Litcius/Paper detail

Synthesis, <i>in Vitro</i> Bio-Evaluation and <i>in Silico</i> Molecular Docking Studies of Thiadiazole-Based Schiff Base Derivatives

Yousaf Khan, Aneela Maalik, Wajid Rehman, Mohammed M. Alanazi, Shoaib Khan, Rafaqat Hussain, Liaqat Rasheed, Abdul Saboor, Shahid Iqbal

2024Future Medicinal Chemistry21 citationsDOI

Abstract

Aim: Recently, thiadiazole-containing drugs have gained greater clinical relevance and are being explored for the development of new antidiabetic, antiurease and antimicrobial agents that target drug resistance. Methods & results: The authors disclose the synthesis of N-(5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl)methanimine derivatives starting from 4-(trifluoromethyl)benzoic acid. All of the synthesized derivatives were evaluated for their biological potential in order to investigate the inhibitory activity against antidiabetic, antiurease and antibacterial profiles. Compounds 1, 2 and 9 showed excellent inhibitory activities due to the hydrogen bonding presence of -OH, -F and -CF3 substitutions attached with the phenyl ring. Conclusion: The present study provides potent antidiabetic, antiurease and antimicrobial agents that can be further optimized to discover novel antidiabetic, antiurease drugs.

Topics & Concepts

TrifluoromethylAntimicrobialChemistryCombinatorial chemistryIn silicoHydrogen bondDocking (animal)Benzoic acidStereochemistryIn vitroAntibacterial activityBiochemistryOrganic chemistryMoleculeBiologyMedicineBacteriaNursingGeneticsGeneAlkylSynthesis and biological activityEnzyme function and inhibitionClick Chemistry and Applications