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]

Benificial effect of administration of green tea with celecoxib

This study was conducted on rats to investigate the anti-inflammatory and ulcerogenic effects of four-day administration of green tea and its beneficial co-administration with celecoxib, a COX-2 inhibitor. The oral administration of green tea [20 and 40 mg/kg] exhibited a significant anti-inflammatory activity in carrageenan induced paw edema model; however, this effect was less than that evoked by celecoxib [25 mg/kg] which produced an anti-inflammatory activity superior to that of indomethacin [5 mg/kg] as a reference drug. The administration of celecoxib [25 mg/kg] with green tea [20 or 40 mg/kg] enhanced its anti-inflammatory activity. Green tea at both doses significantly inhibited plasma prostaglandin E2 [PGE2] level, but to an extent less than that produced by either celecoxib or indomethacin. The combined administration of green tea and celecoxib normalized plasma PGQ level. Green tea [20 and 40 mg/kg] exhibited a very weak ulcerogenicity [UI is 1.71 and 3.28, respectively] compared with that of celecoxib [UI is 10.43], which exhibited an ulcerogenic effect much less than that of indomethacin [UI is 21.6]. The combined administration of green tea [20 and 40 mg/kg] and celecoxib reduced the ulcerogenicity of celecoxib [UI is 8.37 and 8.84, respectively]. Moreover, serum urea nitrogen and creatinine levels were significantly increased after treatment with celecoxib, but to a less degree than that of indomethacin. The combined administration of green tea [20 and 40 mg/kg] significantly antagonized this effect and normalized urea nitrogen and creatinine levels

Electrical properties of some vitamins with respect to their biological effects

The dielectric constant, epsilon', and the dielectric loss, epsilon", for vitamins B1, B6, C and D2, within the frequency range 105 to 107 Hz and the temperature range 20 to 50 degrees were measured. The dispersion absorption bands were interpreted, and the relaxation times were calculated from the frequencies corresponding to maximum energy. The activation enthalpy and the entropy change of dielectric relaxation were calculated from the chemical rate process equation, and all the results were correlated and interpreted with regard to vitamin structures. Chemical, biochemical and biological effects of investigated vitamins are discussed and correlated with respect to their electrical properties