884600-82-2Relevant academic research and scientific papers
ANTIVIRAL COMPOUNDS
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Paragraph 1001, (2015/03/13)
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
Synthesis and biological evaluation of N-difluoromethyl-1,2-dihydropyrid-2-one acetic acid regioisomers: Dual Inhibitors of cyclooxygenases and 5-lipoxygenase
Yu, Gang,Praveen Rao,Chowdhury, Morshed A.,Abdellatif, Khaled R.A.,Dong, Ying,Das, Dipankar,Velázquez, Carlos A.,Suresh, Mavanur R.,Knaus, Edward E.
experimental part, p. 2168 - 2173 (2010/06/17)
A new group of acetic acid (7a-c, R1 = H), and propionic acid (7d-f, R1 = Me), regioisomers wherein a N-difluoromethyl-1,2-dihydropyrid-2-one moiety is attached via its C-3, C-4, and C-5 position was synthesized. This group of compounds exhibited a more potent inhibition, and hence selectivity, for the cyclooxygenase-2 (COX-2) relative to the COX-1 isozyme. Attachment of the N-difluoromethyl-1,2-dihydropyrid-2-one ring system to an acetic acid, or propionic acid, moiety confers potent 5-LOX inhibitory activity, that is, absent in traditional arylacetic acid NSAIDs. 2-(1-Difluoromethyl-2-oxo-1,2-dihydropyridin-5-yl)acetic acid (7c) exhibited the best combination of dual COX-2 and 5-LOX inhibitory activities. Molecular modeling (docking) studies showed that the highly electronegative CHF2 substituent present in 7c, that showed a modest selectivity for the COX-2 isozyme, is oriented within the secondary pocket (Val523) present in COX-2 similar to the sulfonamide (SO2NH2) COX-2 pharmacophore present in celecoxib, and that the N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore is oriented close to the region containing the LOX enzyme catalytic iron (His361, His366, and His545). Accordingly, the N-difluoromethyl-1,2-dihyrdopyrid-2-one moiety possesses properties suitable for the design of dual COX-2/5-LOX inhibitory drugs.
PIPERIDINES AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 40, (2010/11/08)
Compounds of formula (I), selectively inhibit production of Aβ (1-42) and hence are useful in treatment or prevention of disease assocaited with deposition of β -amyloid in the brain.
