The 2-cyclopropyl substituted benzimidazole 2 has been used as a starting point for further optimization of an LHRH antagonist series. SAR studies revealed that a tert-butyl urea fragment connected through a simple carbon chain would improve activity. Further modification of the benzylsulfonamide moiety led to the discovery of 23 (IC(50): 4.2 nM).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2004.10.090 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Benzimidazole Derivatives in Breast Cancer: Target-Specific Therapeutic Breakthroughs.
Curr Top Med Chem
January 2025
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru 560107, Karnataka, India.
Despite ongoing advancements in drug design and developments, breast cancer remains a serious and devastating disease and is ranked as the second most common illness in women. Breast cancer rates have increased significantly during the last 40 years. This necessitates the development of novel treatment techniques.
View Article and Find Full Text PDFAn Outline on benzimidazole Containing Marketed Drugs with Proton Pump Inhibitor and H Receptor Antagonist Activities.
Mini Rev Med Chem
January 2025
Department of Chemistry, Kurukshetra University, Kurukshetra, Kurukshetra, 136119, India.
Heterocyclic compounds are increasingly used in medicinal chemistry because they are the main components of many biological processes and materials. Benzimidazole remains the core center of the heterocyclic chemical group, with essential traits such as six-five-member connected rings and two nitrogen atoms at the 1,3 position in a six-membered benzene and five-membered imidazole- fused ring system. Molecules with benzimidazole derivatives serve important functions as therapeutic agents and have shown excellent results in clinical and biological research.
View Article and Find Full Text PDFAntiproliferative Activity and Molecular Docking of Some Pyrazole-Based Quinazolinone, Benzimidazole, and Tetrazinethione Derivatives.
J Biochem Mol Toxicol
January 2025
Chemistry Department, Faculty of Science, Ain Shams University, Cairo, Egypt.
Researchers are actively looking for novel anticancer medications because cancer is one of the leading causes of mortality worldwide. A fascinating area of study in medicinal chemistry is the screening of antioxidants for novel anticancer medicines, as antioxidants have lately been used as therapeutic candidates to combat a variety of ailments in aerobic species. Additionally, pyrazole-based heterocycle synthesis is a productive approach to the drug development process.
View Article and Find Full Text PDFReal-World Comparison of Maribavir to Foscarnet for the Treatment of Cytomegalovirus in Solid Organ and Hematopoietic Stem Cell Transplant Recipients.
Viruses
December 2024
Division of Infectious Diseases, Department of Medicine, David Geffen School of Medicine at UCLA, Los Angeles, CA 90095, USA.
Cytomegalovirus (CMV) infection in solid organ transplant (SOT) and hematopoietic cell transplant (HCT) recipients may increase the risk of rejection or allograft dysfunction, other infection(s), and morbidity and mortality. Treatment can be challenging due to medication-associated toxicities. Maribavir (MBV) is a promising option for the treatment of resistant or refractory (R/R) CMV infection in lieu of foscarnet (FOS), which has long been the recommended therapy for (val)ganciclovir-resistant infection.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!