Solution-phase parallel synthesis of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles as activators of soluble guanylate cyclase withimproved oral bioavailability

Authors
Selwood, DL Brummell, DG Glen, RC Goggin, MC Reynolds, K Tatlock, MA Wishart, G
Citation
Dl. Selwood et al., Solution-phase parallel synthesis of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles as activators of soluble guanylate cyclase withimproved oral bioavailability, BIOORG MED, 11(8), 2001, pp. 1089-1092
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
8
Year of publication
2001
Pages
1089 - 1092
Database
ISI
SICI code
0960-894X(20010423)11:8<1089:SPSO51>2.0.ZU;2-A
Abstract
A lipophilicity constrained library of 5-carboxamido 1-benzyl-3-(3-dimethyl aminoproploxy)-1H-pyrazoles was prepared by solution-phase parallel synthes is with removal of acidic by-products using the strongly basic MP-carbonate resin. Compounds show both activation of soluble guanylate cyclase and inh ibition of platelet aggregation. Compound 12 also shows 22% oral bioavailab ility in rats. (C) 2001 Elsevier Science Ltd. All rights reserved.