TY - JOUR
T1 - Synthesis and biological activity of novel backbone-bicyclic
T2 - Substance- P analogs containing lactam and disulfide bridges
AU - Bitan, Gal
AU - Sukhotinsky, Inna
AU - Mashriki, Yaffa
AU - Hanani, Menachem
AU - Selinger, Zvi
AU - Gilon, Chaim
PY - 1997
Y1 - 1997
N2 - A biased library of 60 novel backbone-bicyclic Substance P analogs was prepared by the simultaneous multiple peptide synthesis method. The peptides, containing both a lactam and a disulfide ring, were synthesized by combined Boc and Fmoc chemistries, and were cyclized on the resin. Cleavage of the S- benzyl group and oxidation of the sulfhydryl groups was enabled by adaptation of the diphenylsulfoxide trichloromethylsilane method to solid-phase synthesis. The peptides were screened for NK-1 and NK-3 activity, and were found to be weak agonists.
AB - A biased library of 60 novel backbone-bicyclic Substance P analogs was prepared by the simultaneous multiple peptide synthesis method. The peptides, containing both a lactam and a disulfide ring, were synthesized by combined Boc and Fmoc chemistries, and were cyclized on the resin. Cleavage of the S- benzyl group and oxidation of the sulfhydryl groups was enabled by adaptation of the diphenylsulfoxide trichloromethylsilane method to solid-phase synthesis. The peptides were screened for NK-1 and NK-3 activity, and were found to be weak agonists.
KW - Backbone-cyclic peptides
KW - Peptide libraries
KW - Substance P analog
UR - http://www.scopus.com/inward/record.url?scp=0030948998&partnerID=8YFLogxK
U2 - 10.1111/j.1399-3011.1997.tb00894.x
DO - 10.1111/j.1399-3011.1997.tb00894.x
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C2 - 9211223
AN - SCOPUS:0030948998
SN - 1397-002X
VL - 49
SP - 421
EP - 426
JO - Journal of Peptide Research
JF - Journal of Peptide Research
IS - 5
ER -