Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams

C Hulme; K Moriarty; F C Huang; J Mason; D McGarry; R Labaudiniere; J Souness; S Djuric

doi:10.1016/s0960-894x(98)00036-5

Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams

Bioorg Med Chem Lett. 1998 Feb 17;8(4):399-404. doi: 10.1016/s0960-894x(98)00036-5.

Authors

C Hulme¹, K Moriarty, F C Huang, J Mason, D McGarry, R Labaudiniere, J Souness, S Djuric

Affiliation

¹ Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.

PMID: 9871693
DOI: 10.1016/s0960-894x(98)00036-5

Abstract

This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE IV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition.

MeSH terms

3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
Cyclic Nucleotide Phosphodiesterases, Type 4
Lactams / chemical synthesis*
Lactams / chemistry
Lactams / pharmacology*
Phosphodiesterase Inhibitors / chemical synthesis*
Phosphodiesterase Inhibitors / chemistry
Phosphodiesterase Inhibitors / pharmacology*
Structure-Activity Relationship

Substances

Lactams
Phosphodiesterase Inhibitors
3',5'-Cyclic-AMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 4