Synthesis and antifungal activities of pradimicin A derivatives modification of the alanine moiety.
Chemical modifications of the carboxyl group in the alanine moiety of pradimicin A were performed and in vitro and in vivo antifungal activities of the derivatives were examined in comparison with those of pradimicin A. The amide derivatives showed activities comparable to pradimicin A, indicating that the free carboxyl group can be modified without impairing the antifungal activity.
Nishio
M
M
Bristol-Myers Squibb Research Institute, Tokyo, Japan.
Ohkuma
H
H
Kakushima
M
M
Ohta
S
S
Iimura
S
S
Hirano
M
M
Konishi
M
M
Oki
T
T
D000409:Alanine / Q000031:analogs & derivatives; D000818:Animals; D018943:Anthracyclines; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002177:Candidiasis / Q000188:drug therapy; D051379:Mice; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D000095643:Pradimicins and Benanomicins
D000409:Alanine; D018943:Anthracyclines; D000903:Antibiotics, Antineoplastic; D000935:Antifungal Agents; C058036:pradimicin A; D000095643:Pradimicins and Benanomicins