PF1022A--a novel anthelmintic cyclooctadepsipeptide. Modification and exchange of the N-methyl leucine residues.
The first structure-activity relationships of the anthelmintic cyclooctadepsipeptide PF1022A have been established via a systematic exchange of the leucine residues by a series of related N-alkylated amino acids. The data presented strongly suggest that (L)-N-methyl-leucine is crucial for high in vivo activity.
Scherkenbeck
J
J
Bayer AG, Leverkusen, Germany. JUERGEN SCHERKENBECK.JS@bayer-ag.de
Harder
A
A
Plant
A
A
Dyker
H
H
D000478:Alkylation; D000596:Amino Acids; D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D047630:Depsipeptides; D015195:Drug Design; D005243:Feces / Q000469:parasitology; D006188:Haemonchiasis / Q000188:drug therapy*; D006189:Haemonchus / Q000302:isolation & purification; D007930:Leucine; D015394:Molecular Structure; D010270:Parasite Egg Count; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry* / Q000627:therapeutic use; D011487:Protein Conformation; D012756:Sheep; D013329:Structure-Activity Relationship
D000596:Amino Acids; D000871:Anthelmintics; D047630:Depsipeptides; D010456:Peptides, Cyclic; C075544:PF 1022A; D007930:Leucine