European Journal of Medicinal Chemistry, Год журнала: 2022, Номер 247, С. 115026 - 115026
Опубликована: Дек. 21, 2022
Язык: Английский
RSC Advances, Год журнала: 2025, Номер 15(5), С. 3928 - 3953
Опубликована: Янв. 1, 2025
This review studies magnetically recoverable catalysts designed for the efficient multicomponent synthesis of organosulfur compounds. These enhance process by combining efficiency with environmental sustainability.
Язык: Английский
Процитировано
10
Tetrahedron, Год журнала: 2025, Номер 173, С. 134467 - 134467
Опубликована: Янв. 12, 2025
Язык: Английский
Процитировано
3
Pharmaceutics, Год журнала: 2022, Номер 14(11), С. 2538 - 2538
Опубликована: Ноя. 21, 2022
This review describes the recently FDA-approved drugs (in year 2022). Many of these products contain active moieties that FDA had not previously approved, either as a single ingredient or part combination. These frequently provide important new therapies for patients with multiple unmet diseases. The diverse small molecules are described according to date approval and their syntheses is discussed. comprises classical chemical scaffolds together innovative such deuterium-containing drug.
Язык: Английский
Процитировано
50
Nature Communications, Год журнала: 2023, Номер 14(1)
Опубликована: Июль 7, 2023
Abstract The sulfonamides (sulfas) are the oldest class of antibacterial drugs and inhibit bacterial dihydropteroate synthase (DHPS, encoded by folP ), through chemical mimicry its co-substrate p -aminobenzoic acid ( ABA). Resistance to sulfa is mediated either mutations in or acquisition sul genes, which code for sulfa-insensitive, divergent DHPS enzymes. While molecular basis resistance well understood, mechanisms mediating -based have not been investigated detail. Here, we determine crystal structures most common Sul enzyme types (Sul1, Sul2 Sul3) multiple ligand-bound states, revealing a substantial reorganization their ABA-interaction region relative corresponding DHPS. We use biochemical biophysical assays, mutational analysis, trans complementation E. coli Δ show that Phe-Gly sequence enables enzymes discriminate against sulfas while retaining ABA binding necessary broad sulfonamides. Experimental evolution results strain harboring sulfa-resistant variant carries insertion active site, recapitulating this mechanism. also possess increased site conformational dynamics DHPS, could contribute substrate discrimination. Our reveal foundation Sul-mediated drug facilitate potential development new less prone resistance.
Язык: Английский
Процитировано
43
Organic Letters, Год журнала: 2023, Номер 25(6), С. 1014 - 1019
Опубликована: Фев. 6, 2023
Alkyl sulfonamides are an important class of bioactive molecules. Historical syntheses have relied on multistep sequences incorporating harsh reaction conditions. Photochemical methods been limited to hydrosulfamoylation, installing only one substituent across olefin. Herein, radical/polar crossover (RPC) is used establish the first multicomponent 1,2-difunctionalization a sulfonamide moiety and second partner. This protocol, exemplified range olefins, utilizes various commercial sulfamoyl chlorides organotrifluoroborates as coupling partners.
Язык: Английский
Процитировано
30
Antibiotics, Год журнала: 2024, Номер 13(3), С. 271 - 271
Опубликована: Март 18, 2024
Infectious diseases are a significant challenge to global healthcare, especially in the face of increasing antibiotic resistance. This urgent issue requires continuous exploration and development new antimicrobial drugs. In this regard, secondary metabolites derived from endophytic microorganisms stand out as promising sources for finding antimicrobials. Endophytic microorganisms, residing within internal tissues plants, have demonstrated capacity produce diverse bioactive compounds with substantial pharmacological potential. Therefore, numerous been isolated endophytes, particularly fungi actinomycetes. However, only limited number these subjected comprehensive studies regarding their mechanisms action against bacterial cells. Furthermore, investigation effects on antibiotic-resistant bacteria identification biosynthetic gene clusters responsible synthesizing conducted subset compounds. Through analysis current research findings, review describes drugs antibacterial activities natural endophytes bacteria, synthesis metabolites.
Язык: Английский
Процитировано
18
European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 273, С. 116364 - 116364
Опубликована: Апрель 4, 2024
Язык: Английский
Процитировано
18
Saudi Pharmaceutical Journal, Год журнала: 2024, Номер 32(5), С. 102025 - 102025
Опубликована: Март 12, 2024
Based on previous developments of our research programs in trying to find new compounds with multiple biological targets such as antioxidant, anti-diabetic, anti-Alzheimer's, and anti-arthritic agents. In the context, a novel series sulfonamide derivatives based pyrazole or pyridine moieties 3a, b, 7–9, 11–13, 15a, 16 were synthesized from amine sulfonyl chloride derivatives. The structures elucidated via spectroscopy (1H 13C NMR). biologically assessed vitro for their anti-diabetic (α-amylase α-glucosidase inhibition) anti-Alzheimer's (acetylcholinesterase activities. results revealed that compound 15a is powerful enzyme inhibitor α-amylase α-glucosidase. Also, 15b demonstrated activity against acetylcholinesterase enzyme. structure–activity relationship study was accomplished. Furthermore, complementary silico molecular properties, drug-likeness, ADMET prediction, surface properties two more fulfilled computed. These studies recommend candidates modifications before vivo assays.
Язык: Английский
Процитировано
15
Environmental Geochemistry and Health, Год журнала: 2024, Номер 46(4)
Опубликована: Апрель 1, 2024
Язык: Английский
Процитировано
14
Journal of Molecular Structure, Год журнала: 2024, Номер 1312, С. 138554 - 138554
Опубликована: Май 6, 2024
Язык: Английский
Процитировано
11