Probing benzenesulfonamide-thiazolidinone hybrids as multitarget directed ligands for efficient control of type 2 diabetes mellitus through targeting the enzymes: α-glucosidase and carbonic anhydrase II
Eur J Med Chem. 2024 Apr 20;271:116434. doi: 10.1016/j.ejmech.2024.116434. Online ahead of print.ABSTRACTDiabetes mellitus is a chronic metabolic disorder characterized by improper expression/function of a number of key enzymes that can be regarded as targets for anti-diabetic drug design. Herein, we report the design, synthesis, and biological assessment of two series of thiazolidinone-based sulfonamides 4a-l and 5a-c as multitarget directed ligands (MTDLs) with potential anti-diabetic activity through targeting the enzymes: α-glucosidase and human carbonic anhydrase (hCA) II. The synthesized sulfonamides were evaluated ...
Source: European Journal of Medicinal Chemistry - April 23, 2024 Category: Chemistry Authors: Mona A Gamal Samar H Fahim Simone Giovannuzzi Marwa A Fouad Alessandro Bonardi Paola Gratteri Claudiu T Supuran Ghaneya S Hassan Source Type: research
Acute Myopic Shift after a Single Dose of Acetazolamide: A Case Report and Review of the Literature
We report the case of a 32-year-old male who presented with an acute myopic shift as a result of uveal effusion following a single administration of 250 mg acetazolamide. The drug was discontinued and following cycloplegia and topical steroid therapy, we observed progressive deepening of the anterior chamber, reopening of the iridocorneal angle, and complete resolution of the myopic shift after 5 days. A literature review since 1956 identified 23 cases, including ours, which developed a myopic shift after a median time of 24 h (3 - 24) following a median dose of 500 mg (125 - 1000) acetazolamide, with about a third complic...
Source: Klinische Monatsblatter fur Augenheilkunde - April 23, 2024 Category: Opthalmology Authors: Eirini Kaisari Hana Abouzeid Laurent Magnin Melanie Boeuf Evangelia Gkaragkani Ann Schalenbourg Thomas J Wolfensberger Pierre-Fran çois Kaeser Source Type: research
Probing benzenesulfonamide-thiazolidinone hybrids as multitarget directed ligands for efficient control of type 2 diabetes mellitus through targeting the enzymes: α-glucosidase and carbonic anhydrase II
Eur J Med Chem. 2024 Apr 20;271:116434. doi: 10.1016/j.ejmech.2024.116434. Online ahead of print.ABSTRACTDiabetes mellitus is a chronic metabolic disorder characterized by improper expression/function of a number of key enzymes that can be regarded as targets for anti-diabetic drug design. Herein, we report the design, synthesis, and biological assessment of two series of thiazolidinone-based sulfonamides 4a-l and 5a-c as multitarget directed ligands (MTDLs) with potential anti-diabetic activity through targeting the enzymes: α-glucosidase and human carbonic anhydrase (hCA) II. The synthesized sulfonamides were evaluated ...
Source: European Journal of Medicinal Chemistry - April 23, 2024 Category: Chemistry Authors: Mona A Gamal Samar H Fahim Simone Giovannuzzi Marwa A Fouad Alessandro Bonardi Paola Gratteri Claudiu T Supuran Ghaneya S Hassan Source Type: research
Nephrology: What You May Have Missed in 2023
This article highlights a selection of important nephrology studies published in 2023 that have relevance for nonnephrologist physicians. Four studies examined progression of chronic kidney disease or cardiovascular disease with respect to finerenone use, magnesium supplementation, iron markers, and COVID-19. Two studies examined treatments to improve specific aspects of chronic kidney disease management, including daprodustat to address anemia and patiromer to address hyperphosphatemia. One study showed that acetazolamide added to loop diuretics increased diuresis in acute decompensated heart failure across a wide range o...
