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Synthesis of 6-(Thienylmethylene)penam Sulfones and their ${\beta}$-Lactamase Inhibitory Activities  

Kim, Dong-Hyeon (College of Pharmacy, Yeungnam University)
Thapa, Pritam (College of Pharmacy, Yeungnam University)
Karki, Radha (College of Pharmacy, Yeungnam University)
Jahng, Yurng-Dong (College of Pharmacy, Yeungnam University)
Lee, Eung-Seok (College of Pharmacy, Yeungnam University)
Publication Information
YAKHAK HOEJI / v.51, no.6, 2007 , pp. 447-454 More about this Journal
Abstract
The resistance of bacteria against ${\beta}$-lactam antibiotics is mainly caused by the production of ${\beta}$-lactamase enzymes. ${\beta}$-Lactamase inhibitors are used in combination with known antibiotics to overcome the growing problem of bacterial resistance. We prepared 6-(thienylmethylene)penam sulfones for the development of potent ${\beta}$-lactamase inhibitors and evaluated their ${\beta}$-lactamase inhibitory activities.
Keywords
${\beta}$-lactamase inhibitor; sulbactam; bacterial resistance; 6-(thienylmethylene)penam sulfone;
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1 Im, C, Maiti, S. N., Micetich, R. G. and Kunugita, C. : Synthesis and $\beta$-lactamase inhibitory activity of 6-[(l-hetero-arylthioethyl-l,2,3-triazol-4-yl)-methylene]penam sulfones. J. Antibiot. 47, 1030 (1994)
2 Buynak, J. D., Wu, K., Bachmann, B., Khasnis, D., Hua, L., Nguyen, H. K. and Carver, C. L. : Synethsis and biological activity of 7-alkylidenecephems. J. Med. Chem. 38, 1022 (1995)
3 Chen, Y. L., Chang, C. W. and Hedberg, K. : Synthesis of a potent $\beta$-lactamase inhibitor-l,l-dioxo-6-(2-pyridyl)methyl-enepenicillanic acid and its reaction with sodium methoxide. Tetrahedron Lett. 27, 3449 (1986)
4 Knowles, J. R. : Penicillin resistance : The chemistry of $\beta$-lactamase inhibitor. Acc. Chem. Res. 18, 97 (1985)
5 Sykes, R. B.: ${\beta}-Lactam$ antibiotics. Academic press, New York, p. 199 (1981)
6 Foulds, C. D., Kosmirak, M. and Sammes, E G. : Synthesis penicillanic and 1,1-dioxides as $\beta$-lactamase inhibitors: Studies on 6-benzylidene-and hydroxybenzylpenam sulfones. J. Chem. Soc. Perkin Trans. I 963 (1985)
7 Chen, Y. L., Chang, C. W., Hedberg, K. and Guarino, K. : Structure-activity relationships of 6-(heterocyclyl)methylene penam sulfones: A new class of $\beta$-lactamase inhibitors. J. Antibiot. 40, 803 (1987)
8 Ogawara, H. : Antibiotic resistance in pathogenic and producing bacteria with special reference to ${\beta}-lactam$ antibiotics. Microbiol. Rev. 45, 591 (1981)