SYNTHESIS AND ANTIFUNGAL ACTIVITY OF PRADIMICIN DERIVATIVES: MODIFICATIONS ON THE AGLYCONE PART

Synthesis and antifungal activity of pradimicin analogs modified on the aglycone part is described. Upon modification studies at various sites of the aglycone part using pradimicin A (PRM A), C-11 position was found to be the sole site to be modified without loosing antifungal activity. Further modi...

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Veröffentlicht in:	Journal of antibiotics 1993/09/25, Vol.46(9), pp.1447-1457
Hauptverfasser:	ABURAKI, S., OKUYAMA, S., HOSHI, H., KAMACHI, H., NISHIO, M., HASEGAWA, T., MASUYOSHI, S., IIMURA, S., KONISHI, M., OKI, T.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics, Antineoplastic - chemical synthesis Antibiotics, Antineoplastic - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antifungal Agents - chemical synthesis Antifungal Agents - pharmacology Biological and medical sciences Carbohydrate Sequence Magnetic Resonance Spectroscopy Medical sciences Microbial Sensitivity Tests Molecular Sequence Data Molecular Structure Pharmacology. Drug treatments
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Zusammenfassung:	Synthesis and antifungal activity of pradimicin analogs modified on the aglycone part is described. Upon modification studies at various sites of the aglycone part using pradimicin A (PRM A), C-11 position was found to be the sole site to be modified without loosing antifungal activity. Further modification studies at C-11 position were carried out with 11-OH derivative of pradimicin T1 (PRM T1) because of its easy availability. Among the compounds prepared, 11-demethoxy derivative of PRM A (12) and 11-O-ethyl (13) and 11-O-fluoroethyl (14) derivatives of PRM T1 showed promising antifungal activity comparable to that of PRM A.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.46.1447