Synthesis and biological activities of [beta-Malyl1]- and [beta-Malyl1, Leu8]-angiotensin II analogues.
The synthesis of [beta-Malyl1]- and [beta-Malyl1, Leu8]-angiotensin II using a solid phase procedure is reported. The replacement of the N-terminal amino group of aspartic acid by a hydroxyl group gives analogues with lower affinity than [Asn1]- and [Asn1, Leu8]-AII. However, the isoster [beta-Malyl1]-AII shows higher potency than [Asn1]-AII and this may be due to metabolic or enzymatic resistance.
D000596:Amino Acids / Q000032:analysis; D000804:Angiotensin II / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D011817:Rabbits; D051381:Rats
D000596:Amino Acids; D000804:Angiotensin II; C037896:angiotensin II, 1-malyl-Leu(8)-; C037895:angiotensin II, 1-malyl-