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cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.

Abstract：

:The 5,5-bicycles cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene 3 and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole 4 were designed as rotationally restricted templates towards the preparation of inhibitors of CAC1 cysteinyl proteinases. The design strategy was exemplified through the solution and solid phase preparation of potent inhibitors of human cathepsin K and may potentially be applied to inhibitors of other CAC1 proteinases.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wang Y,Benn A,Flinn N,Monk T,Ramjee M,Watts J,Quibell M

doi

10.1016/j.bmcl.2005.01.022

subject

Has Abstract

pub_date

2005-03-01 00:00:00

pages

1327-31

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00069-7

journal_volume

15

pub_type

杂志文章

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