Abstract:
:A novel series of 4-arylphthalazin-1(2H)-one linked to arylpiperidines were synthesized and evaluated as MCH-R1 antagonists. The results of an extensive SAR study probing the effects of substituents on the 4-arylphthalazin-1(2H)-one C-4 aryl group led to the identification of the 4-(3,4-difluorophenyl) derivative as a highly potent MCH-R1 inhibitor with an IC(50)=1nM. However, further investigations showed that this substance has unacceptable pharmacokinetic properties including a high clearance and volume of distribution.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Lim CJ,Kim SH,Lee BH,Oh KS,Yi KYdoi
10.1016/j.bmcl.2011.10.111subject
Has Abstractpub_date
2012-01-01 00:00:00pages
427-30issue
1eissn
0960-894Xissn
1464-3405pii
S0960-894X(11)01518-6journal_volume
22pub_type
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