Abstract
The diltiazem binding site of L-type calcium channels is the least characterized to date. In this paper, we present some of the available chemotypes that bind to the benzothiazepine binding site: natural compounds, compounds synthesized by varying the benzothiazepine scaffold, and compounds discovered by means of computational approaches.
Keywords: (+)-cis-Diltiazem, L-type calcium channels, benzothiazepine, chemotype, computational approaches, voltage gated calcium channel, calcium entry blockers, structural and functional analogs
Mini-Reviews in Medicinal Chemistry
Title: Ligands of Diltiazem Binding Site: An Overview of Some Chemotypes
Volume: 9 Issue: 12
Author(s): R. Budriesi, P. Ioan, E. Carosati, G. Cruciani, B. S. Zhorov and A. Chiarini
Affiliation:
Keywords: (+)-cis-Diltiazem, L-type calcium channels, benzothiazepine, chemotype, computational approaches, voltage gated calcium channel, calcium entry blockers, structural and functional analogs
Abstract: The diltiazem binding site of L-type calcium channels is the least characterized to date. In this paper, we present some of the available chemotypes that bind to the benzothiazepine binding site: natural compounds, compounds synthesized by varying the benzothiazepine scaffold, and compounds discovered by means of computational approaches.
Export Options
About this article
Cite this article as:
Budriesi R., Ioan P., Carosati E., Cruciani G., Zhorov S. B. and Chiarini A., Ligands of Diltiazem Binding Site: An Overview of Some Chemotypes, Mini-Reviews in Medicinal Chemistry 2009; 9 (12) . https://dx.doi.org/10.2174/138955709789957369
DOI https://dx.doi.org/10.2174/138955709789957369 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- 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
-
Emerging Risk Factors for Cerebrovascular Disease
Current Drug Targets Tetramethoxyluteolin for the Treatment of Neurodegenerative Diseases
Current Topics in Medicinal Chemistry Similarities and Differences Between Renal Sympathetic Denervation and Carotid Baroreceptor Stimulation
Current Vascular Pharmacology Clinical Potential of VIP by Modified Pharmaco-kinetics and Delivery Mechanisms
Endocrine, Metabolic & Immune Disorders - Drug Targets Vascular Inflammation During Human Rickettsioses: An Essential Host Response and a Potential Target for Supplemental Therapy
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Meet Our Editorial Board Member
Current Pharmaceutical Biotechnology Relationship between Augmentation Index and Wall Thickening Fraction during Hypotension in an Animal Model of Myocardial Ischemia-Reperfusion and Heart Failure
Current Hypertension Reviews An Overview of Neolignans of the Genus Piper L.: Isolation Methods and Biological Activities
Mini-Reviews in Medicinal Chemistry Anti-VEGF Strategies – from Antibodies to Tyrosine Kinase Inhibitors: Background and Clinical Development in Human Cancer
Current Pharmaceutical Design Post Dural Puncture Headache and Hypertension
Current Hypertension Reviews Citicoline and Retinal Ganglion Cells: Effects on Morphology and Function
Current Neuropharmacology The Role of Natural Killer T Cells in Acute Kidney Injury: Angel or Evil?
Current Protein & Peptide Science The Management of Phosphodiesterase-5 (PDE5) Inhibitor Failure
Current Vascular Pharmacology The High Potency of Polymeric Nanoparticles in the Drug Delivery System for Hypertension Treatment: A Systematic Review
Current Hypertension Reviews An Overview of the Modulatory Effects of Oleic Acid in Health and Disease
Mini-Reviews in Medicinal Chemistry Angiotensin Converting Enzyme Inhibitory Peptides Derived from Food Proteins: Biochemistry, Bioactivity and Production
Current Pharmaceutical Design CGRP-Receptor Antagonism in Migraine Treatment
CNS & Neurological Disorders - Drug Targets Adipose Tissue and Bone Marrow as Sources for Cell-based Therapeutic Angiogenesis in Ischemic Tissues: Biological Foundation and Clinical Prospects for Age-related Vascular Disease
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Impaired Cerebral Autoregulation and Vasomotor Reactivity in Sporadic Alzheimer’s Disease
Current Alzheimer Research Beta-arrestin Biased Agonism/Antagonism at Cardiovascular Seven Transmembrane-spanning Receptors
Current Pharmaceutical Design