92082-85-4Relevant academic research and scientific papers
Synthesis and molecular modelling studies of novel sulphonamide derivatives as dengue virus 2 protease inhibitors
Timiri, Ajay Kumar,Subasri, Selvarasu,Kesherwani, Manish,Vishwanathan, Vijayan,Sinha, Barij Nayan,Velmurugan, Devadasan,Jayaprakash, Venkatesan
, p. 74 - 82 (2015/08/11)
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.
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.
