RESUMO
Delta1-Tetrahydrocannabinol, which is resinous and insoluble in water and therefore difficult to study pharmacologically, can be converted to a watersoluble derivative without loss of its biological activity. This has been achieved by preparing esters bearing a nitrogen moiety with the use of carbodiimide as the condensing agent. The availability of such water-soluble derivatives will allow the evaluation of Delta1-tetrahydrocannabinol in self-administration studies in monkeys for its addiction liability potential in man. This technique of water solubilization is also applicable to other compounds of chemical and biological significance.
Assuntos
Cannabis/síntese química , Anfetamina/farmacologia , Animais , Comportamento Animal/efeitos dos fármacos , Pressão Sanguínea/efeitos dos fármacos , Depressão Química , Cães , Dronabinol/administração & dosagem , Dronabinol/síntese química , Dronabinol/farmacologia , Interações Medicamentosas , Epinefrina/farmacologia , Iminas , Raios Infravermelhos , Injeções Intravenosas , Espectroscopia de Ressonância Magnética , Atividade Motora/efeitos dos fármacos , Norepinefrina/farmacologia , Solubilidade , Análise EspectralRESUMO
As part of a general program of structural modification in beta-lactam antibiotics, we have synthesized several simple penicillins from 6-aminopenicillanic acid where the C-3 carboxyl group has been replaced by a hydroxy or an acetoxy group and the C-6 side chain has been substituted by bromine or hydrogen. Some of the compounds exhibit mild activity against the Gram-positive strain Bacillus subtilis.
Assuntos
Ácido Penicilânico , Penicilinas/síntese química , beta-Lactamas , Bactérias/efeitos dos fármacos , Sinergismo Farmacológico , Testes de Sensibilidade Microbiana , Penicilinas/farmacologiaRESUMO
Antibiotic and penicillinase inhibitor activities of various penicillin and cephalosporin analogs are reported. The compounds include C-6 penicillin and C-7 cephalosporin carbon, oxygen and sulfur analogs obtained by replacing the NH of the amide side chains with CH2, O and S, respectively. In almost all cases, analogs were considerably less active than the standard compounds (benzylpenicillin and cephalothin). However, some of the analogs act as penicillinase inhibitors.