10.1007/s12039-011-0138-8
The research focuses on the efficient green synthesis of Schiff bases and azetidinones derivatised with 1,2,4-triazoles. The study employs Mg(ClO4)2 as a catalyst for the synthesis of Schiff bases from 1-amino-2-aryl-3-oxo-1,2,4-triazoles with various aldehydes under solvent-free conditions. The resulting Schiff bases are then reacted with chloroacetyl chloride to yield azetidinones, also in solvent-free conditions, with excellent yields. The synthesized compounds were analyzed for their potential as drugs by evaluating properties such as penetration into biological membranes (clogP), drug-likeliness, and drug scores. Additionally, the compounds were screened for antitubercular and antimicrobial activities. The analyses included techniques such as IR spectroscopy, 1H NMR spectroscopy, mass spectrometry, and elemental analysis, as well as thin layer chromatography (TLC) to check the purity of the compounds. The pharmacological evaluation was carried out at a separate facility, and the OSIRIS property explorer was used for computational drug analysis.
10.1007/s12039-012-0354-x
The research focuses on the synthesis and evaluation of a series of 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)acetamide-based azetidinone derivatives as potential antibacterial and antifungal agents. The study involved the synthesis of twelve compounds, which were subjected to in vitro antibacterial testing against E. coli, S. aureus, K. pneumoniae, P. aeruginosa, and antifungal testing against C. albicans, A. niger, and A. flavus using the cup-plate method. The synthesized compounds were confirmed through spectral data interpretation, including Fourier Transform-Infrared (FT-IR) spectroscopy, proton nuclear magnetic resonance (1H-NMR) spectroscopy, electrospray ionization mass spectrometry (ESI-MS), and elemental analysis. The experiments utilized various reactants such as pyruvic acid, o-phenylenediamine, ethylchloroacetate, potassium carbonate, and different aromatic aldehydes, along with chloroacetylchloride and triethylamine for the final compound formation. The structures of the synthesized compounds were elucidated using these analytical techniques, and their biological activities were assessed and compared with standard drugs to determine their potential as antimicrobial agents.
10.1016/j.tetlet.2018.03.066
The research aims to develop selective anion receptors that utilize weak C-H hydrogen bonds, with a focus on phosphinate receptors. Phosphinates are significant in nature due to their association with metabolic diseases and conditions like obesity, NASH, hypercholesterolemia, and diabetes. The researchers designed and synthesized three receptors (1, 2, and 3) that utilize both amide N-H and alpha C-H (Cα-H) to the carbonyl group, differing in the substituent group attached to the alpha carbon, which affects the polarity of the CαH bond and thus the strength of association with anion guests. The study concluded that host 3, with a positively charged pyridinium group, showed the highest binding affinity due to the increased polarity of the Cα-H bond, demonstrating the importance of C-H hydrogen bonding as a modulating element for anionic recognition. Key chemicals used in the synthesis include 1,2-phenylenediamine, acetic acid, cyanoacetic acid, chloroacetyl chloride, pyridine, and various anions for testing, such as dimethyl phosphinate, benzoate, nitrite, and others.
T,
N,
C
T:Toxic;
