- Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors
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EPAC proteins are therapeutic targets for the potential treatment of cardiac hypertrophy and cancer metastasis. Several laboratories use a tetrahydroquinoline analog, CE3F4, to dissect the role of EPAC1 in various disease states. Here, we report SAR studies with tetrahydroquinoline analogs that explore various functional groups. The most potent EPAC inhibitor 12a exists as a mixture of inseparable E (major) and Z (minor) rotamers. The rotation about the N-formyl group indeed impacts the activity against EPAC.
- Sonawane, Yogesh A.,Zhu, Yingmin,Garrison, Jered C.,Ezell, Edward L.,Zahid, Muhammad,Cheng, Xiaodong,Natarajan, Amarnath
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supporting information
p. 1183 - 1187
(2017/11/15)
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- BENZOXAZINONE DERIVATIVES, PREPARATION THEREOF AND USES IN THE TREATMENT OF CNS AND OTHER DISORDERS
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:wherein A, R1, R2, R3, p, q, A and X are as defined in the specification. Preparation of the compounds and uses in the treatment of CNS and other disorders, including dep
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- Process for 6,7-dihydro-5,8-dimethyl-9-fluoro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid
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A process for preparing 6,7-dihydro-9-fluoro-5,8-dimethyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, an antimicrobial, using 6-fluoro-2-methylquinoline as a starting material. A synthetic intermediate is also disclosed.
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- Antimicrobial 8-alkoxy-6,7-dihydro-5-methyl-9-fluoro-1-oxo-1H,5H-benzo[ij]qu
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The 8-alkoxy-6,7-dihydro-5-methyl-9-fluoro-1-oxo- 1H,5H-benzo[ij]quinolizine-2-carboxylic acids are disclosed as potent antimicrobial agents with a broad spectrum of activity. Esters, acyl chlorides, amides, alkylaminoalkyl ester salts and pharmaceutically acceptable carboxylate salts are also disclosed. Methods of using these compounds, pharmaceutical compositions comprising these compounds and synthetic intermediates for preparing these compounds are also described.
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