Pradimicin amide derivatives

C - Chemistry – Metallurgy – 07 – H

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C07H 15/252 (2006.01) C07H 15/244 (2006.01)

Patent

CA 2011117

Disclosed herein are pradimicin amides which are active as antifungal agents. Such compounds have the formula Image In the foregoing formula R1 is selected from the group consisting of H, methyl and hydroxymethyl; when R1 is methyl or hydroxymethyl the resulting amino acid has the D-configuration; R2 is selected from the group consisiting of -NR6R7, -NHNR6R7, NHCH2CO2H and (D)-NHCH(CH3)C02H; R6 is H and R7 is selected from the group consisting of H, C1-6alkyl, C3-6cycloalkyl, C6-10aryl, and C7-15aralkyl; or R6 and R7 are independently C1-6alkyl; or R6, R7 and the nitrogen to which they are attached form a 3- to 6-membered ring; R3 and R4 are each independently selected from the group consisting of H and C1-6alkyl; and R5 is H or .beta.-D-xylosyl; or a pharmaceutically acceptable salt thereof.

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