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

Aliasghar Jarrahpoura (1) , Roghayeh Heirana (1) , Véronique Sinouc (2) , Christine Latourc (2) , Lamia Djouhri Bouktabd (3) , Jean Michel Brunel (3) , Javed Sheikhe (4) , Taibi Ben Haddaf (5)

1 SUTech - Shiraz University of Technology
2 MCT - Membranes et cibles thérapeutiques
3 CRCM - Centre de Recherche en Cancérologie de Marseille
4 Dhote Bandhu Science College
5 Université Mohammed Premier [Oujda]

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.

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

Domains: Chemical Sciences; Chemical Sciences; Organic chemistry; Life Sciences [q-bio]; Life Sciences [q-bio]; Microbiology and Parasitology; Life Sciences [q-bio]; Microbiology and Parasitology; Bacteriology; Life Sciences [q-bio]; Microbiology and Parasitology; Parasitology

Aliasghar Jarrahpoura, Roghayeh Heirana, Véronique Sinouc, Christine Latourc, Lamia Djouhri Bouktabd, et al.. Synthesis of New β-Lactams Bearing the Biologically Important Morpholine Ring and POM Analyses of Their Antimicrobial and Antimalarial Activities. Iranian Journal of Pharmaceutical Research, 2019, 18 (1), pp.34-48. ⟨10.22037/ijpr.2019.2348⟩. ⟨hal-02392394⟩