Inhibitory effects of sulfenimides on human and bovine carbonic anhydrase enzymes
A series of sulfenimide derivatives (1a-i) were investigated as inhibitors of human (hCA-I, hCA-II) and bovine (bCA) carbonic anhydrase enzymes. The compounds were synthesised by the reaction of substituted thiophenols with phthalimide by means of an ...
Hasan Yakan +12 more
doaj +1 more source
Conformational effects on the Circular Dichroism of Human Carbonic Anhydrase II: a multilevel computational study [PDF]
Circular Dichroism (CD) spectroscopy is a powerful method for investigating conformational changes in proteins and therefore has numerous applications in structural and molecular biology. Here a computational investigation of the CD spectrum of the Human
Uno Carlsson +27 more
core +1 more source
Discovery and validation of SIRT2 inhibitors based on tenovin-6 : use of a 1H-NMR method to assess deacetylase activity [PDF]
The search for potent and selective sirtuin inhibitors continues as chemical tools of this type are of use in helping to assign the function of this interesting class of deacetylases.
Pirrie, L +26 more
core +1 more source
Carbonic anhydrase (CA) inhibitors have a long history of safe clinical use as mild diuretics, in the treatment of glaucoma and for altitude sickness prevention.
Ejaife O. Agbani +6 more
doaj +1 more source
Carbonic anhydrase inhibitory properties of some uracil derivatives
Inhibitors of carbonic anhydrase (CA) have been carried out in many therapeutic applications, especially antiglaucoma activity. In this study, we investigated some uracil derivatives (4–12) to inhibit human CA I (hCA I) and II (hCA II) isoenzymes. The KI
Emir Alper Türkoğlu +3 more
doaj +1 more source
Click chemistry approaches for developing carbonic anhydrase inhibitors and their applications
Click chemistry reactions constitute an important and relatively new approach in the medicinal chemistry toolbox and offer substantial advantages to medicinal chemists in terms of overcoming the limitations of facile chemical synthesis, increased ...
Andrea Angeli, Claudiu T. Supuran
doaj +1 more source
High‐risk bladder cancer is typically treated with Bacillus Calmette‐Guérin (BCG), but 30–40% of patients relapse. No FDA‐ or CE‐approved biomarkers currently predict or prognosticate BCG failure. We systematically reviewed the literature and identified 72 eligible studies, revealing several promising biomarkers associated with BCG treatment response ...
Rui Ribeiro‐Pereira +7 more
wiley +1 more source
Identification of anti-cyanobacterial leads targeting carbonic anhydrase from phytochemical database using in silico approach [PDF]
In cyanobacteria, carbonic anhydrase (zinc metalloenzyme) is a major enzyme that converts CO 2 to HCO 3- main¬taining the carbon concentration around the vicinity of RuBisCo, leading to cyanobacterial biomass generation.
Mir, Showkat A. +9 more
core +1 more source
Click‐to‐release (C2R) chemistry is redirected from payload liberation toward ligand‐directed covalent protein labeling through a transient dihydropyridazine methide (DHP‐methide). This concept opens the way to dual‐functional systems combining covalent target engagement with controlled effector release.
Dóra Kern +9 more
wiley +2 more sources
SYNTHESIS, BIOCHEMICAL AND IN SILICO EXPLORATION OF NOVEL IMIDAZOLE BASED 1,2,3-TRIAZOLES AS POTENTIAL HIT AGAINST CARBONIC ANHYDRASE II ISOZYME [PDF]
This study aimed to synthesize novel compounds as more effective carbonic anhydrase II inhibitors. For this purpose, 2-(3-methoxy-4-(prop-2-yn-1-yloxy)phenyl)-4,5-diphenyl-1H-imidazole (3) was reacted with 3-methoxy-4-(prop-2-yn-1-yloxy)benzaldehyde ...
Mumtaz Hussain +12 more
doaj +1 more source

