Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Dunlap Richard Paul"'
Autor:
Dennis J. Hlasta, Dunlap Richard Paul, Ranjit C. Desai, Jian Shen, Catherine A. Franke, John J. Court, Timothy G. Talomie, Albert J. Mura
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2941-2946
Distinct differences in the SAR for HLE and PPE inhibition in this class of compounds were observed. For example, larger lipophilic substituents at the benzisothiazolone 4-position afforded inhibitors that were potent against HLE, but inactive agains
Autor:
Dennis J. Hlasta, David Robinson, Catherine A. Franke, Judith A. Johnson, James L. Kofron, Robert P. Farrell, Timothy G. Talomie, Dunlap Richard Paul, James H. Ackerman, John J. Court
Publikováno v:
Journal of Medicinal Chemistry. 38:4687-4692
Human leukocyte elastase (HLE) has been proposed to be a primary mediator of pulmonary emphysema, and inhibitors of this enzyme should be effective in the treatment of emphysema and other pulmonary diseases. We have discovered a novel class of alicyc
Autor:
Dennis J. Hlasta, Edward Ferguson, Robert J. Gordon, John Court, Catherine A. Franke, Ranjit C. Desai, Dunlap Richard Paul
Publikováno v:
Journal of Medicinal Chemistry. 38:1571-1574
A novel class of alkyl and aryl phosphonate and phosphinate acid-based leaving groups has been developed for utilization in the synthesis of benzoisothiazolone (BIT) inhibitors of human leukocyte elastase (HLE). A number of BITs were synthesized with
Autor:
Robert J. Gordan, Chakrapani Subramanyam, W. Mark Eickhoff, Marion L. Drozd, David T. Robinson, Edward D. Pagani, Judith A. Johnson, Dennis J. Hlasta, Catherine A. Franke, Ranjit Ch Desai, Paul J. Silver, Alan L. Maycock, John F. Newton, Edward W. Ferguson, Dunlap Richard Paul, Eugene R. Baizman
Publikováno v:
Drug Development Research. 34:306-316
The proteolytic activity of human neutrophil elastase (HNE) has been implicated in a number of pulmonary diseases. We report on the activity of an orally bioavailable, selective HNE inhibitor, WIN 63759 [6-methoxy-4-(1-methylethy)-3-oxo-1,2-benzisoth
Autor:
Virendra Kumar, Malcolm R. Bell, Arup K. Ghose, Catherine A. Franke, Albert J. Mura, Dunlap Richard Paul, Chakrapani Subramanyam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:325-330
Potent mechanism based inhibition of human leukocyte elastase (HLE) by tetrahydrobenzisothiazolones ( 2 ) is described. Structure activity relationships studies led to the identification of WIN 62816 ( 2c ), the most potent inhibitor in this series w
Autor:
Dennis J. Hlasta, Virendra Kumar, Kenneth C. Cundy, Malcolm R. Bell, Chakrapani Subramanyam, Alan L. Maycock, Ranjit C. Desai, E. Ferguson, A. J. Mura, C. A. Franke, Dunlap Richard Paul, Anne G. Rowlands, Robert J. Gordon, Shari L. Eiff, John J. Court
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:331-336
The lead compound for this SAR study, benzisothiazolone 1a, was a 15 nM inhibitor of HLE, but was unstable in human blood ( t 1 2 min). The introduction of lipophilic substituents at the R4-position such as ethyl or isopropyl and modulation of the el
Autor:
Robert G. Gordon, Albert J. Mura, Edward Ferguson, Malcolm R. Bell, Dunlap Richard Paul, Catherine A. Franke, Chakrapani Subramanyam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:319-324
A series of 4-isopropyl benzisothiazolinylmethyl aryl ethers were prepared and evaluated as inhibitors of human leukocyte elastase (HLE). Among the phenols attached as leaving groups onto N-methyl of the 4-isopropyl benzisothiazolone nucleus, the sul
Autor:
Timothy G. Talomie, C. A. Franke, Dunlap Richard Paul, E. Ferguson, Ranjit C. Desai, Robert J. Gordon, Robert P. Farrell, Dennis J. Hlasta
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:105-109
Alkoxy substituted benzisothiazolones (BIT) are reported as inhibitors of human leukocyte elastase (HLE). Structure-activity relationship study results are described. The contribution of alkoxy substituents towards improving the stability of BIT deri
Autor:
A. J. Mura, Dennis J. Hlasta, Chakrapani Subramanyam, C. A. Franke, Dunlap Richard Paul, Malcolm R. Bell, John J. Court, Ranjit C. Desai, Neil W. Boaz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1801-1806
A new type of mechanism-based inhibitor of human leukocyte elastase (HLE) is described that are designed to inhibit HLE by a suicide route to form an inhibitor-enzyme complex by cross linking the enzyme active site. A mechanism of HLE inhibition is p
Autor:
Ranjit C. Desai, Dennis J. Hlasta, Robert J. Gordon, Robert P. Farrell, E. Ferguson, Timothy G. Talomie, C. A. Franke, Dunlap Richard Paul
Publikováno v:
ChemInform. 26
Alkoxy substituted benzisothiazolones (BIT) are reported as inhibitors of human leukocyte elastase (HLE). Structure-activity relationship study results are described. The contribution of alkoxy substituents towards improving the stability of BIT deri