Litcius/Paper detail

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

Anum Masood, Mohsin Abbas Khan, Irshad Ahmad, Breena Awan, Asim Raza, Farhat Ullah, Syed Adnan Alı Shah

2023Molecules11 citationsDOIOpen Access PDF

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.

Topics & Concepts

TetrazoleBiphenylChemistryCharacterization (materials science)StereochemistryOrganic chemistryMedicinal chemistryMaterials scienceNanotechnologySynthesis of Tetrazole DerivativesQuinazolinone synthesis and applicationsSynthesis and biological activity