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J Med Chem ; 63(14): 7857-7866, 2020 07 23.
Artigo em Inglês | MEDLINE | ID: mdl-32588620

RESUMO

In this work, a series of water-soluble propofol prodrugs were synthesized, and their propofol release rate and pharmacodynamic characteristics were measured. We found that inserting glycolic acid as a linker between propofol and the cyclic amino acid accelerated the release of propofol from prodrugs into the plasma while preserving its safety. In animal experiments, prodrugs (3e, 3g, and 3j) were significantly better than fospropofol (the only water-soluble propofol prodrug that has been used clinically) in terms of safety, onset, and duration time of anesthesia. Their molar dose, onset time, and anesthesia duration time were comparable to those of propofol, helping to maintain the clinical benefits of propofol. The experimental results showed the potential of such compounds as water-soluble prodrugs of propofol.


Assuntos
Aminoácidos Cíclicos/farmacologia , Anestésicos Intravenosos/farmacologia , Glicolatos/farmacologia , Pró-Fármacos/farmacologia , Propofol/farmacologia , Aminoácidos Cíclicos/síntese química , Anestésicos Intravenosos/síntese química , Animais , Desenho de Fármacos , Glicolatos/síntese química , Masculino , Camundongos , Pró-Fármacos/síntese química , Propofol/síntese química , Solubilidade , Água/química
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