- Chromene-containing aromatic sulfonamides with carbonic anhydrase inhibitory properties
-
Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. A series of chromene-based sulfonamides were synthesized and tested as possible CA inhibitors. Their inhibitory activity was assessed against the cytosolic human isoforms hCA I, hCA II and the transmembrane hCA IX and XII. Several of the investigated derivatives showed interesting inhibition activity towards the tumor associate isoforms hCA IX and hCA XII. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds, within the active site of hCA IX.
- Angeli, Andrea,Kartsev, Victor,Petrou, Anthi,Pinteala, Mariana,Brovarets, Volodymyr,Slyvchuk, Sergii,Pilyo, Stepan,Geronikaki, Athina,Supuran, Claudiu T.
-
-
- SUBSTITUTED CYCLOLAKYLS AS MODULATORS OF THE INTEGRATED STRESS PATHWAY
-
Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.
- -
-
Page/Page column 255; 305
(2020/11/12)
-
- Optimizing the synthetic route of chromone-2-carboxylic acids: A step forward to speed-up the discovery of chromone-based multitarget-directed ligands
-
6-Bromochromone-2-carboxylic acid (3) was synthesized by a microwave-assisted process. The optimization of the reaction was performed varying parameters, such as type of base/number of reagent equivalents, solvent, temperature and reaction time. The yield of the reaction was improved to 87%. The new synthetic route is versatile as several chromone-2-carboxylic acids (compounds 4B-10B) were obtained with good yields (54-93%). Only in the case of the nitro substituent (compound 11B), an ester was obtained instead of the desired carboxylic acid. Following this synthetic route chromone carboxylic acids can be attained with a high degree of purity, without the need of the tedious and expensive purification processes through column chromatography. The reaction is safe, cost-effective, fast and robust, and can be used in the development of concise and diversity-oriented libraries based on chromone scaffold. The overall study can be looked as a step forward to speed-up the discovery of chromone-based multitarget-directed ligands.
- Cagide, Fernando,Oliveira, Catarina,Reis, Joana,Borges, Fernanda
-
-
- Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof
-
Compounds that are antagonists of the VR1 receptor, having formula (I) [image] or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
- -
-
Page/Page column 57
(2008/06/13)
-
- Synthesis and Reactions of Some 4-Oxo-4H-1-benzopyran-2-carboxaldehydes
-
Some new 4-oxo-4H-1-benzopyran-2-carboxaldehydes (III) have been prepared, and the conversion of the 2-carboxaldehyde group in III into 2-carbonitrile and 2-carboxylic acid groups has been discussed.Unlike the general behaviour of the 4-oxo-4H-1-benzopyrans towards some nucleophiles, where the reaction takes place with opening of the pyronering, the 6-methyl- and 6-chloro-4-oxo-4H-1-benzopyran-2-carboxaldehydes (IIIa and IIIb) have been found to react with different nucleophiles such as hydroxylamine hydrochloride, hydrazine, phenylhydrazine and primary aromatic amines to give the corresponding condensation products (IV, VII, VIII, X, XI) without the opening of pyrone ring.The only exception to this observation is the reaction of IIIa and IIIb with ethylene diamine where the opening of pyronering does not take place to give the expected 5,6-dihydropyrazine derivatives (XIIa and XIIb).The reactions of IIIa and IIIb with active methylene compounds, malonic acid, malonodinitrile, cyanoacetic acid, ethyl cyanoacetate, cyanoacetamide and hippuric acid have also been discussed.
- Sami, S. M.,Ibrahim, S. S.,Abdel-Halim, A. M.,Aly, Y. L.
-
p. 384 - 389
(2007/10/02)
-