Abstract
Protein tyrosine phosphatase 1B (PTP1B) is a well known drug target for the treatment of type 2 diabetes mellitus (T2DM). Diverse inhibitors have been reported in literature that inhibit PTP1B. We have reported 2-substituted benzoxazole class of In PTP1B inhibitors earlier. Present work describes 2-substituted benzothiazole compounds as PTP1B inhibitor as an extension of our previous study. Compound 23c, a disubstituted para-Bromobenzyl sulfonamide compound, exhibited moderate biochemical potency (Ki) of 1.4 µM. SAR on synthesized compounds was explained using molecular modeling study.
Keywords: Benzothiazoles, Oxamic acids, PTP1B, Type 2 Diabetes, pTyr mimetics, Disubstituted sulfonamides.
Letters in Drug Design & Discovery
Title:Design and Synthesis of Novel 2- Substituted Benzothiazole Compounds as PTP1B Inhibitors
Volume: 11 Issue: 4
Author(s): Arun P. Chandrasekharappa, Sangamesh E. Badiger, Pramod K. Dubey, Sunil K. Panigrahi and Sekhar Reddy VVV. Manukonda
Affiliation:
Keywords: Benzothiazoles, Oxamic acids, PTP1B, Type 2 Diabetes, pTyr mimetics, Disubstituted sulfonamides.
Abstract: Protein tyrosine phosphatase 1B (PTP1B) is a well known drug target for the treatment of type 2 diabetes mellitus (T2DM). Diverse inhibitors have been reported in literature that inhibit PTP1B. We have reported 2-substituted benzoxazole class of In PTP1B inhibitors earlier. Present work describes 2-substituted benzothiazole compounds as PTP1B inhibitor as an extension of our previous study. Compound 23c, a disubstituted para-Bromobenzyl sulfonamide compound, exhibited moderate biochemical potency (Ki) of 1.4 µM. SAR on synthesized compounds was explained using molecular modeling study.
Export Options
About this article
Cite this article as:
Chandrasekharappa P. Arun, Badiger E. Sangamesh, Dubey K. Pramod, Panigrahi K. Sunil and Manukonda Reddy VVV. Sekhar, Design and Synthesis of Novel 2- Substituted Benzothiazole Compounds as PTP1B Inhibitors, Letters in Drug Design & Discovery 2014; 11 (4) . https://dx.doi.org/10.2174/15701808113106660076
DOI https://dx.doi.org/10.2174/15701808113106660076 |
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
-
Clinical Applications of Transcranial Doppler Sonography
Reviews on Recent Clinical Trials Diabetes Beyond Insulin: Review of New Drugs for Treatment of Diabetes Mellitus
Current Drug Discovery Technologies Non Enzymatic Glycated Proteins in the Blood and Cardiovascular Disease
Current Pharmaceutical Design Cardiovascular Effects of Hypoglycemic Agents in Diabetes Mellitus
Current Drug Safety Cross-linked Mucoadhesive Microspheres based on Anionic Heteropolysaccharide for Nasal Delivery of Felodipine: Optimization and in vitro Evaluation
Drug Delivery Letters Meet Our Editorial Board Member (Bioinformatics)
Current Chinese Science Functional Genome and Proteome Analyses of Cutaneous Autoimmune Diseases
Current Pharmaceutical Design Clinical Research on the Aortic Elasticity in Patients with Type 1 Diabetes Mellitus Complicated with Hypertension
Current Medical Imaging Anti-Angiogenesis Activities of Dietary Constituents and Health Foods with Potential Anti-Hepatocellular Carcinoma Activity
Recent Patents on Biomarkers MTHFR Gene Polymorphism and Diabetic Retinopathy
Current Diabetes Reviews Cholinesterase Inhibitors Modulate Autonomic Function in Patients with Alzheimer´s Disease and Mixed Dementia
Current Alzheimer Research Omega-3 Fatty Acids for Nutrition and Medicine: Considering Microalgae Oil as a Vegetarian Source of EPA and DHA
Current Diabetes Reviews Preface (Hot Topic: Medicinal Strategies in the Treatment of Obesity Guest Editor: Akio Inui)
Current Medicinal Chemistry - Central Nervous System Agents Recent Patents on Oral Insulin Delivery
Recent Patents on Drug Delivery & Formulation Therapeutic Implications of Beta-Adrenergic Receptor Pharmacodynamic Properties
Current Clinical Pharmacology Isolated Compounds from Natural Products with Potential Antidiabetic Activity - A Systematic Review
Current Diabetes Reviews Neural Pathways and Neuropeptides Mediate the Therapeutic Actions of DPP IV Inhibitors in Type-2 Diabetes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Non Peptidic Urotensin II Antagonists: Perspectives for a New Class of Drugs
Cardiovascular & Hematological Agents in Medicinal Chemistry Assessment and Relevance of Carotid Intima-Media Thickness (C-IMT) in Primary and Secondary Cardiovascular Prevention
Current Pharmaceutical Design Cardiorenal Consequences of Atherosclerosis and Statins Therapy: From the Past to the Future
Current Pharmaceutical Design