Structure activity studies on chemically modified homologues of the antibiotic phytotoxic leucinostatin A.
The synthesis and a conformational study of a number of homologues of the well known antibiotic, phytotoxic leucinostatin A are reported. The circular dichroism of all the compounds are discussed. Some conclusions on the SAR of these compounds are drawn. The influence of the alpha-helical conformation and/or the increased lipophile character on their interesting biological activities is emphasized.
Vertuani
G
G
Dipartimento de Scienze Farmaceutiche, Università di Ferrara, Italy.
Boggian
M
M
Scatturin
A
A
Ricci
M
M
Meli Balbocchino
B
B
Tuttobello
L
L
Rossi
C
C
D000595:Amino Acid Sequence; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D023181:Antimicrobial Cationic Peptides; D002942:Circular Dichroism; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008969:Molecular Sequence Data; D010455:Peptides; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000903:Antibiotics, Antineoplastic; D023181:Antimicrobial Cationic Peptides; D010455:Peptides; C008268:leucinostatin A