The Synthesis and Antifungal Activity of Nitrogen Containing Hemiaminal Ethers of LY303366

LY303366, currently in phase II clinical trials, is a semisynthetic, broad spectrum, fungicidal agent derived through extensive structure-activity relationship (SAR) studies based on the echinocandin B (ECB) nucleus. Possession of such potent activity against clinically important fungi such as Asper...

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Veröffentlicht in:	Journal of antibiotics 1998/02/25, Vol.51(2), pp.239-242
Hauptverfasser:	JAMISON, JAMES A., LAGRANDEUR, LISA M., RODRIGUEZ, MICHAEL J., TURNER, WILLIAM W., ZECKNER, DOUGLAS J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anidulafungin Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antifungal Agents - chemical synthesis Antifungal Agents - chemistry Antifungal Agents - pharmacology Aspergillus fumigatus Biological and medical sciences Candida albicans Candida parapsilosis Candidiasis - drug therapy Echinocandins Male Medical sciences Mice Mice, Inbred ICR Microbial Sensitivity Tests Peptides, Cyclic - chemical synthesis Peptides, Cyclic - chemistry Peptides, Cyclic - pharmacology Pharmacology. Drug treatments Structure-Activity Relationship
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Zusammenfassung:	LY303366, currently in phase II clinical trials, is a semisynthetic, broad spectrum, fungicidal agent derived through extensive structure-activity relationship (SAR) studies based on the echinocandin B (ECB) nucleus. Possession of such potent activity against clinically important fungi such as Aspergillus fumigatus, Candida albicans and Candida parapsilosis has prompted subsequent SAR studies focused on two major properties. First, improving the water solubility (
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.51.239