Synthesis of New β-Lactams Bearing the Biologically Important Morpholine Ring and POM Analyses of Their Antimicrobial and Antimalarial Activities

Oxana B Kazakova (1) , Jean Michel Brunel (2) , Elmira F Khusnutdinova (1) , Sophie Negrel (2) , Gulnara V Giniyatullina (1) , Tatyana V Lopatina (1) , Anastasiya V Petrova (1)

1 Russian Academy of Sciences (Ufa)
2 MCT - Membranes et cibles thérapeutiques

Some new β-lactams bearing biologically important morpholine ring have been synthesized by acylation of amino β-lactams in the presence of morpholine-4-carbonyl chloride. These novel β-lactams were prepared under mild reaction conditions without any solvent in short reaction times. Their biological activities have been examined against microbial agents such as Staphylococcus aureus (S. aureus), Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa) and fungi such as Candida albicans (C. albicans) and Candida glabrata (C. glabrata). They have been also tested against Plasmodium falciparum K14 resistant strain and showed moderate to good IC 50 values.

Mots clés: β-Lactam; 2-Azetidinones; Acylation; Antimalarial activities; POM analyses

Domaines: Chimie; Sciences du Vivant [q-bio]; Microbiologie et Parasitologie

Oxana B Kazakova, Jean Michel Brunel, Elmira F Khusnutdinova, Sophie Negrel, Gulnara V Giniyatullina, et al.. Synthesis of New β-Lactams Bearing the Biologically Important Morpholine Ring and POM Analyses of Their Antimicrobial and Antimalarial Activities. Molbank, 2019, 2019 (3), pp.M1078. ⟨10.3390/M1078⟩. ⟨hal-02391762v1⟩