Source: Annals of Internal Medicine - April 15, 2024 Category: Internal Medicine Authors: Ali A M AlHabobi Ashwaq M S Almutairi Danah A S Y Bohemid Ashwini R Sehgal Source Type: research
Nephrology: What You May Have Missed in 2023
This article highlights a selection of important nephrology studies published in 2023 that have relevance for nonnephrologist physicians. Four studies examined progression of chronic kidney disease or cardiovascular disease with respect to finerenone use, magnesium supplementation, iron markers, and COVID-19. Two studies examined treatments to improve specific aspects of chronic kidney disease management, including daprodustat to address anemia and patiromer to address hyperphosphatemia. One study showed that acetazolamide added to loop diuretics increased diuresis in acute decompensated heart failure across a wide range o...
Source: Annals of Internal Medicine - April 15, 2024 Category: Internal Medicine Authors: Ali A M AlHabobi Ashwaq M S Almutairi Danah A S Y Bohemid Ashwini R Sehgal Source Type: research
Nephrology: What You May Have Missed in 2023
This article highlights a selection of important nephrology studies published in 2023 that have relevance for nonnephrologist physicians. Four studies examined progression of chronic kidney disease or cardiovascular disease with respect to finerenone use, magnesium supplementation, iron markers, and COVID-19. Two studies examined treatments to improve specific aspects of chronic kidney disease management, including daprodustat to address anemia and patiromer to address hyperphosphatemia. One study showed that acetazolamide added to loop diuretics increased diuresis in acute decompensated heart failure across a wide range o...
Source: Annals of Internal Medicine - April 15, 2024 Category: Internal Medicine Authors: Ali A M AlHabobi Ashwaq M S Almutairi Danah A S Y Bohemid Ashwini R Sehgal Source Type: research
Nephrology: What You May Have Missed in 2023
This article highlights a selection of important nephrology studies published in 2023 that have relevance for nonnephrologist physicians. Four studies examined progression of chronic kidney disease or cardiovascular disease with respect to finerenone use, magnesium supplementation, iron markers, and COVID-19. Two studies examined treatments to improve specific aspects of chronic kidney disease management, including daprodustat to address anemia and patiromer to address hyperphosphatemia. One study showed that acetazolamide added to loop diuretics increased diuresis in acute decompensated heart failure across a wide range o...
Source: Annals of Internal Medicine - April 15, 2024 Category: Internal Medicine Authors: Ali A M AlHabobi Ashwaq M S Almutairi Danah A S Y Bohemid Ashwini R Sehgal Source Type: research
Spinocerebellar ataxia 27B (SCA27B), a frequent late-onset cerebellar ataxia
Rev Neurol (Paris). 2024 Apr 11:S0035-3787(24)00486-7. doi: 10.1016/j.neurol.2024.03.007. Online ahead of print.ABSTRACTGenetic cerebellar ataxias are still a diagnostic challenge, and yet not all of them have been identified. Very recently, in early 2023, a new cause of late-onset cerebellar ataxia (LOCA) was identified, spinocerebellar ataxia 27B (SCA27B). This is an autosomal dominant ataxia due to a GAA expansion in intron 1 of the FGF14 gene. Thanks to the many studies carried out since its discovery, it is now possible to define the clinical phenotype, its particularities, and the progression of SCA27B. It has also b...
Source: Revue Neurologique - April 12, 2024 Category: Neurology Authors: G Cl ément S Puisieux D Pellerin B Brais C Bonnet M Renaud Source Type: research
In silico study, synthesis, and antineoplastic evaluation of thiazole-based sulfonamide derivatives and their silver complexes with expected carbonic anhydrase inhibitory activity
This study aimed to design, synthesize, and evaluate the cytotoxic activity of novel thiazole-sulfanilamide derivatives, specifically compounds M3, M4, and M5, through molecular docking and biological assays. The synthesis utilized essential chemical compounds, including sulfanilamide, chloro-acetyl chloride, thiourea, derivatives of benzaldehyde, and silver nitrate. The docking study was carried out using Molecular Operating Environment (MOE) software, and cytotoxic activity was predicted by MTT assay. The synthesized compounds demonstrated a reduction in the viability of cancer cells. Compound M5 had an IC50 of 18.53 µg...
Source: Journal of Medicine and Life - April 8, 2024 Category: General Medicine Authors: Esraa Mahdi Naji Noor Hatef Naser Sahar Aqeel Hussein Source Type: research
