1991
DOI: 10.1021/jm00108a011
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Synthesis and biochemical evaluation of baclofen analogs locked in the baclofen solid-state conformation

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Cited by 49 publications
(24 citation statements)
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“…Rolipram exhibits varied biological activities9 and is employed in the treatment of depression 10. Baclofen11 is used as a muscle relaxant and antispastic agent 12. Pregabalin is the active ingredient in the drug Lyrica, which is used for the treatment of epilepsy, neuropathic pain, and generalized anxiety disorders 13.…”
Section: Methodsmentioning
confidence: 99%
“…Rolipram exhibits varied biological activities9 and is employed in the treatment of depression 10. Baclofen11 is used as a muscle relaxant and antispastic agent 12. Pregabalin is the active ingredient in the drug Lyrica, which is used for the treatment of epilepsy, neuropathic pain, and generalized anxiety disorders 13.…”
Section: Methodsmentioning
confidence: 99%
“…40 Baclofen, meanwhile, is a muscle relaxant currently used in the treatment of neuropathic pain. 41 The (−)-(R)-enantiomer is identified as being responsible for the biological activity; however, Baclofen is commercialized in its racemic form.…”
Section: The Synthesis Gaba Derivatives (+/−)-Phenibut (+/−)-Baclofenmentioning
confidence: 99%
“…Gabapentin (12) was obtained in 49 % yield ) and is used to treat epilepsy. [27,28] Baclofen (16), used to treat spasticity, [29] was obtained in 65 % yield (10.3 g day À1 , 48.1 mmol day À1 ), and Phenibut (10), utilized for its anxiolytic effects, [30] was obtained in 65 % yield (8.6 g day À1 , 48.1 mmol day À1 ). In summary, we have developed the first non-iterative chemical assembly system.…”
mentioning
confidence: 99%