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Central Nervous System Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5249
ISSN (Online): 1875-6166

Synthesis, Anticonvulsant and Binding Interaction Study of Novel Piperamides with Bovine Serum Albumin by Fluorescence Spectroscopy

Author(s): Maralekere K. Prashanth, Hemavathi N. Deepakumari, Madihalli S. Raghu, Hosakere D. Revanasiddappa and Bantal Veeresh

Volume 16 , Issue 1 , 2016

Page: [60 - 66] Pages: 7

DOI: 10.2174/1871524915666150531190229

Price: $65

Abstract

A series of piperamides (PA) 8a-j were designed, synthesized and evaluated for their antimicrobial and anticonvulsant activity. Compounds 8a and 8h showed considerable antibacterial activity against B. subtilis with minimum inhibitory concentration (MIC) of 8 and 10 µg/mL, respectively. Compounds 8a and 8h showed advanced anticonvulsant activity as well as lower neurotoxicity than the reference drugs. The interaction between bovine serum albumin (BSA) and PA was investigated using fluorescence quenching and UV-vis absorption spectroscopy. Results showed that PA could strongly quinch the intrensic fluorescence of BSA through a static quencing procedure. The binding constant and number of binding sites of PA with BSA were obtained. The binding distance was calculated based on Forster non-radiative energy transfer theory.

Keywords: Anticonvulsant, bovine serum albumin, fluorescence quenching, piperamide.

Graphical Abstract

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