| 摘要 |
Disclosed herein are peptide derivatives which inhibit the activity of human immunodeficiency virus (HIV) protease. The peptide derivatives can be represented by general formula R<1>-R<2>-Y-R<3>-R<4> wherein R<1> is an optionally substituted 3-(1,2,3,4-tetrahydroisoquinolyl)carbonyl residue, R<2> and R<3> are amino acid or analogous amino acid residues (R<3> may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R<4> is [-NR<1><7>CH(R<1><8>)C(O)]p-Z wherein R<1><7> is hydrogen or lower alkyl, R<1><8> is an amino acid or analogous amino acid side chain, p is zero or 1 and Z is a terminal group (e.g. hydroxy or amino), or R<4> is -NR<1><7>CR<1><8>(R<2><1>)CH2OH wherein R<1><7> and R<1><8> are as noted hereinabove and R<2><1> is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives also inhibit renin activity. Accordingly, the derivatives can be used for combating HIV infections or for treating hypertension or congestive heart failure. |
