COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations with other pharmace
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Page/Page column 74
(2017/07/19)
Design and synthesis of certain substituted cycloalkanecarboxamides structurally related to safinamide with anticonvulsant potential
A series of novel safinamide derivatives were synthesized and biologically evaluated for their anticonvulsant activity against maximal electroshock seizure assay and subcutaneous pentylenetetrazole (s.c. PTZ) screening test. Compound 13b is the most active derivative in s.c. PTZ screening test with an ED50 value lower than that of safinamide by about tenfold. A molecular modeling study, including fitting to sodium channel blockers 3D-pharmacophore model and docking into a branched-chain aminotransferase enzyme active site were consistent with the in vivo results.
Aboul-Enein, Mohamed N.,El-Azzouny, Aida A.,Maklad, Yousreya A.,Ismail, Mohamed A.,Ismail, Nasser S. M.,Hassan, Rasha M.
p. 3767 - 3791
(2015/06/08)
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