115577-35-0Relevant academic research and scientific papers
Structure-guided optimization of small molecules inhibiting human immunodeficiency virus 1 Tat association with the human coactivator p300/CREB binding protein-associated factor
Pan, Chongfeng,Mezei, Mihaly,Mujtaba, Shiraz,Muller, Michaela,Zeng, Lei,Li, Jiaming,Wang, Zhiyong,Zhou, Ming-Ming
, p. 2285 - 2288 (2007)
Human immunodeficiency virus 1 (HIV-1) trans-activator Tat recruits the human transcriptional coactivator PCAF (p300/CREB binding protein-associated factor) to facilitate transcription of the integrated HIV-1 provirus. We report here structure-based lead optimization of small-molecule inhibitors that block selectively Tat and PCAF association in cells. Our lead optimization was guided by grand-canonical ensemble simulation of the receptor/lead complex that leads to definition of chemical modifications with improved lead affinity through displacing weakly bound water molecules at the ligand-receptor interface.
ACYLSULFONAMIDES AND PROCESSES FOR PRODUCING THE SAME
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Page/Page column 100, (2012/03/09)
The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
Compounds, Compositions and Methods
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Page/Page column 18, (2009/08/14)
Certain substituted urea derivatives modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
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Page/Page column 56, (2008/06/13)
Certain substituted urea derivatives modulate diskeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and are useful in the treatment of obesity, sarcopenia, wasting syndrome, frailty, muscle spasm, cachexia, neuromuscular diseases (e.g., amyotrophic lateral sclerosis, spinal muscular atrophy, familial or acquired myopathies or muscular dystrophies), post-surgical and post-traumatic muscle weakness, and other conditions.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
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Page/Page column 43, (2010/11/27)
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
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Page/Page column 86, (2010/11/27)
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
COMPOUNDS, COMPOSITIONS AND METHODS
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Page/Page column 44, (2010/11/28)
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Compounds, compositions and methods
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Page/Page column 31, (2008/06/13)
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Synthesis and evaluation of fluorine-substituted 1H-pyrrolo[2,3-b]pyridine derivatives for dopamine D4 receptor imaging
Oh, Seung-Jun,Lee, Kyo Chul,Lee, Sang-Yoon,Ryu, Eun Kyoung,Saji, Hideo,Choe, Yearn Seong,Chi, Dae Yoon,Kim, Sang Eun,Lee, Jeewoo,Kim, Byung-Tae
, p. 5505 - 5513 (2007/10/03)
Seven fluorine-substituted 1H-pyrrolo[2,3-b]pyridine derivatives were synthesized based on a lead ligand, 3-[[4-(4-iodophenyl)piperazin-1-yl]-methyl]- 1H-pyrrolo[2,3-b]pyridine (L-750,667) and evaluated as potential dopamine D 4 receptor imagin
(1H-imidazol-1-ylmethyl) substituted benzimidazole derivatives and use thereof in treating androgen dependent disorders
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, (2008/06/13)
Novel (1H-imidazol-1-ylmethyl) substituted benzimidazole derivatives, compositions containing the same, and methods of treating androgen dependent disorders in mammals.
