Article Details

DESIGN, SYNTHESIS OF SCHIFF BASE CIPROPFLOXACIN-VANILLIN DERAVATIVES OF POTENT BACTERIAL DNA GYRASE INHIBITOR

Swain Sudhansu Sekhara, Sahoo Chita Ranjana,b, Sahoo Jyotirmayac, Padhy Rabindra Nathb, Ravi Kumar B. V. V.d and Paidesetty Sudhir Kumara*

a School of Pharmaceutical Sciences, Department of Medicinal Chemistry, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar 751003, Odisha, India 

b  The Central Research Laboratory, Institute of Medical Sciences & Sum Hospital, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar 751003, Odisha, India

 

c School of Pharmacy, ARKA JAIN University, Gamharia, Seraikela Kharsawan, Jameshedpur, Jharkand, Pin-832108, India

d Roland Institute of Pharmaceutical Sciences, Khodasingi, Berhampur, Odisha, Pin:760010, India

* For Correspondence E-mail: psudhirkumar@soa.ac.in


ABSTRACT

A series of Schiff base ciprofloxacin hydrazones with vanillin analogues were designed and validated for druggability properties by advanced computational tools, from which two shortlisted compounds were synthesized and characterized by different spectral studies. These compounds were used against bacterial DNA gyrase; purposedly attempted in molecular docking studies, the compounds 5h and 5i indicated good binding affinity of -8.2 and -8.5 kcal/mol, respectively. Moreover, in vitro antibacterial activities against uropathogenic bacteria, E. coli, was assessed and the compounds 5h, and 5i had significant inhibitory actions. SAR studies revealed that the presence of the quinolone nucleus, azomethine functional group and vanillyl ester might have shown the response of antibacterial inhibition. Thus, vanillyl esters condensed with ciprofloxacin hydrazone through Schiff base, have more antibacterial inhibitory actions. The recorded antibacterial results were corroborated with docking results.

Year 2020 | Volume No. 57 | Issue No.3 | Page No. 21-26
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