DEVELOPMENT AND SYNTHESIS OF AMINO ACID DERIVATIVES OF N-METHYL ANALOGUE OF PROCAINE AND BENZOCAINE BASED ON PHARMACOPHORE FUSION STRATEGY
Abstract and keywords
Abstract (English):
Razrabotan racional'nyy sposob sinteza aminokislotnyh proizvodnyh N-metil'nogo analoga prokaina i benzokaina s ispol'zovaniem N,N-karbonildiimidazol'nogo metoda v rastvore. S ispol'zovaniem kompleksa programmnogo obespecheniya PASS bylo vypolneno prognozirovanie biologicheskoy aktivnosti serii gibridnyh soedineniy, poluchennyh sliyaniem aminoefirnyh i aminoanilidnyh anestetikov. Bylo pokazano, chto pri sliyanii farmokoforov u vseh gibridnyh soedineniy nablyudaetsya potencial'noe otsutstvie znachimoy gepatotoksichnosti s povysheniem urovnya srednesmertel'noy dozy kak pri vnutri-bryushinnom, tak i pri podkozhnom sposobah vvedeniya. Sintezirovannye soedineniya predstavlyayut interes v kachestve potencial'nyh terapevticheskih agentov s mestnoanesteziruyuschey aktivnost'yu v sochetanii s nizkoy toksichnost'yu.

Keywords:
benzokain, Boc-α-aminokisloty, N,N-karbonildiimidazol, 4-aminobenzoynaya kislota, mestnye anestetiki
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