TY - JOUR
T1 - 3-Chloro-2-methylphenyl-substituted semicarbazones
T2 - Synthesis and anticonvulsant activity
AU - Yogeeswari, Perumal
AU - Thirumurugan, Rathinasabapathy
AU - Kavya, Ramkumar
AU - Samuel, Jayakar Selwyn
AU - Stables, James
AU - Sriram, Dharmarajan
N1 - Funding Information:
One of the authors Mr. R. Thirumurugan deeply acknowledges the Council of Scientific and Industrial Research for providing Senior Research Fellowship. The authors are grateful to Mr. A.R. Subramanian, CDRI, Lucknow for the generation of 1 H-NMR and elemental analyses data.
PY - 2004/8
Y1 - 2004/8
N2 - A series of 3-chloro-2-methylphenyl substituted semicarbazones (3-33) was synthesized and evaluated for anticonvulsant and CNS activities. After intraperitoneal injection to mice or rats, the semicarbazone derivatives were examined in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ), and subcutaneous strychnine (scSTY)-induced seizure and neurotoxicity screens. The aryl urea (1) and the semicarbazide (2) showed anticonvulsant activity in the MES and scPTZ screens with acute neurotoxicity, whereas the semicarbazone derivatives showed good anticonvulsant potency in the scSTY screen with moderate activity against MES and scPTZ screens. Compound 21 exhibited anticonvulsant potency against all the three screens with lesser neurotoxicity. Some titled compounds exhibited lesser CNS depression and neurotoxicity compared to phenytoin or carbamazepine as was evident from the CNS studies.
AB - A series of 3-chloro-2-methylphenyl substituted semicarbazones (3-33) was synthesized and evaluated for anticonvulsant and CNS activities. After intraperitoneal injection to mice or rats, the semicarbazone derivatives were examined in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ), and subcutaneous strychnine (scSTY)-induced seizure and neurotoxicity screens. The aryl urea (1) and the semicarbazide (2) showed anticonvulsant activity in the MES and scPTZ screens with acute neurotoxicity, whereas the semicarbazone derivatives showed good anticonvulsant potency in the scSTY screen with moderate activity against MES and scPTZ screens. Compound 21 exhibited anticonvulsant potency against all the three screens with lesser neurotoxicity. Some titled compounds exhibited lesser CNS depression and neurotoxicity compared to phenytoin or carbamazepine as was evident from the CNS studies.
KW - 3-Chloro-2-methyl substituted phenyl semicarbazones
KW - Anticonvulsants
KW - Aryl semicarbazones
KW - CNS depressants
UR - http://www.scopus.com/inward/record.url?scp=3242746776&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=3242746776&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2004.03.008
DO - 10.1016/j.ejmech.2004.03.008
M3 - Article
C2 - 15276306
AN - SCOPUS:3242746776
SN - 0223-5234
VL - 39
SP - 729
EP - 734
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
IS - 8
ER -