Acyclic tri-peptide c-terminal carboxylic acid.

Abstract

Racemate diastereoisome and optical isome of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-l6 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with Cl-6 alkyl; Cl-6 alkoxy; Cl-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with Cl-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4-C(O)-; a carboxyl of formula R4-O-C(O)-; an amide of formula R4-NH-C(O)-; a thioamide of formula R4-N(R5)-C(S)-;or a sulfonyl of formula R4-SO2; R5 is H or Cl-6 alkyl; and Y is H or Cl-6 alkyl; R3 is Cl-8 alkyl, C3-7 cycloalkyl, or C4-l0 alkylcycloalkyl, all optionally substituted with hydroxy, Cl-6 alkoxy, Cl-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-l6 aralkyl; R2 is CH2-R20, NH-R20, O-R20 or S-R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-l0 (alkylcycloalkyl), all of which being optionally mono-, di- or tri¬substituted with R21, or R20 is a C6 or C10 aryl or C7-l4 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-l4 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; Cl-6 alkyl, C3-7 cycloalkyl, or C2-6 alkenyl, all optionally substituted with halogen.