Synthesis, structure-activity relationships of some aromatic oxybutynyl amine derivatives

Manas T. Omyrzakov, Д.К. Кияшев, Anuarbekova Indira Niayzbekkyzy, Kazbek B. Yerzhanov, AE Mostafa, Ahmed M. Metwaly, Samir Anis Ross

2014

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DOI 10.1055/s-0034-1382635

Data confidence 70 medium

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Abstract

Twelve aromatic oxybutynyl amine derivatives (1 – 12) were synthesized via Mannich reaction. All synthesized compounds were tested for their antimalarial, antibacterial and antifungal activities. Compounds 1, 6 and 7 showed antimalarial activity against chloroquine-sensitive (D6) Plasmodium falciparum protozoan with an IC 50 value of 0.65, 1.64 and 2.98 µg/mL and against chloroquine-resistant (W2) Plasmodium falciparum protozoan with an IC 50 value of 0.25, 0.77 and 1.13 µg/mL respectively. Compounds 1 and 3 showed antimicrobial activity against Cryptococcus neoformans with an IC 50 value of 0.95 and 2.41 µg/mL, against Staphylococcus aureus with an IC 50 value of 1.03 and 1.08 µg/mL, against Methicillin-resistant Staphylococcus aureus with an IC 50 value of 1.16 and 0.86 µg/mL and against Mycobacterium intracellulare with an IC 50 value of < 0.8 and 2.19 µg/mL respectively. Fig. 1