63404-84-2Relevant articles and documents
N- vs O-alkylation in 2(1H)-quinolinone derivatives
Guo, Zhao-Xia,Cammidge, Andrew N.,McKillop, Alexander,Horwell, David C.
, p. 6999 - 7002 (1999)
N- vs O-alkylation reactions of 8-benzyloxy-2(1H)-quinolinone have been investigated using both classical and phase transfer conditions. The influence of reaction solvents/conditions was found to have a dramatic effect on selectivity, with opposite trends
PRMT5 INHIBITORS AND USES THEREOF
-
Paragraph 0442-0443, (2019/04/05)
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for β-Arrestin-Biased D2R Agonists
M?nnel, Barbara,Dengler, Daniela,Shonberg, Jeremy,Hübner, Harald,M?ller, Dorothee,Gmeiner, Peter
supporting information, p. 4693 - 4713 (2017/06/13)
By means of a formal structural hybridization of the antipsychotic drug aripiprazole and the heterocyclic catecholamine surrogates present in the β2-adrenoceptor agonists procaterol and BI-167107 (4), we designed and synthesized a collection of novel hydroxy-substituted heteroarylpiperazines and heteroarylhomopiperazines with high dopamine D2 receptor (D2R) affinity. In contrast to the weak agonistic behavior of aripiprazole, these ligands are capable of effectively mimicking those interactions of dopamine and the D2R that are crucial for an active state, leading to the recruitment of β-arrestin-2. Interestingly, some ligands show considerably lower intrinsic activity in guanine nucleotide exchange experiments at D2R and consequently represent biased agonists favoring β-arrestin-2 recruitment over canonical G protein activation. The ligands' agonistic properties are substantially driven by the presence of an endocyclic H-bond donor.