84547-61-5Relevant academic research and scientific papers
Addressing the Metabolic Stability of Antituberculars through Machine Learning
Stratton, Thomas P.,Perryman, Alexander L.,Vilchèze, Catherine,Russo, Riccardo,Li, Shao-Gang,Patel, Jimmy S.,Singleton, Eric,Ekins, Sean,Connell, Nancy,Jacobs, William R.,Freundlich, Joel S.
supporting information, p. 1099 - 1104 (2017/10/18)
We present the first prospective application of our mouse liver microsomal (MLM) stability Bayesian model. CD117, an antitubercular thienopyrimidine tool compound that suffers from metabolic instability (MLM t1/2 1/2 values greater than or equal to 60 min. It is noteworthy that whole-cell efficacy and lack of relative mammalian cell cytotoxicity could not be predicted simultaneously. These results support the utility of our new MLM stability model in chemical tool and drug discovery optimization efforts.
TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 64, (2016/03/22)
Provided are quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1, R 2, L, X 1, X 2, and X 3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Paragraph 0175, (2014/05/24)
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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, (2014/10/04)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
PYRAZOLE DERIVATIVES AS P2X7 MODULATORS
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Page/Page column 30, (2008/12/08)
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 represents C1-6 alkyl or C3-6 cycloalkyl, either of which is optionally substituted with 1, 2 or 3 ha
Orally active CCR5 antagonists as anti-HIV-1 agents. Part 3: Synthesis and biological activities of 1-benzazepine derivatives containing a sulfoxide moiety
Seto, Masaki,Miyamoto, Naoki,Aikawa, Katsuji,Aramaki, Yoshio,Kanzaki, Naoyuki,Iizawa, Yuji,Baba, Masanori,Shiraishi, Mitsuru
, p. 363 - 386 (2007/10/03)
In order to develop orally active CCR5 antagonists, 1-propyl- or 1-isobutyl-1-benzazepine derivatives containing a sulfoxide moiety have been designed, synthesized, and evaluated for their biological activities. Sulfoxide compounds containing a 2-pyridyl
BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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Page 221-222, (2010/02/06)
The present invention provides a novel benzazepine derivative represented by formula : wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.
Synthesis and antibacterial activity of novel 4-pyrrolidinylthio carbapenems. Part IV. 2-Alkyl substituents containing cationic heteroaromatics linked via a C-C bond
Azami, Hidenori,Barrett, David,Tanaka, Akira,Sasaki, Hiroshi,Matsuda, Keiji,Sakurai, Minoru,Terasawa, Takeshi,Shirai, Fumiyuki,Chiba, Toshiyuki,Matsumoto, Yoshimi,Tawara, Shuichi
, p. 961 - 982 (2007/10/03)
The synthesis and biological activity of a novel series of 2-alkyl-4-pyrrolidinylthio-β-methylcarbapenems containing a variety of cationic heteroaromatic substituents linked via a C-C bond is described. As a result of these studies, we selected FR21818 (1
Studies on β-lactam antibiotics, synthesis and antibacterial activity of novel 1β-methylcarbapenems related to FR21818: 5-membered ring analogs
Azami, Hidenori,Barrett, David,Tanaka, Akira,Sasaki, Hiroshi,Matsuda, Keiji,Sakurai, Minora,Matsumoto, Yoshimi,Tawara, Shuichi,Chiba, Toshiyuki,Sakane, Kazuo
, p. 1409 - 1414 (2007/10/03)
The synthesis and biological activity of the novel series of 1β-methylcarbapenems 1 are described. Most compounds displayed extremely potent antibacterial activity and high renal DHP-I stability. The best compound in this series, FR21818 (1a) displayed ex
