The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I

Christopher Hulme; Kevin Moriarty; Bruce Miller; Rose Mathew; Mercy Ramanjulu; Paul Cox; John Souness; Ken M. Page; Joanne Uhl; Jeffrey Travis; Fu Chih Huang; Richard Labaudiniere; Stevan W. Djuric

doi:10.1016/S0960-894X(98)00324-2

The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I

Christopher Hulme
, Kevin Moriarty
, Bruce Miller
, Rose Mathew
, Mercy Ramanjulu
, Paul Cox
, John Souness
, Ken M. Page
, Joanne Uhl
, Jeffrey Travis
, Fu Chih Huang
, Richard Labaudiniere
, Stevan W. Djuric

Research output: Contribution to journal › Article › peer-review

22 Scopus citations

Abstract

This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds described contain an indole moiety which replaces the 'rolipram- like' 3-methoxy-4-cyclopentoxy motif. Several of the compounds presented possess low nanomolar IC₅₀'s for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-α levels in LPS challenged mice (mouse endotoxemia model) are also reported.

Original language	English (US)
Pages (from-to)	1867-1872
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	8
Issue number	14
DOIs	https://doi.org/10.1016/S0960-894X(98)00324-2
State	Published - Jul 21 1998
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(98)00324-2

Cite this

Hulme, C., Moriarty, K., Miller, B., Mathew, R., Ramanjulu, M., Cox, P., Souness, J., Page, K. M., Uhl, J., Travis, J., Huang, F. C., Labaudiniere, R., & Djuric, S. W. (1998). The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I. Bioorganic and Medicinal Chemistry Letters, 8(14), 1867-1872. https://doi.org/10.1016/S0960-894X(98)00324-2

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AU - Souness, John

AU - Page, Ken M.

AU - Uhl, Joanne

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AU - Djuric, Stevan W.

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The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I

Abstract

ASJC Scopus subject areas

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