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 of some pyrimidine derivatives of expected biological ativities

A series of 4-substituted pyrimidines and fused pyrimidine ring system e.g. pyrido[2,3-d] pyrimidine were synthesized and the antitumor activity have been carried out for 8 compounds. Compound 4a also, which carries the pharmacophoric group IDA was tested for the hepatobilliary imaging effect

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]

Occurrence of superinfection in herpes simplex keratitis

In this work we study the occurrence of secondary infections in patients suffering from herpes simplex keratitis. We discuss the detection of this condition and the various common factors predisposing to superinfection

contribution to the chemical and biological evaluation of santonin from artemisia cina

Santonin from Artemisia cina exhibited a significant antimicrobial activity against Bacillus subtilis ATCC 6633, and B. Cereous. The compound may thus find potential applications as a topical bacteriostatic agent. Based on H1 and CMR3 spectroscopy, the stereochemistry of the product was established as alpha-santonin. A sensitive and precise TLC-colourimetric method is developed for its assay as a drug entity as well as in Flos. Cina

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

Pyrazole-4-carboxaldehyde from chromone-3-carboxaldehyde

It has been perviously reported that the action of hydrazine hydrate on chromones affordes the respective disubstituted pyrazoles [1]. Szabo et al.[2] reported in 1979 that hydrazine hydrate attacks 3-phenylchromone [isoflavone] at C-2 to give 3-[Q-hydroxyphenyl]- 4-phenylpyrazole. Also, the cyclization of acetophenone semicarbazone to 3-phenyl-pyrazole-4-carboxaldehyde was reported by Kira et al. [3]