Synthesis of β-Lactam Conjugates of Thiadiazine Thiones as a New Class of Anti-Nociceptive Agents
نویسندگان
1 Institute of Chemical Sciences, University of Peshawar, Peshawar-25120, Khyber Pakhtunkhwa, PAKISTAN
2 College of Chemistry, Xinjiang University, Urumqi, Xinjiang 830017, P.R. CHINA
3 Department of Agricultural and Livestock Production, Program of Organic Farming, Cal Vocational High School, Pamukkale University, Denizli, 20700, TURKIYE
4 Program of Medical Laboratory and Techniques, Department of Medical Services and Techniques, Vocational School of European, University of Kocaeli Health and Technology, Kocaeli, TURKIYE
5 Program of Medical Laboratory and Techniques, Department of Medical Services and Techniques, Vocational School of European, University of Kocaeli Health and Technology, Kocaeli, TURKIYE
6 Institute of Chemical Sciences, University of Peshawar, Peshawar-25120, Khyber Pakhtunkhwa, PAKISTAN
7 School of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, Henan, P.R. CHINA
8 Department of Biotechnology, Faculty of Pharmacy, University of Kocaeli Health and Technology, Kocaeli, TURKIYE
9 Institute of Chemical Sciences, University of Peshawar, Peshawar-25120, Khyber Pakhtunkhwa, PAKISTAN
10 Institute of Chemical Sciences, University of Peshawar, Peshawar-25120, Khyber Pakhtunkhwa, PAKISTAN
11 Department of Biochemistry, Abdul Wali Khan University, Mardan, Mardan-23200, Khyber Pakhtunkhwa, PAKISTAN
doi
10.30492/ijcce.2025.2069202.7257چکیده
A series of newly synthesized β-lactam conjugates of thiadiazine-2-thiones (TDZ-2T) 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 1e, 1f, 1g, 2a, and 2b showing the most significant activity. Additionally, the anti-nociceptive impact of the prepared substances was analyzed by the hot plate technique. Substances 1a, 1b, 1d, 1f, 1g, and 2a demonstrated notable activity at dosages of 80 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-2 (COX) enzyme.
