xanthates and thioacetates
Kakaei, Saeed,Xu, Jiaxi
, p. 9068 - 9075 (2013/09/24)
An efficient and convenient method was developed for the synthesis of protected sulfonopeptides via N-chlorosuccimide (NCS)/HCl oxidative chlorination of N-protected 2-aminoalkyl xanthates or thioacetates to the corresponding sulfonyl chlorides followed b
An efficient and facile synthesis of N-Cbz-β-aminoalkanesulfonamides
Meng, Fanhua,Chen, Ning,Xu, Jiaxi
, p. 2548 - 2553 (2013/06/27)
An efficient method for the synthesis of N-Cbz-β- aminoalkanesulfonamides was described. N-Cbz-β-aminoalkanesulfona-mides were readily prepared in good yields from a variety of amino alcohols, including optically active ones, via N-Cbz protection with ben
Synthesis and activity of endomorphin-2 and morphiceptin analogues with proline surrogates in position 2
Giordano, Cesare,Sansone, Anna,Masi, Annalisa,Lucente, Gino,Punzi, Pasqualina,Mollica, Adriano,Pinnen, Francesco,Feliciani, Federica,Cacciatore, Ivana,Davis, Peg,Lai, Josephine,Ma, Shou-Wu,Porreca, Frank,Hruby, Victor
experimental part, p. 4594 - 4600 (2010/10/19)
The opioid agonists endomorphins (Tyr-Pro-Trp-Phe-NH2; EM1 and Tyr-Pro-Phe-Phe-NH2; EM2) and morphiceptin (Tyr-Pro-Phe-Pro-NH 2) exhibit an extremely high selectivity for μ-opioid receptor. Here a series of novel EM2 and morphiceptin analogues containing in place of the proline at position 2 the S and R residues of β-homologues of proline (HPro), of 2-pyrrolidinemethanesulphonic acid (HPrs) and of 3- pyrrolidinesulphonic acid (βPrs) have been synthesized and their binding affinity and functional activity have been investigated. The highest μ-receptor affinity is shown by [(S)βPrs2]EM2 analogue (6e) which represents the first example of a β-sulphonamido analogue in the field of opioid peptides.
