Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2
Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) continues to spread worldwide, with 25 million confirmed cases and 800 thousand deaths. Effective treatments to target SARS-CoV-2 are urgently needed. In the present study, we have identified a
Shin, Young Sup,Lee, Jun Young,Noh, Soojin,Kwak, Yoonna,Jeon, Sangeun,Kwon, Sunoh,Jin, Young-hee,Jang, Min Seong,Kim, Seungtaek,Song, Jong Hwan,Kim, Hyoung Rae,Park, Chul Min
supporting information
(2020/11/13)
DERIVATIVES OF BENZOTHIAZINES, PREPARATION THEREOF AND APPLICATION THEREOF AS DRUGS
The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11β-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R'4 represent a hydrogen.
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Page/Page column 38-39
(2010/09/18)
Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl} benzamide analogs as potent Kv1.3 ion channel blockers. Part 2
We report the synthesis and in vitro activity of a series of novel substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl} benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several demonstrated similar po
Haffner, Curt D.,Thomson, Stephen A.,Guo, Yu,Petrov, Kimberly,Larkin, Andrew,Banker, Pierette,Schaaf, Gregory,Dickerson, Scott,Gobel, Jeff,Gillie, Dan,Condreay, J. Patrick,Poole, Chuck,Carpenter, Tiffany,Ulrich, John
scheme or table
p. 6989 - 6992
(2011/02/23)
HIV INTEGRASE INHIBITORS
The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
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Page/Page column 12
(2010/11/27)
HIV integrase inhibitors
The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
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Page/Page column 16
(2010/11/27)
BICYCLIC HETEROCYCLES AS HIV INTEGRASE INHIBITORS
The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
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Page/Page column 115
(2010/11/27)
Bicyclic heterocycles as HIV integrase inhibitors
The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
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Page/Page column 54
(2008/06/13)
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