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.
Central Nervous System Agents in Medicinal Chemistry
Title:Synthesis, Anticonvulsant and Binding Interaction Study of Novel Piperamides with Bovine Serum Albumin by Fluorescence Spectroscopy
Volume: 16 Issue: 1
Author(s): Maralekere K. Prashanth, Hemavathi N. Deepakumari, Madihalli S. Raghu, Hosakere D. Revanasiddappa and Bantal Veeresh
Affiliation:
Keywords: Anticonvulsant, bovine serum albumin, fluorescence quenching, piperamide.
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.
Export Options
About this article
Cite this article as:
K. Prashanth Maralekere, N. Deepakumari Hemavathi, S. Raghu Madihalli, D. Revanasiddappa Hosakere and Veeresh Bantal, Synthesis, Anticonvulsant and Binding Interaction Study of Novel Piperamides with Bovine Serum Albumin by Fluorescence Spectroscopy, Central Nervous System Agents in Medicinal Chemistry 2016; 16 (1) . https://dx.doi.org/10.2174/1871524915666150531190229
DOI https://dx.doi.org/10.2174/1871524915666150531190229 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Transfusion-related Acute Lung Injury: An Overview
Current Pharmaceutical Design Developing Pharmacotherapies for Cannabis and Cocaine Use Disorders
Current Neuropharmacology The Management and Outcomes of Pharmacological Treatments for Tinnitus
Current Neuropharmacology Dopamine: Agonists and Neurodegenerative Disorders
Current Drug Targets Role of PGE2 in Blood Pressure Regulation
Current Hypertension Reviews Cardiovascular Alterations After Spinal Cord Injury: An Overview
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Current Metabolomic Methodologies & their Application to Thermal Stress
Current Metabolomics Pharmacokinetics of Drugs in Neonates: Pattern Recognition Beyond Compound Specific Observations
Current Pharmaceutical Design Toll-Like Receptors and Inflammation in the CNS
Current Drug Targets - Inflammation & Allergy COX-Inhibiting Nitric Oxide Donors (CINODs): Potential Benefits on Cardiovascular and Renal Function
Cardiovascular & Hematological Agents in Medicinal Chemistry Contribution and Value of Biomarkers in Acute Aortic Syndromes
Current Pharmaceutical Biotechnology Caring for HIV-Infected Patients in the ICU in The Highly Active Antiretroviral Therapy Era
Current HIV Research Waste Material of Propolis as a Film Forming Agent Intended to Modify the Metronidazole Release: Preparation and Characterization
Current Drug Delivery Increased Salt Sensitivity in Obese Hypertension: Role of the Sympathetic Nervous System
Current Hypertension Reviews Induction of Haemolysis and DNA Fragmentation in a Normal and Malarial-Infected Blood by Commonly - used Antimalarial Drugs in the North-Western Region of Nigeria
Drug Metabolism Letters Ribonucleases, Nucleases and Antiangiogenins in Antiproliferative Activities
Current Signal Transduction Therapy Isoniazid: Metabolic Aspects and Toxicological Correlates
Current Drug Metabolism Revisiting Antipsychotic-induced Akathisia: Current Issues and Prospective Challenges
Current Neuropharmacology Adenosine in the Inflamed Gut: A Janus Faced Compound
Current Medicinal Chemistry Fabry Disease Cardiomyopathy: from Genes to Clinical Manifestations
Current Pharmaceutical Biotechnology