2 .beta.-substituted thiomethylpenicillin derivatives and their

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540304, 540310, 514196, 514197, 514200, A61K 31425, C07D49900

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active

048617687

ABSTRACT:
Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.

REFERENCES:
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patent: 4218374 (1980-08-01), Kamiya et al.
English et al., "Antimicrobial Agents & Chemotherapy", vol. 14, No. 3, Sep. 1978, pp. 414-419.
Hall, T. W. et al., "Recent Advances in the Chemistry of .beta.-Lactam Antibiotics", 1985, pp. 242-254.
Gottstein et al., J. Med Chem., 1981, 24, 1531-1534.
J. Med. Chem., 1985, 28, 518-522, Gottstein et al.
Chemical Abstracts, vol. 100, No. 11, Mar. 12th, 1984, p. 256, No. 85504y.

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