Synthesis and biological properties of a new series of anti-MRSA β-lactams; 2-(thiazol-2′-ylthio)carbapenems

Makoto Sunagawa; Hiroshi Yamaga; Hisatoshi Shinagawa; Hitoshi Houchigai; Yoshihiro Sumita

doi:10.1016/S0960-894X(01)80596-5

Synthesis and biological properties of a new series of anti-MRSA β-lactams; 2-(thiazol-2′-ylthio)carbapenems

Makoto Sunagawa, Hiroshi Yamaga, Hisatoshi Shinagawa, Hitoshi Houchigai, Yoshihiro Sumita

University Hospital

Research output: Contribution to journal › Article › peer-review

13 Citations (Scopus)

Abstract

Synthesis and biological properties of a new series of 1β-methyl carbapenems that have been variously substituted thiazol-2′-ylthio side chain on C-2 are described. Amongst synthesized compounds, 4′-arylthiazole derivatives showed potent anti-MRSA activity and the introduction of a quaternary cation was effective to reduce binding to human serum albumin without affecting the anti-MRSA activity.

Original language	English
Pages (from-to)	2793-2798
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	4
Issue number	23
DOIs	https://doi.org/10.1016/S0960-894X(01)80596-5
Publication status	Published - Dec 1994

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)80596-5

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AU - Sunagawa, Makoto

AU - Yamaga, Hiroshi

AU - Shinagawa, Hisatoshi

AU - Houchigai, Hitoshi

AU - Sumita, Yoshihiro

PY - 1994/12

Y1 - 1994/12

N2 - Synthesis and biological properties of a new series of 1β-methyl carbapenems that have been variously substituted thiazol-2′-ylthio side chain on C-2 are described. Amongst synthesized compounds, 4′-arylthiazole derivatives showed potent anti-MRSA activity and the introduction of a quaternary cation was effective to reduce binding to human serum albumin without affecting the anti-MRSA activity.

AB - Synthesis and biological properties of a new series of 1β-methyl carbapenems that have been variously substituted thiazol-2′-ylthio side chain on C-2 are described. Amongst synthesized compounds, 4′-arylthiazole derivatives showed potent anti-MRSA activity and the introduction of a quaternary cation was effective to reduce binding to human serum albumin without affecting the anti-MRSA activity.

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IS - 23

ER -

Synthesis and biological properties of a new series of anti-MRSA β-lactams; 2-(thiazol-2′-ylthio)carbapenems

Abstract

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