Potential Analgesic and Anticonvulsant Bioactivity of 1,1-Disubstituted Cyclohexane Candidates

Author

PROF DR AIDA AL AZOUNI
M.N. Aboul-Enein1a, Aida El-Azzouny 1a, Y.Maklad 1b, F.Ragab 2 and
M.S.Abdel Maksoud1a
Medicinal and Pharmaceutical Chemistry Dept.1 (Pharmaceutical
Chemistry Groupa and Pharmacology Groupb), National Research
Center, Dokki, Cairo, Egypt; Pharmaceutical Chemistry Dept.,
Faculty of Pharmacy,Cairo University, Egypt2.
Email: This email address is being protected from spambots. You need JavaScript enabled to view it.

Language

English

Title

Potential Analgesic and Anticonvulsant Bioactivity    of 1,1-Disubstituted Cyclohexane Candidates

Proceeding

7th INTRACOM – 2nd ICBWI 2009

Date

24th July 2009

Place Held

PWTC, Kuala Lumpur

Abstract

Many bioactive molecules possess 1,1-disubstituted cyclohexane were moiety, such as the drugs: Valamine, Sernyl, Gevilon and Dicyclomine, which display broad spectrum psychotropic  activities varying from  psychosedatives to psychoenergizers. Accordingly, the impetus has been drawn to the synthesis of certain 1,1-disubstituted cyclohexane derivatives;namely:N-(1-(cyclohexylcarbamoyl)cyclohexyl)-N-phenylbenzamides  [1], N-(1-((cyclohexylamino)methyl)cyclohexyl)-N-phenylbenzamides [2], N-aralkyl(1-aminomethylcyclohexyl)benzenamines[3],3-cyclohexyl-2-substituted phenyl 1-phenyl 1,3-diazaspiro[4.5]decanes [4], where R = H, Cl,OCH3, NO2 ,3,4,5(OCH3)3 and X= hetero-cycloalkyl or hetero-aralkyl; with the aim to evaluate their bioactivities as  analgesics and anticonvulsants. The structures of these new candidates were confirmed by spectral analyses. The hot-plate technique was applied for the determination of the  analgesic profile. The maximal pentylenetetrazol (PTZ) induced  seizures test was performed to evaluate the anticonvulsant activity. The bioactivity of the newly synthesized compounds exhibited analgesic and anticonvulsant activities at doses from 0.08 mmol/kg to 0.11 mmol/kg, compared with tramadol (0.12 mmol/kg) as  analgesic reference; and diphenylhydantoin (0.20 mmol/Kg) as well as  valproic acid (0.24 mmol/Kg) as anticonvulsant references. The LD50 and ED50 of the most bioactive candidates were determined and statistically evaluated.

Keywords

Anticonvulsant Bioactivity  , 1,1-Disubstituted Cyclohexane

Session

Symposium 2C (ICBWI)

Topic

Biomolecule Discovery