| 摘要 |
Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs:
R1-A1-A2-A3-A4-A5-R2 (I)
wherein:
A1 is Aib, Apc or Inp;A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp;A3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp;A4 is 2Fua, Orn, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl);A5 is Apc, Dab, Dap, Lys, Orn, or deleted;R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; andR2 is OH or NH2;
and pharmaceutical compositions and methods of use thereof. |
| 主权项 |
1. A compound according to formula (I):
R1-A1-A2-A3-A4-A5-R2 (I)or a pharmaceutically acceptable salt thereof, wherein:
A1 is Apc; A2 is D-Bal, D-1Nal, or D-2Nal; A3 is D-Bal or D-Trp; A4 is 2Fua, 2Pal, 3Pal, 4Pal, Pff, Phe, Taz, 2Thi, or 3Thi; A5 is Apc or deleted; R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and R2 is OH or NH2;provided that:
when A5 is deleted, then:
A4 is 2Fua, Pff, or Taz; orA1 is Apc and—
A2 is D-Bal; orA3 is D-Bal; orA4 is 2Thi, 3Thi, 2Pal, 3Pal, or 4Pal. |
