Synthesis of certain 2-endo-dimethylaminomethyl-1,7,7 - trimethylbicyclo [2.2.1] heptan-2-exo-ol esters with antiinflammatory, anticonvulsant and hypoglycaemic effects

The synthesis of certain esters of 2-endo-dimethylaminomethyl-1,7,7- trimethylbicyclo [2.2.1] heptan-2-exo-ol [4a-g] has been performed. These compounds have been evaluated for their antiinflammatory, anticonvulsant and hypoglycaemic potential as well as their ulcerogenic effect. Compounds 4-benzoic acid 2-endo-dimethyfamlnomethyl-1,7,7-trimethylbicyclo [2.2.1] hept-2-exo-yl ester [4a]; 4-bromo-benzoic acid 2-endo-dimethylaminomethyl-l,7,7-trimethylbicyclo [2.2.1] hept-2-exo-yl ester [4c]; 3,4,5 trimethoxybenzoic acid 2-endo-dimethylaminomethyl-l,7,7-trimethylbicycio [2.2.1] hept-2-exo-yl ester [4e] and 4-methoxybenzoic acid 2-endo-dimethylaminomethyl-1,7,7-trimethylbicyclo [2.2.1] hept-2-exo-yl ester [4d] displayed the most potent anti-inflammatory activity, besides being devoid of ulcerogenicity. Moreover, Compounds 4e and 4d exhibited the highest anticonvulsant effect. Compounds 4d and 4a showed almost equal hypoglycaemic properties, but still less than gliclazide as a reference drug

Synthesis and biological evaluation of certain N-Benzyl-N [1-piperidin-1-yl-cyclohexyl methyl]-benzamides

A series of N-benzyl-N-[1-piperidin- l-yl cyclohexylmethyl] benzamides 5a-i has been synthesized and evaluated for their analgesic, anticonvulsant and antihistaminic activities. The highest peripheral analgesic potency was achieved with compound 5f [20mg/kg] in respect with acetylsalicylic acid [200mg/kg]. Compound 5g exhibited the highest anticonvulsant property among the series and 10 fold as active as diphenylhydantoin soduim [DPH.Na] used as reference drug since it showed 100% lrotection at a dose level of 5 mg/kg while the reference drug gave 100% protection at 50 mg/kg. Moreover, the highest inhibitory activity on plasma histamine level was displayed with compound 5d [62%,3Omg/kg] compared with chlorpheniramine maleate [50%,0.3 mg/kg]

facile synthesis of 2', 3', 7', 8',-tetrahydro-7'-aryl and aralkylspiro [cycloalkyl-1,6' [5'H] -imidazo [1,2-a] pyrazine] -5-'ones A heterocycle of potential analgesic profile

The condensation of 1-[n-aryl and aralkyl-N- cyanomethyl]-aminocycloalkane-carboxamides 4 with ethylenediamine yielded unexpectedly the heterocycle 2', 3', 7', 8'-tetrahydro-7'-aryl one [1]. A series of 1 has been prepared and screened for their analgesic activity. All the compounds exhibited analgesic potency comparable with that of morphine in the hot-plate test