A5070890722- Enzyme function and inhibition
- Synthesis and Catalytic Reactions
- Synthesis and biological activity
- Phenothiazines and Benzothiazines Synthesis and Activities
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Characterization of Heterocyclic Compounds
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Crystal structures of chemical compounds
- Chemical Reactions and Mechanisms
- Synthesis and Biological Evaluation
- Cancer therapeutics and mechanisms
- Quinazolinone synthesis and applications
- Tuberculosis Research and Epidemiology
- Organometallic Compounds Synthesis and Characterization
- Metal complexes synthesis and properties
- Renin-Angiotensin System Studies
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Analytical Methods in Pharmaceuticals
- Biochemical Acid Research Studies
- Bioactive Compounds and Antitumor Agents
- Analytical Chemistry and Chromatography
- Digestive system and related health
- Piperaceae Chemical and Biological Studies
- Synthesis of heterocyclic compounds
Istanbul University
2011-2024
University of Florence
2008-2020
Orient-Institut Istanbul
2015
Texas A&M University at Galveston
2009
A series of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides has been derivatized by reaction with 2,4,6-trimethylpyrylium perchlorate, leading to pyridinium derivatives. The new sulfonamides were evaluated as inhibitors two β-carbonic anhydrases (CAs, EC 4.2.1.1) from Mycobaterium tuberculosis, Rv1284 and Rv3273. whole showed excellent nanomolar inhibitory activity, several subnanomolar being detected. Rv3273 have potential for developing antimycobacterial agents an alternate mechanism action.
Trypanosoma cruzi, the causative agent of Chagas disease, encodes for an α-carbonic anhydrase (CA, EC 4.2.1.1) possessing high catalytic activity (TcCA) which was recently characterized (Pan et al. J. Med. Chem. 2013, 56, 1761-1771). A new class sulfonamides low nanomolar/subnanomolar TcCA inhibitory is described here. Aromatic/heterocyclic incorporating halogeno/methoxyphenacetamido tails inhibited with KIs in range 0.5-12.5 nM, being less effective against human off-target isoforms hCA I...
A series of 2/3/4-[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)amino]benzenesulfonamides, obtained from substituted isatins and 2-, 3- or 4-aminobenzenesulfonamide, showed low nanomolar inhibitory activity against the tumor associated carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX XII - recently validated antitumor drug targets, being much less effective as inhibitors off-target cytosolic CA I II.
Carbonic anhydrases (CAs) are widespread metalloenzymes with the core function of catalyzing interconversion CO
Novel sulfonamidoindole-based hydrazones with a 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide scaffold were synthesized and tested in enzyme inhibition assays against the tumor-associated carbonic anhydrase isoforms, hCA IX XII, off-targets, I II. The compounds showed selectivity XII over Six KI values lower than 10 nM or XII. Molecular modeling studies performed to suggest binding interactions between ligand active sites.
In our efforts to find new and selective thiazolidinone-based anti-Candida agents, we synthesized tested 26 thiazolidinones against several Candida spp. Gram-positive Gram-negative bacteria. The compounds showed antifungal activity with potency similar fluconazole clotrimazole, while lacking strong antibacterial activity. Molecular docking molecular dynamics studies were performed on CYP51a1 carbonic anhydrase (CA) enzymes further suggest putative targets that could mediate the effects of...
A small collection of 26 structurally novel thiazolidinone-containing compounds, without the well-known sulphonamide zinc-binding group, were synthesised and tested in enzyme inhibition assays against tumour-associated hCA IX enzyme. Inhibition constants lower micromolar region (KI < 25 μM) have been measured for 17 compounds. Even though KI values are relatively weak, fact that they do not contain a moiety suggests these compounds interact with active site zinc ion. Therefore, docking...