81805-53-0Relevant academic research and scientific papers
Diverted Total Synthesis of Carolacton-Inspired Analogs Yields Three Distinct Phenotypes in Streptococcus mutans Biofilms
Solinski, Amy E.,Koval, Alexander B.,Brzozowski, Richard S.,Morrison, Kelly R.,Fraboni, Americo J.,Carson, Carrie E.,Eshraghi, Anisa R.,Zhou, Guangfeng,Quivey, Robert G.,Voelz, Vincent A.,Buttaro, Bettina A.,Wuest, William M.
, p. 7188 - 7191 (2017)
The oral microbiome is a dynamic environment inhabited by both commensals and pathogens. Among these is Streptococcus mutans, the causative agent of dental caries, the most prevalent childhood disease. Carolacton has remarkably specific activity against S. mutans, causing acid-mediated cell death during biofilm formation; however, its complex structure limits its utility. Herein, we report the diverted total synthesis and biological evaluation of a rationally designed library of simplified analogs that unveiled three unique biofilm phenotypes further validating the role of natural product synthesis in the discovery of new biological phenomena.
Galantamine-curcumin hybrids as dual-site binding acetylcholinesterase inhibitors
Atanasova, Mariyana,Atanasova, Teodora,Doytchinova, Irini,Ivanov, Stefan,Konstantinov, Spiro,Lukarski, Atanas,Philipova, Irena,Stavrakov, Georgi,Zheleva, Dimitrina,Zhivkova, Zvetanka D.
supporting information, (2020/08/06)
Galantamine (GAL) and curcumin (CU) are alkaloids used to improve symptomatically neurodegenerative conditions like Alzheimer's disease (AD). GAL acts mainly as an inhibitor of the enzyme acetylcholinesterase (AChE). CU binds to amyloid-beta (Aβ) oligomers and inhibits the formation of Aβ plaques. Here, we combine GAL core with CU fragments and design a combinatorial library of GAL-CU hybrids as dual-site binding AChE inhibitors. The designed hybrids are screened for optimal ADME properties and BBB permeability and docked on AChE. The 14 best performing compounds are synthesized and tested in vitro for neurotoxicity and anti-AChE activity. Five of them are less toxic than GAL and CU and show activities between 41 and 186 times higher than GAL.
EP4 antagonists number
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Paragraph 1157; 1170-1172, (2018/10/03)
We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
CLPX INHIBITORY COMPOUNDS FOR THE TREATMENT OF MULTI RESISTANT STAPHYLOCOCCUS AUREUS VIRULENCE AND FOR THE TREATMENT OF LEUKEMIA
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Page/Page column 26, (2018/07/26)
The present invention relates to antibiotic compounds and their use as ClpX inhibitors and in the treatment of bacterial infections, such as infections with multi-resistant Staphylococcus aureas, and in the treatment of leukemia. The present invention fur
A Chemical Disruptor of the ClpX Chaperone Complex Attenuates the Virulence of Multidrug-Resistant Staphylococcus aureus
Fetzer, Christian,Korotkov, Vadim S.,Th?nert, Robert,Lee, Kyu Myung,Neuenschwander, Martin,von Kries, Jens Peter,Medina, Eva,Sieber, Stephan A.
supporting information, p. 15746 - 15750 (2017/10/20)
The Staphylococcus aureus ClpXP protease is an important regulator of cell homeostasis and virulence. We utilized a high-throughput screen against the ClpXP complex and identified a specific inhibitor of the ClpX chaperone that disrupts its oligomeric sta
6-AMINO-QUINOLINE-3-CARBONITRILS AS COT MODULATORS
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Page/Page column 104; 105, (2017/01/26)
The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
Novel HIV reverse transcriptase inhibitors
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Page/Page column 70-71, (2008/06/13)
The invention is related to compounds of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
NOVEL HETEROARYL DERIVATIVE
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, (2008/06/13)
A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.
NOVEL HETEROARYL DERIVATIVE
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Page/Page column 100-101, (2008/06/13)
A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. (1) wherein: the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl, etc.
Picolinyl group as an efficient alcohol protecting group: Cleavage with Zn(OAc)2·2H2O under a neutral condition
Ju, Yuel Baek,Shin, Yong-Joo,Heung, Bae Jeon,Kwan, Soo Kim
, p. 5143 - 5147 (2007/10/03)
As an efficient alcohol protecting group, picolinates (Pic), prepared from the corresponding alcohols using commercial picolinoyl chloride, are readily cleaved by Zn(OAc)2 or Cu(OAc)2, even in the presence of other common alcohol protecting groups. Moreover, the picolinyl group at C-2 position in carbohydrates can be selectively cleaved to give methyl 4,6-O-benzylidene-3-O-picolinyl-α-d-glucopyranoside and 3-O-picolinyl methyl-4,6-O-benzylidene-α-d-galactopyranoside in good yields.
