548798-25-0Relevant articles and documents
Reduction of bis(5-alkyl-2-furyl)(2-nitroaryl)methane with aqueous titanium trichloride solution
Deng, Wei,Li, Dong-Kun,Tan, Jing-Yi,Xu, Zheng-Yang
supporting information, (2021/09/29)
In this article, we introduces a new method for the synthesis of substituted indole by reductive recyclization of bis(5-alkyl-2-furyl)(2-nitroaryl)methane. Bis(5-alkyl-2-furyl)(2-nitroaryl)methane undergo reduction to provide indole or aniline. In the pro
4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1
Chen, Grace Shiahuy,Chern, Ji-Wang,Hsieh, Chen-En,Hung, Pei-Yun,Jagtap, Ajit Dhananjay,Kondekar, Nagendra B.,Yang, Chia-Ron
, (2020/01/11)
Herein, we report the identification, design, and synthesis of a series of 4-substituted 2-amino-3,4-dihydroquinazolines with hairpin turn side chains as novel inhibitors of BACE-1. The dihydroquinazoline derivatives were rationally designed by modifying the amide group and relocating the α -hydrophobic substituent on the hairpin turn side chain of lead compound 2 to the C4-position on the 3,4-dihydroquinazoline scaffold to facilitate interactions with the S1, S2 and S1′ subsites of BACE-1. Among these derivatives, two compounds exhibited potent BACE-1 inhibitory activity: 4-methyl-substituted (22a, BACE-1 CFA IC50 = 0.38 μM; BACE-1 WCA IC50 = 0.14 μM) and 4-cyclohexylmethyl-substituted (22b, BACE-1 CFA IC50 = 0.49 μM; BACE-1 WCA IC50 = 0.14 μM) 2-amino-3,4-dihydroquinazoline, each bearing a side chain of N-cyclohexyl-N-((1-methyl-1H-pyrazol-4-yl)methyl amide. The results suggest that the structural modifications maintain the hairpin turn topology similar to that of compound 2 and provide an additional interaction with the S2 subsite.
Radiolabelled MMP selective compounds
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Page/Page column 10; 13-14, (2009/12/05)
The invention is directed to radiolabelled MMP selective compounds, a processes for the preparation thereof, and uses thereof. The derivatives of the invention have formula (I) wherein Y represents O, CH2, (CH2)2, S, NH, o
2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (β-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead
Baxter, Ellen W.,Conway, Kelly A.,Kennis, Ludo,Bischoff, Fran?ois,Mercken, Marc H.,De Winter, Hans L.,Reynolds, Charles H.,Tounge, Brett A.,Luo, Chi,Scott, Malcolm K.,Huang, Yifang,Braeken, Mirielle,Pieters, Serge M. A.,Berthelot, Didier J. C.,Masure, Stefan,Bruinzeel, Wouter D.,Jordan, Alfonzo D.,Parker, Michael H.,Boyd, Robert E.,Qu, Junya,Alexander, Richard S.,Brenneman, Douglas E.,Reitz, Allen B.
, p. 4261 - 4264 (2008/03/11)
A new aspartic protease inhibitory chemotype bearing a 2-amino-3,4- dihydroquinazoline ring was identified by high-throughput screening for the inhibition of BACE-1. X-ray crystallography revealed that the exocyclic amino group participated in a hydrogen
2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF B-SECRETASE (BACE)
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Page/Page column 144-145, (2010/10/20)
The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibi
NOVEL 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
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Page/Page column 144-145, (2010/10/20)
The present invention is directed to novel 2-amino-3, 4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of P-secretase, also known as n-site cleaving enzyme and BACE.