Several imidazolylphenyl sulfamate and (imidazolylphenoxy)alkyl sulfamate derivatives were synthesized and evaluated as topically active carbonic anhydrase inhibitors. Water solubility, pKa, carbonic anhydrase inhibition, and partition coefficient for the compounds were measured. Sulfamic acid 2-[4-(1H-imidazol-1-yl)phenoxy]ethyl ester monohydrochloride (16) has the best combination of properties and showed excellent topical activity in lowering the intraocular pressure in New Zealand white rabbits.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm00104a003 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Design of natural asphalt sulfamic acid (NA-NHSOH) as a scalable natural asphalt-derived heterogeneous Brønsted acid to catalyze multicomponent reactions meeting green chemistry goals.
Heliyon
January 2025
Department of Chemistry, Faculty of Basic Sciences, Ilam University, P.O. Box 69315516, Ilam, Iran.
This study highlights an innovative approach to catalysis by utilizing natural asphalt as a support material for developing carbon-based catalysts. By leveraging the principles of green chemistry, the research aims to create recyclable and environmentally friendly heterogeneous catalytic systems. This aligns with the growing demand for greener technologies and the use of biocompatible materials in chemical processes.
View Article and Find Full Text PDFNano structural regulation of lignin and evaluation of its ultraviolet light absorption properties through quantum chemistry calculations.
Int J Biol Macromol
January 2025
Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Materials Science and Engineering, Nanjing Forestry University, Nanjing 210037, China.
Lignin, a biomass-derived material containing chromophores, possesses the potential to serve as a versatile organic ultraviolet (UV) light screening agent. By employing quantum chemical computation techniques, an amphoteric deep eutectic solvent (DES) based on sulfamic acid was purposefully designed and engineered to create a solvent system tailored for the nanoparticle formation and functionalization of lignin. As confirmed by experimental evidence, the size of the modified lignin nanoparticles (LNPs) varies from 168.
View Article and Find Full Text PDFPalladium-catalyzed [3 + 2] cycloaddition of 4-vinyl-4-butyrolactones with sulfamate-derived cyclic imines: construction of sulfamate-fused pyrrolidines.
Org Biomol Chem
December 2024
Department of Chemistry and Innovation Center of Pesticide Research, China Agricultural University, Beijing 100193, P. R. China.
The palladium-catalyzed [3 + 2] decarboxylative cycloaddition of 4-vinyl-4-butyrolactones with sulfamate-derived cyclic imines has been developed, providing the sulfamate-fused pyrrolidine derivatives in high yields with good diastereoselectivities. The scale-up reaction and further derivation of the product worked well, demonstrating the potential application of the current reaction in organic synthesis. A plausible reaction mechanism was also proposed.
View Article and Find Full Text PDFAsymmetric Construction of Chiral 2-Azetines and Axially Chiral Tetrasubstituted Allenes Via Phosphine Catalysis.
Angew Chem Int Ed Engl
January 2025
Department of Chemistry, China Agricultural University, 2 West Yuanmingyuan Road, Beijing, 100193, P. R. China.
Chiral 2-azetines and allenes are highly valuable structural units in natural products and useful chemicals. However, enantioselective synthesis of both 2-azetines and allenes has been extremely challenging. Herein, we present asymmetric construction of chiral 2-azetines (70-98 % yields and up to 96 % ee) through chiral phosphine-catalyzed [2+2] annulation of yne-enones with sulfamate-derived cyclic imines.
View Article and Find Full Text PDFSynthesis of furan-2-ones and spiro[furan-2,3'-indoline] derivatives using polyether sulfone sulfamic acid catalysis.
Sci Rep
October 2024
Department of Chemistry, College of Basic Sciences, Shahre Rey Branch, Yadegar-e- Imam Khomeini (RAH), Islamic Azad University, Tehran, Iran.
Polyether sulfone sulfamic acid (PES-NHSOH) was prepared by simple sulfonation of a modified polyether sulfone. The number of acidic sites (SOH) was determined to be 4.23 mmol H/g by acid-base titration and 4.
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!