Caprazene as a novel compound and derivatives thereof, and...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/067 (2006.01) A61K 31/7072 (2006.01)

Patent

CA 2726147

Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1"'--amide derivative of the formula (II) (see formula II) and a caprazene-1" '-ester derivative of the formula (III) (see formula III) from caprazene. Further, there could be synthesized a caprazol-1" '-amide derivative of the formula (V) (see formula V) and a caprazol-1" '- amide-3'''-ester derivative and a caprazol-3'''-ester derivative, etc. from caprazol. Furthermore, an imidazolidinone derivative could be synthesized from the ring-opened product of the 1,4-diazepinone ring of caprazol. The novel caprazene derivative, novel caprazol derivative and novel imidazolidinone derivative now synthesized exhibit excellent antibacterial activities against a variety of bacteria, including acid-fast bacteria.

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