Estery aminopyrazinkarboxylové kyseliny jako potenciální antimykobakteriální léčiva

Byla připravena série sedmi esterů 3-aminopyrazin-2-karboxylové kyseliny jako potenciální antimykobakteriální léčiva. Syntéza probíhala s využitím mikrovlnného reaktoru CEM Discover s autosamplerem Explorer 24, který sloužil k urychlení reakce. Připravené produkty byly charakterizovány pomocí IČ, ¹H NMR, ¹³C NMR spekter, elementární analýzy a teplotou tání. Byly vypočteny hodnoty log P a ClogP. U nasyntetizovaných látek byla hodnocena in vitro antimykobakteriální aktivita. Nejúčinnější sloučeninou byl hexyl-3-aminopyrazin-2-karboxylát (7), jehož antimykobakteriální aktivita (MIC) proti M. tuberculosis H37Rv byla 6.25 μg/mL.

Klíčová slova:
proléčiva – estery pyrazinkarboxylové kyseliny – výpočet lipofility – in vitro antimykobakteriální aktivita.

Autoři: Martin Doležal; Jana Vobicková; Barbora Servusová; Pavla Paterová
Působiště autorů: Department of Clinical Microbiology, University Hospital, Hradec Králové, Czech Republic ; Charles University in Prague, Faculty of Pharmacy, Department of Pharmaceutical Chemistry and Drug Control
Vyšlo v časopise: Čes. slov. Farm., 2013; 62, 84-88
Kategorie: Původní práce

Souhrn

Klíčová slova:
proléčiva – estery pyrazinkarboxylové kyseliny – výpočet lipofility – in vitro antimykobakteriální aktivita.

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