187963-92-4Relevant academic research and scientific papers
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice
Purkey, Hans E.,Robarge, Kirk,Chen, Jinhua,Chen, Zhongguo,Corson, Laura B.,Ding, Charles Z.,Dipasquale, Antonio G.,Dragovich, Peter S.,Eigenbrot, Charles,Evangelista, Marie,Fauber, Benjamin P.,Gao, Zhenting,Ge, Hongxiu,Hitz, Anna,Ho, Qunh,Labadie, Sharada S.,Lai, Kwong Wah,Liu, Wenfeng,Liu, Yajing,Li, Chiho,Ma, Shuguang,Malek, Shiva,O'Brien, Thomas,Pang, Jodie,Peterson, David,Salphati, Laurent,Sideris, Steve,Ultsch, Mark,Wei, Binqing,Yen, Ivana,Yue, Qin,Zhang, Huihui,Zhou, Aihe
supporting information, p. 896 - 901 (2016/10/22)
A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with 50 in a MiaPaca2 cell line. Optimization of the series led to 29, a potent cell active molecule (MiaPaca2 IC50 = 0.67 μM) that also possessed good exposure when dosed orally to mice.
PIPERIDINE-DIONE DERIVATIVES
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Page/Page column 98; 99, (2015/11/10)
The invention provides novel compounds having the general formula (I) and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.
METHOD OF CONTROLLING LACTATE PRODUCTION WITH PIPERDINE-DIONE DERIVATIVES
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Page/Page column 79, (2015/11/10)
The invention provides novel compounds having the general formula: and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.
Preparation and coupling reaction of thienylmanganese bromides
Kim, Seung-Hoi,Rieke, Reuben D.
, p. 993 - 996 (2007/10/03)
3-Thienylmanganese bromide, 3-bromo-4-thienylmanganese bromide and 4-substituted 3-thienylmanganese bromides were prepared from the reactions of Rieke manganese with 3-bromothiophene, 3,4-dibromothiophene and 4-substituted 3-bromothiophenes, respectively. The resulting thienylmanganese bromides underwent cross-coupling reactions under mild reaction conditions.
Direct Preparation of 3-Thienyl Organometallic Reagents: 3-Thienylzinc and 3-Thienylmagnesium Iodides and 3-Thienylmanganese Bromides and Their Coupling Reactions
Rieke, Reuben D.,Kim, Seung-Hoi,Wu, Xiaoming
, p. 6921 - 6927 (2007/10/03)
3-Thienylzinc and 3-thienylmagnesium iodides can be generated from the direct oxidative addition of Rieke zinc and magnesium to 3-iodothiophene, respectively. The direct preparation of 3-thienylmanganese bromides from the reaction of Rieke manganese with 3-bromothiophene and 3,4-dibromothiophene is also performed. These 3-thienyl organometallic reagents have been found to be regiostable intermediates and undergo coupling reactions with a variety of versatile electrophiles such as acid chlorides, aryl iodides, aldehydes, and disulfide.
