Ontology highlight
ABSTRACT:
SUBMITTER: Sidhu PS
PROVIDER: S-EPMC3717983 | biostudies-literature | 2013 Jun
REPOSITORIES: biostudies-literature
Sidhu Preetpal Singh PS Abdel Aziz May H MH Sarkar Aurijit A Mehta Akul Y AY Zhou Qibing Q Desai Umesh R UR
Journal of medicinal chemistry 20130613 12
We recently designed a group of novel exosite-2-directed sulfated, small, allosteric inhibitors of thrombin. To develop more potent inhibitors, monosulfated benzofuran tri- and tetrameric homologues of the parent designed dimers were synthesized in seven to eight steps and found to exhibit a wide range of potencies. Among these, trimer 9a was found to be nearly 10-fold more potent than the first generation molecules. Michaelis-Menten studies indicated an allosteric mechanism of inhibition. Compe ...[more]