Synthesis, Molecular Docking, Anticonvulsant and Antimicrobial Activity of 1, 3, 5-Trisubstituted-2-Pyrazolines Linked Benzimidazole Derivatives

Sagar Hullur, Tanuja A M L, V. Lokeswar Babu, Mallikarjun K A.

Abstract: A series of 1-(3-(4-(2-methyl-5-(substituted)-1H-benzomidazole-1-yl)phenyl)-5-(4-(substituted)phenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethan-1-one (SMa-f [A,B,C]) are synthesized and evaluated their antiepileptic and anti-microbial activity. The formation of benzimidazole proceeds through following mechanism of Phillips reaction. Preparation of chalcones proceeds through following Claisen-Schmidt condensation reaction. Pyrazolines are proceeds through following mechanism of Fischer and Knoevenagel condensation reactions. Antiepileptic screening of the title compounds was performed using pentylenetetrazole seizures test. Compound SMb-B showed significant antiepileptic activity compared to diazepam as standard. Antimicrobial activity against two gram positive and two gram negative bacteria using by serial dilution and agar well diffusion method. The newly synthesized compounds SMa-C and SMb-A have showed excellent antimicrobial activity against tested microorganisms. In correlation to antiepileptic activity, selected compounds were subjected for molecular docking studies and the compounds SMb-A, SMb-B, SMc-B, SMd-A and SMe-A have emerged maximum binding affinity with standard drug using calculated Autodock 4.2.1 with GABA-A receptor (PDB ID:6D6T). The drug likeness properties of evaluated the compounds were also showed the satisfactory results. Compounds were characterized by spectroscopic techniques such as UV, 1HNMR, 13CNMR, IR and mass spectroscopy.

Keywords: 2-methyl benzimidazole, 1,3,5-trisubstituted pyrazolines, anticonvulsant activity, antimicrobial activity, molecular docking, ADME properties, 6D6T

How to Cite?: Sagar Hullur, Tanuja A M L, V. Lokeswar Babu, Mallikarjun K A., "Synthesis, Molecular Docking, Anticonvulsant and Antimicrobial Activity of 1, 3, 5-Trisubstituted-2-Pyrazolines Linked Benzimidazole Derivatives", Volume 15 Issue 8, August 2026, International Journal of Science and Research (IJSR), Pages: 695-706, https://www.ijsr.net/getabstract.php?paperid=SR26808144658, DOI: https://dx.doi.org/10.21275/SR26808144658

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