Abstract
A Quantitative structure-activity relationship study (QSAR) has been made on a novel series of hydroxamic acid-based matrix metalloproteinase (MMP) inhibitors. The inhibition potencies of the compounds against two MMPs, MMP-2 and MMP-3, are found to be significantly correlated with Kiers first-order valence molecular connectivity index (1xv) and Hammetts electronic constant of the substituents. It is thus found that in addition to zinc-binding group of inhibitors interacting with the zinc ion present in the MMPs, some other groups also in the molecules may have some sorts of physicochemical interactions with the sub-sites of MMPs
Keywords: Quantitative structure-activity relationship, Matrix metalloproteinase inhibitors, Hydroxamic acids
Letters in Drug Design & Discovery
Title: A Quantitative Structure-Activity Relationship Study on a Novel Series of Hydroxamic Acid Analogs Acting as Matrix Metalloproteinase Inhibitors
Volume: 5 Issue: 4
Author(s): S. P. Gupta, Priyanka Bagaria and V. S.A. Kumar Satuluri
Affiliation:
Keywords: Quantitative structure-activity relationship, Matrix metalloproteinase inhibitors, Hydroxamic acids
Abstract: A Quantitative structure-activity relationship study (QSAR) has been made on a novel series of hydroxamic acid-based matrix metalloproteinase (MMP) inhibitors. The inhibition potencies of the compounds against two MMPs, MMP-2 and MMP-3, are found to be significantly correlated with Kiers first-order valence molecular connectivity index (1xv) and Hammetts electronic constant of the substituents. It is thus found that in addition to zinc-binding group of inhibitors interacting with the zinc ion present in the MMPs, some other groups also in the molecules may have some sorts of physicochemical interactions with the sub-sites of MMPs
Export Options
About this article
Cite this article as:
Gupta P. S., Bagaria Priyanka and Kumar Satuluri S.A. V., A Quantitative Structure-Activity Relationship Study on a Novel Series of Hydroxamic Acid Analogs Acting as Matrix Metalloproteinase Inhibitors, Letters in Drug Design & Discovery 2008; 5 (4) . https://dx.doi.org/10.2174/157018008784619852
DOI https://dx.doi.org/10.2174/157018008784619852 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
Related Articles
-
Stress Echocardiography
Current Pharmaceutical Design Discharge Interventions and Modifiable Risk Factors for Preventing Hospital Readmissions in Children with Medical Complexity
Reviews on Recent Clinical Trials Poor Safety and Tolerability Hamper Reaching a Potentially Therapeutic Dose in the Use of Thalidomide for Alzheimer’s Disease: Results from a Double-Blind, Placebo-Controlled Trial
Current Alzheimer Research Genes Involved in Hereditary Hearing Impairment
Current Genomics Diabetic Vascular Complications: Pathophysiology, Biochemical Basis and Potential Therapeutic Strategy
Current Pharmaceutical Design HCN Pacemaker Channels and Pain: A Drug Discovery Perspective
Current Pharmaceutical Design Recent Drug Development Approaches in Thrombosis, Stroke and other Cardiovascular Diseases
Current Pharmaceutical Design Ion Channels and Epilepsy
Current Pharmaceutical Design Regulation of Insulin Synthesis and Secretion and Pancreatic Beta-Cell Dysfunction in Diabetes
Current Diabetes Reviews Phosphatidylinositol 3-kinase Signaling as a Therapeutic Target for Cervical Cancer
Current Cancer Drug Targets Calcium Related Genes in Dogs as Potential Cardiac Biomarkers for the Detection of Chronic Mitral Valve Disease
Recent Patents on Biomarkers Dietary Fatty Acids in Metabolic Syndrome, Diabetes and Cardiovascular Diseases
Current Diabetes Reviews Editorial [Hot Topic:Metabolic Therapy: An Important Therapeutic Option for the Treatment of Cardiovascular Diseases (Executive Editors: G.M.C. Rosano and G. Barbaro)]
Current Pharmaceutical Design Guggulsterone for Chemoprevention of Cancer
Current Pharmaceutical Design The Novel Functions of cGMP-Specific Phosphodiesterase 5 and its Inhibitors in Carcinoma Cells and Pulmonary/Cardiovascular Vessels
Current Topics in Medicinal Chemistry Aldose Reductase, Oxidative Stress and Diabetic Cardiovascular Complications
Cardiovascular & Hematological Agents in Medicinal Chemistry A Review of Intracoronary Abciximab in Percutaneous Coronary Interventions- where are we now and where do we go from here?
Recent Patents on Cardiovascular Drug Discovery Adherence to Secondary Prophylaxis for Acute Rheumatic Fever and Rheumatic Heart Disease: A Systematic Review
Current Cardiology Reviews The Cardiovascular Protective Effects of Chrysin: A Narrative Review on Experimental Researches
Cardiovascular & Hematological Agents in Medicinal Chemistry Flavonoids Influence Epigenetic-Modifying Enzyme Activity: Structure-Function Relationships and the Therapeutic Potential for Cancer
Current Medicinal Chemistry