104266-88-8Relevant articles and documents
Batrachotoxin binding site antagonists
Schow,Rossignol,Lund,Schnee
, p. 181 - 186 (1997)
The preparation and SAR of a series of batrachotoxin partial structures that antagonize binding and activity of batrachotoxin are reported in this communication.
Unprecedented 8,9′-neolignans: Enantioselective synthesis of possible stereoisomers for structural determination
Takahashi, Masato,Suzuki, Noriyuki,Ishikawa, Tsutomu,Huang, Hung-Yi,Chang, Hsun-Shuo,Chen, Ih-Sheng
, p. 2585 - 2589 (2014)
(+)-Wutaienin (3) and its C-7 methyl ether (4), isolated from Zanthoxylum wutaiense, were found to be unprecedented 8,9′-neolignans containing an (S)-2-(1,1-dimethyl-1-hydroxymethyl)-7-methoxydihydrobenzofuran skeleton. Wutaienin (3) was present in the pl
PROCESS FOR PREPARATION OF BRIVARACETAM
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Paragraph 0195, (2019/05/22)
The present invention relates to a process for the preparation of brivaracetam and salts thereof. The present invention provides process for the preparation of brivaracetam and salts thereof with high chiral purity. The present invention provides process for the preparation of brivaracetam and salts thereof wherein the amount of other stereoisomers of brivaracetam is low.
Hepatitis C replication inhibitors that target the viral NS4B protein
Miller, John F.,Chong, Pek Y.,Shotwell, J. Brad,Catalano, John G.,Tai, Vincent W.-F.,Fang, Jing,Banka, Anna L.,Roberts, Christopher D.,Youngman, Michael,Zhang, Huichang,Xiong, Zhiping,Mathis, Amanda,Pouliot, Jeffery J.,Hamatake, Robert K.,Price, Daniel J.,Seal, John W.,Stroup, Lisa L.,Creech, Katrina L.,Carballo, Luz H.,Todd, Dan,Spaltenstein, Andrew,Furst, Sylvia,Hong, Zhi,Peat, Andrew J.
supporting information, p. 2107 - 2120 (2014/04/03)
We describe the preclinical development and in vivo efficacy of a novel chemical series that inhibits hepatitis C virus replication via direct interaction with the viral nonstructural protein 4B (NS4B). Significant potency improvements were realized through isosteric modifications to our initial lead 1a. The temptation to improve antiviral activity while compromising physicochemical properties was tempered by the judicial use of ligand efficiency indices during lead optimization. In this manner, compound 1a was transformed into (+)-28a which possessed an improved antiviral profile with no increase in molecular weight and only a modest elevation in lipophilicity. Additionally, we employed a chimeric "humanized" mouse model of HCV infection to demonstrate for the first time that a small molecule with high in vitro affinity for NS4B can inhibit viral replication in vivo. This successful proof-of-concept study suggests that drugs targeting NS4B may represent a viable treatment option for curing HCV infection.