Cephalosporin antibiotics can be modified to inhibit human leukocyte elastase
- J. Doherty, B. Ashe, M. Zimmerman
- BiologyNature
- 10 July 1986
It is reported that neutral cephalosporins (that is, compounds not bearing a free carboxyl at position C-4) can be modified to become potent time-dependent inhibitors of HLE.
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
- J. Stelmach, Luping Liu, J. Doherty
- Chemistry, BiologyBioorganic & Medicinal Chemistry Letters
- 20 January 2003
Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
- J. Doherty, S. K. Shah, G. O. Chandler
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 15 September 1993
The properties of L-680,833 allow it to effectively supplement the activity of natural inhibitors of PMNE in vivo, suggesting that this type of low-molecular-weight synthetic inhibitor could have therapeutic value in diseases where PMNE damages tissue.
The Discovery and Biologic Properties of Cephalosporin‐Based Inhibitors of PMN Elastase
- P. Davies, B. Ashe, J. Doherty
- BiologyAnnals of the New York Academy of Sciences
- 1 May 1991
A failure to maintain normal levels of elastase and cathepsin G in mature PMNs in the beige mousezo has been described which may be due to inactivation of enzyme by inhibitors present.
Orally Active β‐Lactam Inhibitors of Human Leukocyte Elastase. Part 3. Stereospecific Synthesis and Structure‐Activity Relationships for 3,3‐Dialkylazetidin‐2‐ones.
- P. Finke, Shrenik K. Shah, J. Doherty
- Chemistry
- 17 October 1995
The organic chemistry of drug design and drug action. Von R. B. Silverman. Academic Press, New York, 1992. 422 S., geb. 38.00 £. – ISBN 0‐12‐643730‐0
- J. Doherty
- Chemistry
- 4 July 1994
A comparison of alpha 1-proteinase inhibitor methoxysuccinyl-Ala-Ala-Pro-Val-chloromethylketone and specific beta-lactam inhibitors in an acute model of human polymorphonuclear leukocyte…
- D. Fletcher, D. Osinga, J. Doherty
- Chemistry, BiologyAmerican Review of Respiratory Disease
- 1 March 1990
The duration of activity of these compounds as elastase inhibitors in this model correlated directly with the extent of their persistence in lung lavage fluid as determined by HPLC analysis of compound recovered by bronchoalveolar lavage.
Pharmacological profile of the substituted beta‐lactam L‐659,286: A member of a new class of human PMN elastase inhibitors
- R. Bonney, B. Ashe, J. Doherty
- Biology, ChemistryJournal of Cellular Biochemistry
- 1 January 1989
L‐659, 286 administered intratracheally inhibits lung damage caused by administration via the same route of human PMN elastase into hamsters, as it does not inhibit thrombin, trypsin, papain, plasmin, chymotrypsin or cathepsin G.
Crystallographie study of a β-lactam inhibitor complex with elastase at 1.84 Å resolution
- M. Navia, J. Springer, K. Hoogsteen
- Chemistry, BiologyNature
- 7 May 1987
The structure of a com-plex of porcine pancreatic elastase with the time-dependent irreversible inhibitor 3-acetoxymethyl-7-α-chloro-3-cephem-4-carboxylate-l,l-dioxide tert-butyl ester (I), the most potent of the β-lactamElastase inhibitors yet reported, is solved and partially refined at atomic resolution.
SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.
- Luping Liu, J. Stelmach, J. Doherty
- ChemistryBioorganic & Medicinal Chemistry Letters
- 17 November 2003
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