Abstract:
:A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. Optimization of 1 by introduction of a hydrophilic substituent into the thioether part resulted in identification of potent ORL1 antagonists with high selectivity over binding affinity for hERG and other opioid receptors.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Kobayashi K,Kato T,Yamamoto I,Shimizu A,Mizutani S,Asai M,Kawamoto H,Ito S,Yoshizumi T,Hirayama M,Ozaki S,Ohta H,Okamoto Odoi
10.1016/j.bmcl.2009.04.022subject
Has Abstractpub_date
2009-06-01 00:00:00pages
3100-3issue
11eissn
0960-894Xissn
1464-3405pii
S0960-894X(09)00488-0journal_volume
19pub_type
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