919366-32-8Relevant academic research and scientific papers
Highly Enantioselective Catalytic Addition of Grignard Reagents to N-Heterocyclic Acceptors
Guo, Yafei,Harutyunyan, Syuzanna R.
, p. 12950 - 12954 (2019/08/07)
General methods to prepare chiral N-heterocyclic molecular scaffolds are greatly sought after because of their significance in medicinal chemistry. Described here is the first general catalytic methodology to access a wide variety of chiral 2- and 4-substituted tetrahydro-quinolones, dihydro-4-pyridones, and piperidones with excellent yields and enantioselectivities, utilizing a single catalyst system.
NOVEL TETRAHYDROPYRIDOPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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Page/Page column 43; 44, (2018/05/24)
The present invention provides novel compounds having the general formula (I) wherein R1, R2 and Z are as described herein, compositions including the compounds and methods of using the compounds.
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors
Ye, Xiaocong M.,Konradi, Andrei W.,Smith, Jenifer,Xu, Ying-Zi,Dressen, Darren,Garofalo, Albert W.,Marugg, Jennifer,Sham, Hing L.,Truong, Anh P.,Jagodzinski, Jacek,Pleiss, Michael,Zhang, Hongbin,Goldbach, Erich,Sauer, John-Michael,Brigham, Elizabeth,Bova, Michael,Basi, Guriqbal S.
scheme or table, p. 2195 - 2199 (2010/07/05)
Discovery of a series of pyrazolopiperidine sulfonamide based γ-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy.
Catalytic enantioselective addition of dialkylzinc reagents to N-acylpyridinium salts
Fernandez-Ibanez, M. Angeles,Macia, Beatriz,Pizzuti, Maria Gabriella,Minnaard, Adriaan J.,Feringa, Ben L.
supporting information; body text, p. 9339 - 9341 (2010/03/24)
(Chemical equation presented) A pinch of salt: The first catalytic addition of dialkylzinc reagents to N-acylpyridinium salts with good yields and excellent enantioselectivities uses a copper-(S)-L complex as the catalyst. The versatility of the method is
5-(ARYLSULFONYL)-PYRAZOLOPIPERIDINES
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Page/Page column 115, (2010/11/27)
The invention provides N-cyclic sulfonamido compounds of Formula (I) wherein A, B, R1, R1a, R2, R2a, R3 and R3a are as described in the specification. Compounds of Formula (I) are useful in treating or preventing cognitive disorders, such as Alzheimer 's disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I), methods of preparing compounds of formula (I), and methods of treating cognitive disorders, such as Alzheimer's disease.
4-Pyridone derivatives as new inhibitors of bacterial enoyl-ACP reductase FabI
Kitagawa, Hideo,Kumura, Ko,Takahata, Sho,Iida, Maiko,Atsumi, Kunio
, p. 1106 - 1116 (2008/02/01)
Bacterial FAS provides essential fatty acids for use in the assembly of key cellular components. Among them, FabI is an enoyl-ACP reductase which catalyzes the final and rate-limiting step of bacterial FAS. It is a potential target for selective antibacterial action, because it shows low overall sequence homology with mammalian enzymes. Until today, various compounds have been reported as inhibitors of bacterial FabI-inhibitory compounds. To discover novel small-molecular FabI inhibitors, we initially screened our compound library for inhibitory activity toward FabI of Escherichia coli. And discovered 4-pyridone derivatives as a lead compound. Structure optimization studies yielded 4-pyridone derivatives 7n having strong FabI-inhibitory and antibacterial activities against Staphylococcus aureus. There have been no reports concerning 4-pyridone derivatives as FabI inhibitor.
