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
-
Novel Approaches for Allergy
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents New Concepts for Glaucoma Implants - Controlled Aqueous Humor Drainage, Encapsulation Prevention and Local Drug Delivery
Current Pharmaceutical Biotechnology Pharmacologic Agents for the Treatment of Vasodilatory Shock
Current Pharmaceutical Design Humic Acids as Therapeutic Compounds in Lead Intoxication
Current Clinical Pharmacology Prevalence and Risk Factors of Vitamin D Deficiency in Critically Ill Patients
Inflammation & Allergy - Drug Targets (Discontinued) GnRH-Agonist Triggering to Avoid Ovarian Hyperstimulation Syndrome: A Review of the Evidence
Current Drug Targets Radix Astragali (Astragalus): Latest Advancements and Trends in Chemistry, Analysis, Pharmacology and Pharmacokinetics
Current Organic Chemistry Ventricular Arrhythmias in Seniors with Heart Failure: Present Dilemmas and Therapeutic Considerations: A Systematic Review
Current Cardiology Reviews Novel Drugs for Chronic Lymphoid Leukemias: Mechanism of Action and Therapeutic Activity
Current Medicinal Chemistry Therapeutic Properties of Mushrooms in Managing Adverse Effects in the Metabolic Syndrome
Current Topics in Medicinal Chemistry The Role of Renal Nerve Ablation for the Management of Resistant Hypertension and other Disease Conditions: Benefits and Concerns
Current Vascular Pharmacology Cardiovascular Pharmacogenomics
Current Pharmacogenomics and Personalized Medicine Oxidative-Nitrosative Stress as a Contributing Factor to Cardiovascular Disease in Subjects with Diabetes
Current Vascular Pharmacology <i>Nigella Sativa</i> (Black Seeds), A Potential Herb for the Pharmacotherapeutic Management of Hypertension - A Review
Current Cardiology Reviews Radiation-Induced Extracranial Carotid Stenosis
Vascular Disease Prevention (Discontinued) Current Concepts in the Management of Diabetic Polyneuropathy
Current Diabetes Reviews Pathogenesis-Oriented Targets for Adjunctive Therapy
Endocrine, Metabolic & Immune Disorders - Drug Targets Thrombolysis in Ischemic Stroke: Focus on New Treatment Strategies
Recent Patents on Cardiovascular Drug Discovery Pharmacological Manipulation of Peripheral Vascular Resistance in Single Ventricle Patients (Stages I, II, and III of Palliation)
Current Vascular Pharmacology Genetically Engineered Elastin-based Biomaterials for Biomedical Applications
Current Medicinal Chemistry