653573-36-5Relevant academic research and scientific papers
Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units
Choi, Peter J.,Sutherland, Hamish S.,Tong, Amy S.T.,Blaser, Adrian,Franzblau, Scott G.,Cooper, Christopher B.,Lotlikar, Manisha U.,Upton, Anna M.,Guillemont, Jerome,Motte, Magali,Queguiner, Laurence,Andries, Koen,Van den Broeck, Walter,Denny, William A.,Palmer, Brian D.
supporting information, p. 5190 - 5196 (2017/11/01)
Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesised and evaluated. While there was an expected broad positive correlation between lipophilicity and anti-TB activity, the 4-pyridyl derivatives appeared to have an additional contribution to antibacterial potency. The majority of the compounds were (desirably) more polar and had higher rates of clearance than bedaquiline, and showed acceptable oral bioavailability, but there was only limited (and unpredictable) improvement in their hERG liability.
GAMMA-DIKETONES AS WNT/BETA -CATENIN SIGNALING PATHWAY ACTIVATORS
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Paragraph 1714; 1715; 1716; 1722, (2014/09/03)
The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
