This study aimed to evaluate 2-(N-((2′-(2H-tetrazole-5-yl)-[1,1′-biphenyl]-4yl)-methyl)-pentanamido)-3-methyl butanoic acid-based ester derivatives as a new class of angiotensin-II receptor antagonists. For this purpose, a series of compounds were synthesized using a variety of phenols. Their chemical characterization was established by FTIR, ¹HNMR, and ¹³CNMR techniques. The biological activities including antioxidant potentials using the DPPH assay, the antihypertensive assay, the urease enzyme inhibition assay, and the antibacterial assay using agar well diffusion methods were performed. All the new compounds showed significant free radical scavenging potentials more than the parent drug while retaining antihypertensive potentials along with urease inhibition properties. However, the AV2 test compound was found to be the most potent against hypertension. Most of the synthesized analogs showed urease inhibitory actions. Molecular docking studies were performed for all the active analogs to decode the binding detail of the ligands with receptors of the enzyme’s active site.

Background: DNA gyrase and urease enzymes are important targets for the treatment of gastroenteritis, appendicitis, tuberculosis, urinary tract infections and Crohn's disease. Materials & methods: ... Graphical abstract

Aim: Calcium channel antagonists are of considerable interest in treating elevated blood pressure and its pathologies. Materials & methods: Schiff base derivatives of amlodipine were produced to check its urease inhibition potentials as well antibacterial and antioxidant activities. Structural illustration along with chemical characterization were achieved by spectral techniques (1H NMR, FTIR, 13C NMR) and docking studies also performed. Results & conclusion: 3g displayed remarkable anti-hypertensive activity compared with parent drug. 3b, 3f and 3g showed urease inhibition potentials. These compounds can aid as lead for further investigations since they exhibited comparable or superior interactions.

This study focuses on the synthesis and characterization of novel sitagliptin derivatives, aiming to develop potent, orally active anti-diabetic agents with minimal side effects for the management of type 2 diabetes mellitus. Copper (II) (SCu1-SCu9) and zinc (II) (SZn1-SZn9) metal complexes of sitagliptin-based derivatives were synthesized via a template reaction. The synthesized complexes were comprehensively characterized using elemental analysis, FTIR, UV-Vis, 1 h NMR, and 13C NMR spectroscopy. The biological efficacy of these compounds was assessed through α-amylase and α-glucosidase enzyme inhibition assays, with molecular simulation studies providing additional confirmation of their inhibitory activity. Among the tested derivatives, SD7, SD4, SD3, SD5, and SD9 demonstrated enzyme inhibition profiles comparable to the standard inhibitors. However, the metal complexes exhibited absorption challenges, which may influence their bioavailability. These findings highlight the significant anti-diabetic potential of the synthesized compounds against targeted enzymes, establishing a foundation for their development as lead molecules in future therapeutic research.

Schiff bases, owing to their versatile pharmacological and industrial applications, have attracted significant attention in drug design. The newly synthesized Schiff Base derivatives of bromhexine were characterized using spectral techniques, including Infrared (IR), Nuclear Magnetic Resonance (1 H NMR, 13C NMR) analyses. Pharmacokinetic studies via SwissADME web server. Antiviral screening using the hemagglutination inhibition assay identified BM9 as the most potent compound (IC50 = 3.01 ± 1.70). Antioxidant activity was assessed using the DPPH method. Molecular docking studies against α-amylase and α-glucosidase revealed strong inhibition scores, with BM6 and BM7 emerging as the most promising candidates. This study concludes that derivatives could serve as lead compounds in the development of novel therapeutic agents.