41284-92-8Relevant academic research and scientific papers
Diarylthiophenes as inhibitors of the pore-forming protein perforin
Miller, Christian K.,Huttunen, Kristiina M.,Denny, William A.,Jaiswal, Jagdish K.,Ciccone, Annette,Browne, Kylie A.,Trapani, Joseph A.,Spicer, Julie A.
, p. 355 - 360 (2016/01/09)
Evolution from a furan-containing high-throughput screen (HTS) hit (1) resulted in isobenzofuran-1(3H)-one (2) as a potent inhibitor of the function of both isolated perforin protein and perforin delivered in situ by intact KHYG-1 NK cells. In the current study, structure-activity relationship (SAR) development towards a novel series of diarylthiophene analogues has continued through the use of substituted-benzene and -pyridyl moieties as bioisosteres for 2-thioxoimidazolidin-4-one (A) on a thiophene (B) -isobenzofuranone (C) scaffold. The resulting compounds were tested for their ability to inhibit perforin lytic activity in vitro. Carboxamide (23) shows a 4-fold increase(2) in lytic activity against isolated perforin and provides good rationale for continued development within this class.
PROCESSES FOR THE PREPARATION OF CITALOPRAM AND ITS INTERMEDIATE 5-AMINOPHTHALIDE
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Page/Page column 9, (2010/11/24)
The invention relates to processes for the preparation of 5-amino-2-benzofuran- l(3H)-one of Formula (I), and to the use of this compound as an intermediate for the preparation of citalopram. The invention also relates to a process for the preparation of citalopram or a salt thereof, and pharmaceutical compositions that include the citalopram or a salt thereof.
