4435-59-0

Upstream product

• 520-03-6 N-phenylphthalimide 
• 86581-47-7 4-(1,3-dioxoisoindolin-2-yl)benzenesulfonic acid 
• 62-53-3 aniline 
• 85-44-9 phthalic anhydride 

Downstream Products

• 36340-59-7 4-(1,3-dioxoisoindolin-2-yl)-N-(2-thiazolyl)benzenesulfonamide 
• 40266-18-0 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-pyridin-2-yl benzenesulfonamide 
• 396135-20-9 N-(N,N-phthaloyl-sulfanilyl)-sulfanilic acid amide 
• 111721-80-3 4-(1,3-dioxoisoindolin-2-yl)-N-phenylbenzenesulphonamide 
• 4479-70-3 4-(1,3-dioxobenzo[c]azolidin-2-yl)benzenesulfonamide 
• 92082-86-5 2-[4-(1,4-oxazinan-4-ylsulfonyl)phenyl]-1,3-isoindolinedione 
• 136918-14-4 phthalimide 
• 63-74-1 sulfanilamide 
• 1333313-44-2 N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-4-(1,3-dioxoisoindolin-2-yl)-N-isobutylbenzenesulfonamide hydrochloride 
• 1394345-33-5 C₂₄H₁₈N₄O₉S₂ 

Relevant academic research and scientific papers

Synthesis and anti-inflammatory activity of phthalimide derivatives, designed as new thalidomide analogues.

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.

SMALL MOLECULE DIRECT INHIBITORS OF KEAP1-NRF2 PROTEIN-PROTEIN INTERACTION

This patent document diclsoes novel compounds and methods of preventing or treating diseases or conditions related to Keapl-Nrf2 interaction activity by use of the novel compounds. As direct inhibitors of Keapl-Nrf2 interaction, the compounds disclosed herein are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential dmg candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, Parkinson's, and inflammatory bowel disease including ulcerative colitis.

A NOVEL PROCESS FOR THE PREPARATION OF HIV PROTEASE INHIBITOR AND INTERMEDIATES THEREOF

The present invention relates to process for the preparation of Darunavir or a solvate thereof of Formula (I) using a novel intermediate (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (2S,3R)-4-(4-(1,3-dioxoisoindolin-2-yl)-N-isobutylphenylsulfonamido)-3 -hydroxy- 1 -phenylbutan-2- ylcarbamate Compound of formula (II): The present invention also relates to the process for the preparation of novel intermediates (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (2S,3R)-4-(4-(l,3-dioxo iso indolin-2-yl)-N-isobutylphenylsulfonamido)-3 -hydroxy-1-phenylbutan-2-ylcarbamate Compound of formula (II). Darunavir or its solvate of formula (I) are useful therapeutic agent and used in treatment of antiviral diseases.

Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors

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 molecular modelling studies of novel sulphonamide derivatives as dengue virus 2 protease inhibitors

Abstract Development of antivirals for dengue is now based on rational approach targeting the enzymes involved in its life cycle. Among the targets available for inhibition of dengue virus, non-structural protein NS2B-NS3 protease is considered as a promising target for the development of anti-dengue agents. In the current study we have synthesized a series of 4-(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)benzene-1-sulphonamide derivatives and screened for DENV2 protease activity. Compounds 16 and 19 showed IC50 of DENV2 Protease activity with 48.2 and 121.9 μM respectively. Molecular docking and molecular dynamic simulation studies were carried out to know the binding mode responsible for the activity. MD simulations revealed that, NS2B/NS3 protease was more stable when it binds with the active compound. Structure optimization of the lead compounds 16 and 19 and their co-crystallization studies are underway.

Design, synthesis, and pharmacological evaluation of novel hybrid compounds to treat sickle cell disease symptoms. Part II: Furoxan derivatives

Phthalimide derivatives containing furoxanyl subunits as nitric oxide (NO)-donors (3a-g) were designed, synthesized, and evaluated in vitro and in vivo for their potential uses in the oral treatment of sickle cell disease symptoms. All compounds (3a-g) demonstrated NO-donor properties at different levels. Moreover, compounds 3b and 3c demonstrated analgesic activity. Compound 3b was determined to be a promising drug candidate for the aforementioned uses, and it was further evaluated in K562 culture cells to determine its ability to increase levels of γ-globin expression. After 96 h at 5 μM, compound 3b was able to induce γ-globin expression by nearly three times. Mutagenic studies using micronucleus tests in peripheral blood cells of mice demonstrated that compound 3b reduces the mutagenic profile as compared with hydroxyurea. Compound 3b has emerged as a new leading drug candidate with multiple beneficial effects for the treatment of sickle cell disease symptoms and provides an alternative to hydroxyurea treatment.

Derivatives of Cinnamide-4-sulfonyl Chloride and p-(Phthalimido)benzenesulfonyl Chloride

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.