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3.
Synthesis, Characterization and Pharmacological Screening of
Some Chalconyl Derivatives of 4-Methoxyphenyl Substituted
Semicarbazide
Hemendra Pratap Singha, Chandra Shekhar Sharmaa,
C S Chauhana, S N Pandeyab, James P.
Stablec
a
B N College of Pharmacy, Udaipur,
Rajasthan, India
b Saroj Institute of Pharmacy, Lucknow, UP, India
c Epilepsy Branch, National Institutes of Health,
Bethesda, MD, USA
Fax: (91)(294)2413182; Tel: (91)9929378331,
E mail:
hps_medicinalchemistry@yahoo.co.in
Abstract:
A series of chalconyl derivatives of 4-methoxyphenyl
substituted semicarbazide (5a-5j) was synthesized. All the
synthesized compounds were screened for their
pharmacological action in protection of seizures and
behavioral study. After intraperitoneal injection to mice or
rats, the synthesized compounds were examined in the maximal
electroshock seizure (MES), subcutaneous pentylenetetrazole
(scPTZ), and neurotoxicity test models. Compound 5e emerged
as the most active molecule exhibited anticonvulsant potency
against all the screens with lesser neurotoxicity. Some of
the title compounds exhibited lesser CNS depression and
neurotoxicity compared to phenytoin as was evident from the
CNS studies. On the bases of observed result, it can be
concluded that the substitution of –OH group in synthesized
compounds plays major role in pharmacological activity.
Key words:
Chalcones, anticonvulsant, semicarbazide.
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