Heterocycles and their derivatives hold an important place in medicinal chemistry due to
their vast therapeutic and pharmacological significance and wider implications in drug design and
development. Piperidine is a nitrogen-containing heterocyclic moiety that exhibits an array of
pharmacological properties. This review discusses the potential of piperidine derivatives against the
neurodegenerative disease Alzheimer’s. The incidences of Alzheimer’s disease are increasing nowadays, and constant efforts are being made to develop a medicinal agent for this disease. We have
highlighted the advancement in developing piperidine-based anti-neuronal disease compounds and
the profound activities of some major piperidine-bearing drug molecules with their important target site.
This review focuses on advancements in the field of natural and synthetic occurring piperidines active against Alzheimer’s disease, with emphasis on the past 6 years. The discussion also includes
the structure-activity relationship, the structures of the most promising molecules, and their biological activities against Alzheimer’s disease. The promising activities revealed by these piperidinebased scaffolds undoubtedly place them at the forefront of discovering prospective drug candidates.
Thus, it would be of great interest to researchers working on synthesizing neuroprotective drug candidates.
Glycogen synthase kinase-3 (GSK-3) is a multifunctional serine/threonine (ser/thr) kinase that was originally identified as a regulator of glycogen metabolism and coupled with insulin signaling. Due to multifunctionality of this enzyme, it is found to play an important role in the onset and progression of various human diseases. Thiazole nucleus has received special attention by medicinal chemists because of its wide therapeutic potential. The objective of this review is to cover all the aspects of GSK-3β enzyme including its clinical implications, types of inhibitors with special reference to thiazole as GSK-3β inhibitor. Literature search was performed using Pubmed/Medline and Google Scholar to search for articles published in English language.
In the present study, novel 4‐aryloxyquinazoline derivatives were synthesized and screened for in vitro cytotoxicity on human cancer cell lines at 10 μM. Some of the synthesized compounds displayed moderate to significant and selective cytotoxic activity against various leukemia, melanoma, ovarian, breast, and colon cancer cell lines. (E)‐3‐(3,4‐Dimethoxyphenyl)‐1‐(4‐(quinazolin‐4‐yloxy)phenyl)prop‐2‐en‐1‐one (9b) was the most potent compound among all with an average growth inhibition of 70% against leukemia cancer cell lines. The compound also produced strong inhibition (75%) of colon cancer cell lines with 42.58% lethality of HCT‐116 cell line.
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