Hydrogen bond interactions of a series of N-substituted TXA2 receptor antagonists.
A series of N-substituted sulphonamide based thromboxane A2 (TXA2) receptor antagonists were synthesised with the objective to explore the role of hydrogen bond donation properties in the binding of these ligands to the TXA2 receptor. Pharmacological evaluation of these compounds revealed that the binding affinity decreased significantly with the removal of the hydrogen bond donor. This indicates that a hydrogen bond donor is important for the binding of these antagonists to the TXA2 receptor.
Taylor
Dawne M
DM
Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston, SC 29425, USA.
Halushka
Perry V
PV
Meier
G Patrick
GP
D000704:Analysis of Variance; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000378:metabolism / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D006860:Hydrogen Bonding / Q000187:drug effects; D010080:Oxazoles / Q000378:metabolism / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects / Q000502:physiology; D044244:Receptors, Thromboxane A2, Prostaglandin H2 / Q000037:antagonists & inhibitors* / Q000378:metabolism
D019086:Bridged Bicyclo Compounds, Heterocyclic; D010080:Oxazoles; D044244:Receptors, Thromboxane A2, Prostaglandin H2; C078904:ifetroban