Synthesis of β-Lactam Conjugates of Thiadiazine Thiones as a New Class of Anti-Nociceptive Agents

A series of newly synthesized β-lactam conjugates of thiadiazine-۲-thiones (TDZ-۲T) were prepared by reacting various primary amines with carbon disulfide and potassium hydroxide, followed by the addition of formaldehyde and β-lactam antibiotics, including cefaclor and cefadroxil, in phosphate buffer. The synthesized substances were evaluated for their in vitro antimicrobial activity against P. aeruginosa and E. coli. All the substances exhibited activity against each form of bacterial types, with ۱e, ۱f, ۱g, ۲a, and ۲b showing the most significant activity. Additionally, the anti-nociceptive impact of the prepared substances was analyzed by the hot plate technique. Substances ۱a, ۱b, ۱d, ۱f, ۱g, and ۲a demonstrated notable activity at dosages of ۸۰ mg/kg, as evidenced by a significant enhancement during the lag phase. Intact binding studies of the synthesized substance were also performed and showed a good binding interaction with the binding site of the in silico cyclooxygenase-۲ (COX) enzyme.

کلیدواژه ها:

TDZ-۲T derivatives ، Synthesis ، (COX-۲) potential