A new family of 1,2,5-thiadiazolidine 1,1-dioxides: Synthesis, structure and antibacterial activity

A. Amira (1) , H. K’tir (1) , I. Becheker (2) , S. Ouarna (1) , Nicolas Inguimbert (3) , H. Berredjem (2) , M. Berredjem (1) , Nour-Eddine Aouf (4)

1 LAOC - Laboratory of Applied Organic Chemistry
2 Laboratory of Applied Biochemistry and Microbiology
3 CRIOBE - Centre de recherches insulaires et observatoire de l'environnement
4 Laboratoire de Chimie Bioorganique

A convenient synthesis of novel N-N’-substituted 1,2,5-thiadiazolidine 1,1-dioxides starting from amino acids is reported in five step (reduction, carbamoylation-sulfamoylation, intermolecular cyclization via the Mitsunobu reaction and acylation). The newly synthesized compounds were characterized by IR, NMR and mass spectral analysis. Some of the newly synthesized compounds (4c and 4d) were examined for their antibacterial activity against several strains of Gram-positive and Gram-negative bacteria.

Keywords: CSI; Mitsunobu reaction; Cyclosulfamide; Acylation; Antibacterial Activity

Domains: Chemical Sciences; Organic chemistry

A. Amira, H. K’tir, I. Becheker, S. Ouarna, Nicolas Inguimbert, et al.. A new family of 1,2,5-thiadiazolidine 1,1-dioxides: Synthesis, structure and antibacterial activity. Der pharma chemica, 2015, 7 (7), pp.ePUB. ⟨hal-01197166⟩