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 effective, simple and eco-friendly method and the structures were confirmed by IR, H NMR, C NMR, MS and elemental analysis. All derivatives except for the methyl derivative () exhibited effective inhibitory action at low micromolar concentrations on human isoforms, but only four derivatives (, , , ) inhibited the bovine enzyme.

Detection of hip osteoarthritis by using plain pelvic radiographs with deep learning methods.

Objective: The incidence of osteoarthritis is gradually increasing in public due to aging and increase in obesity. Various imaging methods are used in the diagnosis of hip osteoarthritis, and plain pelvic radiography is the first preferred imaging method in the diagnosis of hip osteoarthritis. In this study, we aimed to develop a computer-aided diagnosis method that will help physicians for the diagnosis of hip osteoarthritis by interpreting plain pelvic radiographs.

Synthesis and characterization of some new pyrazolines and their inhibitory potencies against carbonic anhydrases.

The inhibition of the two human cytosolic carbonic anhydrase (hCA; EC 4.2.1.

Design, synthesis, characterization of peripherally tetra-pyridine-triazole-substituted phthalocyanines and their inhibitory effects on cholinesterases (AChE/BChE) and carbonic anhydrases (hCA I, II and IX).

In this study, phthalocyanine precursors (5 and 9) and 1,2,3-triazole-substituted metal-free and metallo phthalocyanines (9a-c) were designed and synthesized for the first time and evaluated in vitro for key molecular targets. The structures of the novel compounds were characterized via FT-IR, H/C NMR, UV-Vis, and mass spectroscopy. The inhibitory activities of the compounds were tested against human carbonic anhydrase isoforms hCA I, II (cytosolic, ubiquitous isozymes), and IX (transmembrane, cancer-associated isozyme) and cholinesterases (AChE and BChE, which are associated with Alzheimer's disease).

Design, synthesis and molecular modelling studies of some pyrazole derivatives as carbonic anhydrase inhibitors.

In this study, newly synthesised compounds , , and other compounds (, and ) and their inhibitory properties against the human isoforms hCA I and hCA II were reported for the first time. Compounds showed effective inhibition profiles with values in the range of 5.13-16.

Triazole substituted metal-free, metallo-phthalocyanines and their water soluble derivatives as potential cholinesterases inhibitors: Design, synthesis and in vitro inhibition study.

In this study, 1,2,3-triazole substituted metal-free and metallo phthalocyanines (4, 5, 6) and their water soluble derivatives (4a, 5a, 6a) were designed, synthesized for the first time and tested in vitro on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Most phthalocyanines exhibited good inhibitory activities on these enzymes. Among the six phthalocyanines and starting compounds, 4a showed the most interesting profile as a submicromolar selective inhibitor of AChE (IC = 0.

The synthesis of axially disubstituted silicon phthalocyanines, their quaternized derivatives and first inhibitory effect on human cytosolic carbonic anhydrase isozymes hCA I and II.

In this study a novel silicon(iv) phthalocyanine bearing [(2)-3-[4-(dimethylamino)phenyl]-1-(4-phenoxy)prop-2-en-1-one] group and its quaternized derivative at their axial positions were synthesized for the first time. Axially disubstituted silicon(iv) phthalocyanines were also characterized by various spectroscopic techniques. The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.

Synthesis and carbonic anhydrase inhibitory properties of novel chalcone substituted benzenesulfonamides.

Carbonic anhydrases (CAs, EC 4.2.1.

Synthesis and Biological Evaluation of Novel Bischalcone Derivatives as Carbonic Anhydrase Inhibitors.

Design and synthesis of a new type of bischalcones as an alternative to natural and synthetic bischalcones are reported for the first time. Key steps involved the solvent-free Claisen-Schmidt condensation of chalcones, and the successful first application of the diazotization-diazocoupling reaction in the synthesis of CNNC-linked bischalcones by simple structural modification of p-aminoacetophenone. The structures of all compounds were confirmed by means of FT-IR, (1) H and (13) C NMR, ESI/MS, and elemental analysis.

An effect of the substituent position and metal type on the electropolymerization properties of chalcone substituted metallophthalocyanines.

Cobalt(II) and manganese(III) phthalocyanines bearing peripherally and non-peripherally tetra substituted {(2E)-3-[4-(dimethylamino)phenyl]prop-2-enoyl}phenoxy groups were synthesized by cyclotetramerization of the phthalonitrile derivatives and their electrochemical properties were examined using CV and SWV techniques for the first time. The novel compounds were characterized by using IR, (1)H-NMR, (13)C-NMR, UV-Vis and MS spectral data. Cyclic and square wave voltammetry revealed well-defined metal-based and ligand-based reduction processes within the complexes.