Structure-Activity studies for a novel series of tricyclic dihydropyrimidines as K(ATP) channel openers (KCOs).
A novel series of tricyclic dihydropyrimidines was synthesized and evaluated for activity as K(ATP) channel openers. The functional activity of several compounds, for example 6A (EC(50)=30nM) and its enantiomers exceeded cromakalim.
Drizin
Irene
I
Neuroscience Research, GPRD, Abbott Laboratories, 100 Abbott Park Road, IL 60064-6101, USA. irene.drizin@abbott.com
Holladay
Mark W
MW
Yi
Lin
L
Zhang
Henry Q
HQ
Gopalakrishnan
Sujatha
S
Gopalakrishnan
Murali
M
Whiteaker
Kristi L
KL
Buckner
Steven A
SA
Sullivan
James P
JP
Carroll
William A
WA
D000818:Animals; D018929:Cell Culture Techniques; D019806:Cromakalim / Q000494:pharmacology; D005453:Fluorescence; D006146:Guanidines / Q000008:administration & dosage / Q000493:pharmacokinetics; D006168:Guinea Pigs; D006575:Heterocyclic Compounds, 3-Ring / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects; D015221:Potassium Channels / Q000819:agonists / Q000187:drug effects*; D011725:Pyridines / Q000008:administration & dosage / Q000493:pharmacokinetics; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D001743:Urinary Bladder / Q000737:chemistry / Q000187:drug effects
D006146:Guanidines; D006575:Heterocyclic Compounds, 3-Ring; D015221:Potassium Channels; D011725:Pyridines; D011743:Pyrimidines; D019806:Cromakalim; C073896:N-cyano-N'-(1,1-dimethylpropyl)-N''-(3-pyridinyl)guanidine