Alzheimer__ampersandsignrsquo;s disease (AD) is a progressive age-related neurodegenerative disorder and is the most common form of dementia among the elderly (65 years). The main pathological hallmarks of AD are the accumulation of amyloid plaques, or senile plaques, containing extracellular deposits of amyloid-__ampersandsignbeta; peptide (A__ampersandsignbeta;) and the presence of intraneuronal neurofibrillary tangles (NFTs), which result from hyperphosphorylated tau-protein. While preparing this review article, a huge collection of published literature from diverse pharmaceutical databases, life science databases, and medical databases such as PubMed, ScienceDirect, Google Scholar, etc. were explored and the literature was classified duly. The article focuses on various cholinesterase inhibitors obtained from diverse sources or categories such as established synthetic inhibitors (Physostigmine, Tacrine, Donepezil, Rivastigmine, Galantamine, and Metrifonate), novel synthetic inhibitors (Phenserine, Tolserine, Tesofensine, and Esolerine), natural inhibitors (Huperzine A, Neferine, Galangin, and Cardanol), synthetic hybrid derivatives (Donepezil and AP2238; Donepezil-Tacrine Hybrid; Tacrine-Ferulic acid Hybrid and Beta Carboline Derivatives; and Tacrine-8-hydroxyquinoline Hybrid), and new experimental synthetic analogues (Phenyl-5,6-dimethoxy-1-oxo-2,3-dihydro-1H-2-indenylmethanone and N-alkyl-7-methoxymatrine). This interesting piece of literature may serve as a readymade reference text material (particularly molecular-weight inhibitors) to the enthusiastic researchers (pharmacologists and medicinal chemists) working delicately in the area of AD. This study will positively open novel opportunities for research and futuristic pharmacotherapeutic application perceptive.