Synthesis, spectral characterization and enzyme inhibition studies of different chlorinated sulfonamides

Sulfonamides are adherent to a biologically dynamic category of compounds and are under consideration of many organic synthetic researches to synthesize pharmacologically important compounds. In this demonstrated research work, a benignant series of chlorinated sulfonamides were synthesized and screened against different enzymes. These various chlorinated sulfonamides [3a-i] were set up by pairing of different substituted anilines [2a-i] with 4-chlorobenzenesulfonyl chloride [1] under basic pH in an aqueous media. The structures of the synthesized chlorinated sulfonamides were furnished by [1] H-NMR, IR and EI-MS. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were urease, butyrylcholinesterase [BChE] and lipoxygenase [LOX]. All the compounds exhibited good inhibitory activities against these enzymes but the strong activity was shown against BChE and hence can be employed for discovery of 'lead' compounds against Alzheimer's disease [AD]

Synthesis, characterization and enzyme inhibition study of O-substituted derivatives of chlorinated coumarin

Coumarins have much importance in dyes, drugs, perfumes and pesticides. In the demonstrated research work, a benignant series of chlorinated coumarins was synthesized and screened against different enzymes. First, 6-Chloro-7-hydroxy-4-methyl-2H-chromen-2-one [3] was geared up by the reaction of 4-chlororesorcinol [1] and ethyl acetoacetate [2] in the presence of concentrated H[2]SO[4]. Second, various O-substituted derivatives of chlorinated coumarins, 5a-j, were set up by pairing different alkyl/aralkyl halides, 4a-j, with 3 in the presence of NaH in DMF as solvent. The structures of all the synthesized compounds were clarified through spectral analysis using EI-MS, IR and [1]H-NMR. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were acetyl cholinesterase [AChE], butyryl cholinesterase [BChE] and lipoxygenase [LOX]. The most proficient activity was shown against both cholinesterase enzymes