A number of 6-(substituted phenyl)-2-(4-substituted phenyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)-4,5-dihydropyridazin-3(2H)-one derivatives were designed and synthesized by a sequence of reactions starting from respective aryl hydrocarbons. The final compounds (4a-4u) were evaluated for antihypertensive activities by non-invasive method using Tail Cuff method. The compounds 4e, 4i and 4k showed appreciable antihypertensive activity comparable with that of standard hydralazine and propranolol.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2010.12.028 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Benzothiazole-triazole hybrids: Novel anticancer agents inducing cell cycle arrest and apoptosis through Bcl-2 inhibition in triple-negative breast cancer.
Bioorg Chem
January 2025
Department of Chemistry, SRICT-Institute of Science and Research, UPL University of Sustainable Technology, Ankleshwar Valia Road, Vataria 393135, India. Electronic address:
In this study, we aim to detail the design and synthesis of a series of benzothiazole tethered triazole compounds that incorporate acetamide chains, with the purpose of investigating their potential as anticancer agents. The structural integrity of the compounds was confirmed through characterization using H NMR, C NMR, mass spectrometry, and IR spectroscopy. The compounds demonstrated notable cytotoxic effects when tested against a range of cancer cell lines, with a specific inhibition observed in triple-negative breast cancer.
View Article and Find Full Text PDFParallel Temperature Replica-Exchange Molecular Dynamics Simulations Capture the Observed Impact of Stapling on Coiled-Coil Conformational Stability.
J Phys Chem B
January 2025
Department of Chemistry and Biochemistry, Brigham Young University, Provo, Utah 84602, United States.
Macrocyclization or stapling is an important strategy for increasing the conformational stability and target-binding affinity of peptides and proteins, especially in therapeutic contexts. Atomistic simulations of such stapled peptides and proteins could help rationalize existing experimental data and provide predictive tools for the design of new stapled peptides and proteins. Standard approaches exist for incorporating nonstandard amino acids and functional groups into the force fields required for MD simulations and have been used in the context of stapling for more than a decade.
View Article and Find Full Text PDFDesign, synthesis, and structure-activity relationships of five-membered heterocyclic incorporated aryl(alkyl)azoles: From antiproliferative thiazoles to safer anticonvulsant oxadiazoles.
Bioorg Chem
December 2024
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran. Electronic address:
In the current study, a novel series of 1,2,4-oxadiazoles were designed, synthesized, and evaluated for their biological activities. A cell-based antiproliferative screening was accomplished on the newly synthesized 1,2,4-oxadiazoles along with our previously reported aryl(alkyl)azoles (AAAs) containing middle heterocyclic cores thiazole and oxazole. Among the tested compounds, naphthyl- thiazoles demonstrated higher antiproliferative activity and B3 was identified as the most potent compound with IC values in the range of 2.
View Article and Find Full Text PDFSynthesis and crystal structure of 1-1,2,4-triazole-3,5-di-amine monohydrate.
Acta Crystallogr E Crystallogr Commun
October 2024
Faculty of Environment and Information Sciences Yokohama National University, 79-7 Tokiwadai Hodogaya-ku Yokohama-shi Kanagawa 240-8501 Japan.
The title compound, a hydrate of 3,5-di-amino-1,2,4-triazole (DATA), CHN·HO, was synthesized in the presence of sodium perchlorate. The evaporation of HO from its aqueous solution resulted in anhydrous DATA, suggesting that sodium perchlorate was required to precipitate the DATA hydrate. The DATA hydrate crystallizes in the 2/ space group in the form of needle-shaped crystals with one DATA and one water mol-ecule in the asymmetric unit.
View Article and Find Full Text PDFStructure-activity relationship of modified amphiphilic cationic cyclodextrins for enhanced siRNA delivery.
Int J Pharm
December 2024
Pharmacodelivery Group, School of Pharmacy, University College Cork, Cork T12 YN60, Ireland. Electronic address:
Article Synopsis
- The study explores how modifying the cyclodextrin (CD) ring structure with hydroxyl groups and functional groups enhances its potential for delivering therapeutic siRNA.
- Multiple cationic amphiphilic CDs were synthesized and evaluated for their ability to encapsulate siRNA and improve gene silencing efficiency in A549-luc cells.
- Key findings revealed that CDs with primary amine modifications at positions C2 and C3 significantly increased gene knockdown levels, achieving up to 80% with specific linker modifications.
Want 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!