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The modulatory role of extracellular nucleotides and adenosine in relevance to purinergic cell signaling mechanisms has long been known and is an object of much research worldwide. These extracellular nucleotides are released by a variety of cell types either innately or as a response to patho-physiological stress or injury. A variety of surface-located(More)
Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes which are ubiquitous in nature and are found in a variety of organisms. In mammals at least 16 different isozymes of CAs have been found. CAs catalyze the reversible hydration of carbon dioxide to bicarbonate with the release of protons. Abnormal levels and/or activities of these enzymes have been(More)
Computational tools of analysis were used on a set of synthetic chromone containing sulfonamide derivatives for evaluation of their enzyme inhibitory activity against Carbonic Anhydrase (CA) isozymes. GOLD docking software was utilized to dock the compounds against two human Carbonic Anhydrase (hCA) proteins; hCAII and hCA-IX. Differences in conformation(More)
A series of 1-aroyl-3-(4-aminosulfonylphenyl)thioureas containing free sulfonamide group has been evaluated for their ability to inhibit bovine carbonic anhydrase II (bCA, EC 4.2.1.1). All compounds in the series were able to inhibit bCA II, the most active inhibitor had IC50 value of 0.26 ± 0.01 µM. Molecular docking studies and detailed structure-activity(More)
INTRODUCTION Schiff bases are synthetically accessible and structurally diverse compounds, typically obtained by facile condensation between an aldehyde, or a ketone with primary amines. Schiff bases contain an azomethine (-C = N-) linkage that stitches together two or more biologically active aromatic/heterocyclic scaffolds to form various molecular(More)
An efficient and environmentally benign simple fusion reaction of 3-chloro-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine (1a) or 3-chloro-6-(3,5-dimethyl-4-nitro-1H-pyrazol-1-yl)pyridazine (2a) with different aliphatic/aromatic amines have produced a series of novel pyrazolylpyridazine amines (4a-4c &5a-5m). All compounds exhibited moderate in vitro yeast(More)
A library of coumarin derived sulfonyl esters (1-38) was synthesized by reacting various hydroxy coumarins with different alkyl and aryl sulfonyl chlorides. All compounds were evaluated for their potential to inhibit alkaline phosphatases (hTNAP and hIAP). Most of the compounds were found to be inhibitors of APs. Compound 20 was found to be the most active(More)
In the title compound, C(16)H(11)FN(2)O(4)S, the mean planes of the bicyclic chromone system and of the benzene ring of the benzothia-diazine derivative make a dihedral angle of 54.28 (5)°. An intra-molecular N-H⋯O hydrogen bond occurs. In the crystal, mol-ecules are linked into layers by N-H⋯O and C-H⋯O hydrogen bonds, generating an infinite(More)
The mol-ecular structure of the title compound, C(16)H(11)BrN(2)O(4)S, is very similar to that of the previously reported fluoro analogue [al-Rashida et al. (2010 ▶). Acta Cryst. E66, o2707]. The mean planes of the bicyclic chromone system and the benzene ring of the benzothia-diazine derivative make a dihedral angle of 58.23 (8)°. An intra-molecular N-H⋯O(More)
Series of chromone containing sulfonamides were prepared by the reaction of (un)substituted 3-formylchromones with 3-aminobenzenesulfonamide and 4-aminobenzenesulfonamide. Bovine carbonic anhydrase (bCA) inhibitory activity of these newly synthesized compounds was determined. All compounds were active and possessed excellent bCA inhibitory activities with(More)