BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors

被引：58
|
作者：
Vlasceanu, Alexandru [3 ]
Jessing, Mikkel [1 ,2 ]
Kilburn, John Paul [1 ,2 ]
机构：
[1] H Lundbeck & Co AS, Discovery Chem, DK-2500 Valby, Denmark
[2] H Lundbeck & Co AS, DMPK, DK-2500 Valby, Denmark
[3] Univ Copenhagen, Dept Chem, DK-2100 Copenhagen, Denmark
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 15期
关键词：
Borazaronaphthalenes; PDE10A inhibitors; Antipsychotics; HETEROAROMATIC-COMPOUNDS; ENZYME-INHIBITORS; BORON COMPOUNDS; B-N; SCHIZOPHRENIA; 2,1-BORAZARONAPHTHALENES; SUBSTITUTION; DERIVATIVES; CHEMISTRY; DISCOVERY;
D O I：
10.1016/j.bmc.2015.06.019
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The application of BN/CC isosterism is explored as a method of expanding the scope of core scaffolds in biologically active compounds. The viability of potential drug candidates incorporating BN-heteroaromatic moieties was investigated through the synthesis of BN-substituted analogs to known phosphodiesterase (PDE10A) inhibitors, namely MP10 and a selection of N-methylanilide analogs. These in some cases revealed unexpectedly potent and relatively stable derivatives, providing further support for the potential of BN-incorporation in medicinal chemistry. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4453 / 4461
页数：9
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