Synthesis, Characterization, and Biological Evaluation of 2-(N-((2′-(2H-tetrazole-5-yl)-[1,1′-biphenyl]-4yl)-methyl)-pentanamido)-3-methyl Butanoic Acid Derivatives

Abstract

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.

Design, Synthesis, and Biological Evaluation of Dexibuprofen Derivatives as Novel Anti‐Inflammatory, Antioxidant and Molecular Docking Studies

“…% of antioxidant activity ¼ ½AÀ B=A� � 100 A = Absorbance of control B = Absorbance of sample. [34] Lipoxygenase Enzyme assay: Lipoxygenase (LOX) activity was sought almost in accordance with the already mentioned procedure. [35][36][37] For the preparation of lipoxygenase assay mixture take 150 μl sodium phosphate buffers (10 Mm and pH of 8) and 15 μl compound (required to be tested) and 20 μl enzyme (169 units/well).…”

Synthesis, Characterization, and Evaluation of Tetrazole Derivatives with Pyrrole‐2,5‐Dione Moieties as Urease Inhibitors: Exploring Structure‐Activity Relationships and Computational Insights

“…[21][22][23][24][25] Numerous efforts have been made to enhance the urease inhibitory potency and selectivity of existing azole drugs by modifying their structures. [26][27][28] Despite the potential antibacterial and antifungal activities associated with certain tetrazoles, the role of the tetrazole moiety in this pharmacophore has been largely overlooked, with only a few studies addressing it. [29][30][31] Furthermore, there is a keen interest in integrating additional chemotherapeutically-active groups into the structure, intending to introduce synergistic effects to the target compounds.…”

“…Consequently, heterocyclic compounds have emerged as key components in the synthesis of therapeutics for a wide range of diseases, including cancer, [20] infectious diseases, and neurological disorders [21–25] . Numerous efforts have been made to enhance the urease inhibitory potency and selectivity of existing azole drugs by modifying their structures [26–28] . Despite the potential antibacterial and antifungal activities associated with certain tetrazoles, the role of the tetrazole moiety in this pharmacophore has been largely overlooked, with only a few studies addressing it [29–31] .…”