Solid phase synthesis of benzylamine-derived sulfonamide library.
Using solid phase synthesis, a library has been constructed of benzylamine-derived sulfonamides which have strong inhibitory activity against the blood coagulant thrombin. The library compounds were obtained in good yield and high purity; four of these thrombin inhibitors showed nanomolar potency (Ki 600-10 nM).
Kim
S W
SW
Biotech Research Institute, LG Chemical Ltd./Research Park Science Town, Taejon, Korea.
Hong
C Y
CY
Lee
K
K
Lee
E J
EJ
Koh
J S
JS
D000925:Anticoagulants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001596:Benzylamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D007202:Indicators and Reagents; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013917:Thrombin / Q000037:antagonists & inhibitors*
D000925:Anticoagulants; D001596:Benzylamines; D007202:Indicators and Reagents; D013449:Sulfonamides; D013917:Thrombin