pyrrolopyrimidine and Pain

pyrrolopyrimidine has been researched along with Pain* in 1 studies

Other Studies

1 other study(ies) available for pyrrolopyrimidine and Pain

Article	Year
Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists. Bioorganic & medicinal chemistry letters, 2012, Mar-01, Volume: 22, Issue:5 Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Na(v)1.7 antagonists. Hit-to-lead SAR studies of the pyrrolopyrimidine core, head, and tail groups of the molecule led to the identification of pyrrolopyrimidine 48 as exceptionally potent Na(v)1.7 blocker with good selectivity over hERG and improved microsomal stability relative to our hit molecule and pyrazolopyrimidine 8 as a promising starting point for future optimization efforts. Topics: Drug Discovery; Humans; Microsomes, Liver; NAV1.7 Voltage-Gated Sodium Channel; Pain; Pyrimidines; Pyrroles; Sodium Channel Blockers; Sodium Channels; Structure-Activity Relationship	2012

Article

Year

Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.

Bioorganic & medicinal chemistry letters, 2012, Mar-01, Volume: 22, Issue:5

Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Na(v)1.7 antagonists. Hit-to-lead SAR studies of the pyrrolopyrimidine core, head, and tail groups of the molecule led to the identification of pyrrolopyrimidine 48 as exceptionally potent Na(v)1.7 blocker with good selectivity over hERG and improved microsomal stability relative to our hit molecule and pyrazolopyrimidine 8 as a promising starting point for future optimization efforts.

Topics: Drug Discovery; Humans; Microsomes, Liver; NAV1.7 Voltage-Gated Sodium Channel; Pain; Pyrimidines; Pyrroles; Sodium Channel Blockers; Sodium Channels; Structure-Activity Relationship

2012