92082-86-5Relevant academic research and scientific papers
Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
Soyer, Zeynep,Uysal, Sirin,Parlar, Sulunay,Tarikogullari Dogan, Ayse Hande,Alptuzun, Vildan
, p. 13 - 19 (2017/11/22)
A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman’s colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE. Among the tested compounds, compound 7 was found to be the most potent against AChE (IC50= 1.35 ± 0.08 μM), while compound 3 exhibited the highest inhibition against BuChE (IC50= 13.41 ± 0.62 μM). Molecular docking studies of the most active compound 7 in AChE showed that this compound can interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE.
Synthesis and anti-inflammatory activity of phthalimide derivatives, designed as new thalidomide analogues.
Lima, Lidia M,Castro, Paulo,Machado, Alexandre L,Fraga, Carlos Alberto M,Lugnier, Claire,de Moraes, Vera Lucia Goncalves,Barreiro, Eliezer J
, p. 3067 - 3073 (2007/10/03)
This paper describes the synthesis and anti-inflammatory activity of new N-phenyl-phthalimide sulfonamides (3a-e) and the isosters N-phenyl-phthalimide amides (4a-e), designed as hybrids of thalidomide (1) and aryl sulfonamide phosphodiesterase inhibitor (2). In these series, compound 3e (LASSBio 468), having a sulfonyl-thiomorpholine moiety, showed potent inhibitory activity on LPS-induced neutrophil recruitment with ED(50)=2.5mg kg(-1), which was correlated with its inhibitory effect on TNF-alpha level.
Derivatives of Cinnamide-4-sulfonyl Chloride and p-(Phthalimido)benzenesulfonyl Chloride
Cremlyn, R. J.,Thandi, K.,Wilson, R.
, p. 94 - 96 (2007/10/02)
Cinnamide and N-phenylsuccinimide have been chlorosulfonated and the corresponding sulfonyl chlorides condensed with nucleophilic reagents to give the sulfonyl derivatives (3-29).The azides (15,27) react with phosphorus(III) compounds to form the phosphinimines (17-19,29-30). p-Phthalimidobenzenesulfonyl chloride condenses with 2 mol of dimethylamine to give the dimethylamide (20); with 4 mol of the amine, cleavage of the imido ring occurs to give the bis-dimethylamide (31).The compounds prepared have been screened against the bacteria Esch. coli and Staph. aureus, and against the fungus Botrytis cinerea.
