Synthesis and evaluation of backbone/amide-modified analogs of leualacin.
Leualacin (1), a cyclic depsi-pentapeptide, and its backbone/amide-modified analogs 2-4 were synthesized. Amide analogue 3 exhibited stronger vasodilatory effects. It also strongly inhibited collagen- and arachidonic acid (AA)-induced platelet aggregations with IC50s of 0.6 microM and 2.0 microM, respectively.
Hu
M K
MK
School of Pharmacy and Department of Pharmacology, National Defense Medical Center, Taipei, Taiwan, Republic of China.
Yang
F C
FC
Chou
C C
CC
Yen
M H
MH
D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D016718:Arachidonic Acid / Q000494:pharmacology; D003094:Collagen / Q000494:pharmacology; D066298:In Vitro Techniques; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D011921:Rats, Inbred WKY; D013929:Thromboxane B2 / Q000037:antagonists & inhibitors; D014665:Vasodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D047630:Depsipeptides
D016718:Arachidonic Acid; D003094:Collagen; D010456:Peptides, Cyclic; D010975:Platelet Aggregation Inhibitors; D013929:Thromboxane B2; D014665:Vasodilator Agents; C076086:leualacin; D047630:Depsipeptides