7α-methoxy-2-[(substituted)methylene]cephem sulfones as inhibitors of human leukocyte elastase and thrombin

Reddy, A. V. N.; Fiakpui, Charles Y.; Czajkowski, David P.; Kaleta, J.; Micetich, Ronald G.; Maiti, Samarendra N.

doi:10.1007/bf02256808

Chem Heterocycl Compd

1998

DOI: 10.1007/bf02256808

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7α-methoxy-2-[(substituted)methylene]cephem sulfones as inhibitors of human leukocyte elastase and thrombin

A. V. N. Reddy¹,

Charles Y. Fiakpui²,

David P. Czajkowski³

et al.

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ChemInform Abstract: 7α‐Methoxy‐2‐[(substituted)methylene]cephem Sulfones as Inhibitors of Human Leukocyte Elastase and Thrombin.

Reddy¹,

Fiakpui²,

Czajkowski³

et al. 1999

ChemInform

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-2327α-Methoxy-2-[(substituted)methylene]cephem Sulfones as Inhibitors of Human Leukocyte Elastase and Thrombin.-A series of title methylene-substituted cephem sulfones (III) is prepared as a mixture of E/Z-isomers by BuLi-mediated coupling of cephem sulfones (I) with hetaryl aldehydes (yields given in g). It is shown that the acetoxymethyl-substituted cephem derivatives are good elastase inhibitors independent on the double bond geometry or the nature of hetaryl substituent. Additionally, they possess good thrombin inhibiting activity. -(REDDY, ANDHE V. NARENDER; FIAKPUI, CHARLES Y.; CZAJKOWSKI, DAVID P.; KALETA, JADWIGA; MICETICH, RONALD G.; MAITI, SAMARENDRA N.; Khim. Geterotsikl. Soedin. (1998) 11, 1510-1516; SynPhar Lab. Inc., Edmonton, Alberta T6E 5V2, Can.; EN)

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ChemInform Abstract: 7α‐Methoxy‐2‐[(substituted)methylene]cephem Sulfones as Inhibitors of Human Leukocyte Elastase and Thrombin.

Reddy¹,

Fiakpui²,

Czajkowski³

et al. 1999

ChemInform

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show abstract

In vitro evaluation of the antielastase activity of polycyclic β-lactams

Monleón¹,

Díez-García²,

Zamora³

et al. 2012

Bioorganic Chemistry

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7α-methoxy-2-[(substituted)methylene]cephem sulfones as inhibitors of human leukocyte elastase and thrombin

Cited by 2 publications

References 11 publications

ChemInform Abstract: 7α‐Methoxy‐2‐[(substituted)methylene]cephem Sulfones as Inhibitors of Human Leukocyte Elastase and Thrombin.

ChemInform Abstract: 7α‐Methoxy‐2‐[(substituted)methylene]cephem Sulfones as Inhibitors of Human Leukocyte Elastase and Thrombin.

In vitro evaluation of the antielastase activity of polycyclic β-lactams

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