National Science Council

Chun Chieh Lin

Shwu-chen Tsay

Jih Ru Hwu

Gholam H Hakimelahi

Wan-Lin Chen

Ching-Tai Chou

Abdolmajid Azaripour

Himatkumar V Patel

Hasan Mottaghian

Buh-Luen Chen

Wen Nan Tseng

Ali A Moshfegh

A series of phloroglucide derivatives are synthesized, which possess potent antibacterial activities. They include unsymmetrical phloroglucide analogs, phloroglucides attached to cephalosporins at the C-3&prime; position, and 7-(phloroglucidamido)cephalosporins.

Phloroglucidic acid and derivatives as antibacterial agents

A phloroglucide derivative having the following formula: ##STR1## wherein Q is halogen; X is CH.sub.2 or C.dbd.O; Y is cephalosporin having a formula of ##STR2## wherein Ph is phenyl, Ac is acetoxy, or pharmaceutically acceptable salts thereof, and an antibacterial pharmaceutical composition derived thereof.

Phloroglucide derivatives and their pharmceutical use

The present invention discloses a photo-induced DNA-cleaving agent composition comprises N-aryl-N-(alkyl or arylalkyl)hydroxylamine having the following formula: ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, halogen or halo(C.sub.1 -C.sub.6 alkyl)wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, halogen or halo(C.sub.1 -C.sub.6 alkyl); R.sub.2 is hydrogen; R.sub.3 is hydrogen or phenyl; R.sub.4 is hydrogen, phenyl, hydroxylphenyl, methoxyphenyl, dimethoxyphenyl, dimethylaminophenyl or naphthyl. The present N-aryl-N-(alkyl or arylalkyl)hydroxylamine is stable in dark, but it can react with O.sub.2 to form HO.multidot. radicals under irradiation of UV light for a period of 2-3 hours. The HO.multidot. radicals then react with DNA to accomplish cleavage of DNA.

Photo-induced DNA-cleaving agents

The present invention discloses a photo-induced DNA-cleaving agent composition comprises N-aryl-N-(alkyl or arylalkyl)hydroxylamine having the following formula: ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, halogen or halo(C.sub.1 -C.sub.6 alkyl)wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, halogen or halo(C.sub.1 -C.sub.6 alkyl); R.sub.2 is hydrogen; R.sub.3 is hydrogen or phenyl; R.sub.4 is hydrogen, phenyl, hydroxylphenyl, methoxyphenyl, dimethoxyphenyl, dimethylaminophenyl or naphthyl. The present N-aryl-N-(alkyl or arylalkyl)hydroxylamine is stable in dark, but it can react with O.sub.2 to form HO. radicals under irradiation of UV light for a period of 2-3 hours. The HO. radicals then react with DNA to accomplish cleavage of DNA.

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Taipei, Taiwan

Chun Chieh Lin