الفهرس 
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Abstract
Abstract
Design, synthesis and computational studies of biologically active nitrogen-containing heterocycles
The original research is directed towards design and synthesis of novel heterocyclic agents containing nitrogen. These agents are set to investigate their biological properties against serious diseases namely, cancer, Alzheimer’s disease and anti-SARS-CoV-2.
A series of 3,5-di[(E)-arylidene]-1-[3-(4-methylpiperazin-1-yl)alkyl]piperidin-4-ones were synthesized through dehydrohalogenation of 1-(2-chloroacyl)piperidin-4-ones with N-methylpiperazine . Most of the synthesized agents exhibited high antiproliferative properties against colon (HCT116) and breast (MCF7) cancer cell lines relative to standard references (sunitinib and 5-fluorouracil). The synthesized agents reveal inhibitory activity against both topoisomerases I and IIα with higher efficacy against topoisomerase IIα rather than topoisomerase I.
Some of the synthesized agents also showed antiviral properties against SARS-CoV-2 with efficacy compared to favipiravir.
A set of dispiro[indoline-3,2’-pyrrolidine-3’,3’’-pyrrolidines] were regioselectively synthesized through dipolar cycloaddition reaction of isatins and sarcosine in ethanol with 3-(arylmethylidene)pyrrolidine-2,5-diones . Single crystal X-ray studies supported the structure. Cholinesterase inhibition properties were observed by some of the
Abstract
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synthesized agents with selectivity index towards AChE over BChE as in Donepezil (clinically used cholinesterase inhibitory drug).
Molecular modeling studies determined the parameters regulating the biological observations.