128133-59-5Relevant academic research and scientific papers
Synthesis and preliminary evaluation of 4-hydroxy-6-(3-[11C]methoxyphenethyl)pyridazin-3(2H)-one, a 11C-labeled D-amino acid oxidase (DAAO) inhibitor for PET imaging
Chen, Zhen,Deng, Xiaoyun,Fujinaga, Masayuki,Hatori, Akiko,Hu, Kuan,Josephson, Lee,Kumata, Katsushi,Liang, Steven,Mori, Wakana,Murtas, Giulia,Pollegioni, Loredano,Rong, Jian,Shao, Tuo,Shao, Yihan,Van, Richard,Wey, Hsiao-Ying,Yu, Qingzhen,Zhang, Ming-Rong,Zhang, Yiding
, (2020)
Selective DAAO inhibitors have demonstrated promising therapeutic effects in clinical studies, including clinically alleviating symptoms of schizophrenic patients and ameliorating cognitive function in Alzheimer's patients with early phase. Herein we repo
BTK Inhibitors and uses thereof
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, (2020/05/02)
The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
SO2F2-Mediated Oxidative Dehydrogenation and Dehydration of Alcohols to Alkynes
Zha, Gao-Feng,Fang, Wan-Yin,Li, You-Gui,Leng, Jing,Chen, Xing,Qin, Hua-Li
supporting information, p. 17666 - 17673 (2019/01/04)
Direct synthesis of alkynes from inexpensive, abundant alcohols was achieved in high yields (greater than 40 examples, up to 95% yield) through a SO2F2-promoted dehydration and dehydrogenation process. This straightforward transformation of sp3-sp3 (C-C) bonds to sp-sp (C=C) bonds requires only inexpensive and readily available reagents (no transition metals) under mild conditions. The crude alkynes are sufficiently free of impurities to permit direct use in further transformations, as illustrated by regioselective Huisgen alkyne-azide cycloaddition reactions with PhN3 to give 1,4-substituted 1,2,3-traiazoles (16 examples, up to 92% yield) and Sonogashira couplings (10 examples, up to 77% yield).
Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds
Sarasamkan, Jiradanai,Scheunemann, Matthias,Apaijai, Nattayaporn,Palee, Siripong,Parichatikanond, Warisara,Arunrungvichian, Kuntarat,Fischer, Steffen,Chattipakorn, Siriporn,Deuther-Conrad, Winnie,Schüürmann, Gerrit,Brust, Peter,Vajragupta, Opa
supporting information, p. 890 - 895 (2016/10/25)
The novel quinuclidine anti-1,2,3-triazole derivatives T1-T6 were designed based on the structure of QND8. The binding studies revealed that the stereochemistry at the C3 position of the quinuclidine scaffold plays an important role in the nAChR subtype selectivity. Whereas the (R)-enantiomers are selective to α7 over α4β2 (by factors of 44-225) and to a smaller degree over α3β4 (3-33), their (S)-counterparts prefer α3β4 over α4β2 (62-237) as well as over α7 (5-294). The (R)-derivatives were highly selective to α7 over α3β4 subtypes compared to (RS)- and (R)-QND8. The (S)-enantiomers are 5-10 times more selective to α4β2 than their (R) forms. The overall strongest affinity is observed for the (S)-enantiomer binding to α3β4 (Ki, 2.25-19.5 nM) followed by their (R)-counterpart binding to α7 (Ki, 22.5-117 nM), with a significantly weaker (S)-enantiomer binding to α4β2 (Ki, 414-1980 nM) still above the very weak respective (R)-analogue affinity (Ki, 5059-10436 nM).
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. A potent and selective series for further drug development
Lilienkampf, Annamaria,Pieroni, Marco,Wan, Baojie,Wang, Yuehong,Franzblau, Scott G.,Kozikowski, Alan P.
supporting information; experimental part, p. 678 - 688 (2010/07/06)
New antituberculosis (anti-TB) drugs are urgently needed to shorten the 6-12month treatment regimen and especially to battle drug-resistant Mycobacterium tuberculosis (Mtb) strains. In this study, we have continued our efforts to develop isoxazole-based a
Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for beta-secretase modulation
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Page/Page column 29, (2008/06/13)
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles
Calcium uptake inhibitors
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, (2008/06/13)
This invention relates to 1-phenyl-3-phenyl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
