A series of novel thiophene pyrazolines were designed as potential bioactive molecules against Alzheimer’s disease. The probable binding modes of these molecules in AChE were evaluated by in silico techniques and promising molecules were then synthesized, characterized and biological activities were profiled to confirm their potential as multifunctional molecules for Alzheimer therapeutics addressing multiple pathological mechanisms. While the anti-oxidant activities of the synthesized molecules needs further optimization, the series as such showed excellent potential in mitigating the multiple causative factors viz Aβ aggregation inhibition, AChE inhibition, metal chelation and inhibition of advanced glycation products.