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|Title:||Cyclic peptide antifungal agents and process for preparation thereof|
|Abstract:||Provided are compounds of the formula (1): ##STR1## wherein R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --; R" and R'" are independently methyl or hydrogen; R and R.sup.y are independently hydroxy or hydrogen; R.sub.1 is hydroxy, hydrogen, or hydroxysulfonyloxy; R.sub.7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy; R.sub.2 is a acyl side chain. Also provided are formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R.dbd.H) forms of the compounds.|
|Inventor(s):||Burkhardt; Frederick J. (Indianapolis, IN), Debono; Manuel (Indianapolis, IN), Nissen; Jeffrey S. (Indianapolis, IN), Turner, Jr.; William W. (Bloomington, IN)|
|Assignee:||Eli Lilly and Company (Indianapolis, IN)|
1. A compound having the following formula: ##STR245##
2. A compound represented by the formula: ##STR246##
wherein R is --O(CH.sub.2).sub.3 CH.sub.3, --O(CH.sub.2).sub.4 CH.sub.3, --O(CH.sub.2).sub.5 CH.sub.3, --O(CH.sub.2).sub.2 O(CH.sub.2).sub.3 CH.sub.3, or --O(CH.sub.2).sub.2 OC(CH.sub.3).sub.3 prepared by acylating an amino nucleus of Echinocandin B with an active ester of a carboxylic acid represented by the formula: ##STR247##
wherein R is defined the same as above.
3. The compound of claim 2 wherein R is --O(CH.sub.2).sub.4 CH.sub.3.
4. The compound of claim 2 wherein said active ester is a 2,4,5-trichlorophenyl ester.
5. A compound represented by the formula: ##STR248##
wherein R is --O(CH.sub.2).sub.3 CH.sub.3, --O(CH.sub.2).sub.4 CH.sub.3, --O(CH.sub.2).sub.5 CH.sub.3, --O(CH.sub.2).sub.2 O(CH.sub.2).sub.3 CH.sub.3, or --O(CH.sub.2).sub.2 OC(CH.sub.3).sub.3.
6. A compound represented by the formula: ##STR249##
7. A pharmaceutically acceptable salt of a compound according to claim 6.
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