Publications by authors named "Sakesh Kumar"
Article Synopsis
- Dopamine receptors are being targeted for treating neurological disorders like Parkinson's and Alzheimer's, with a focus on developing selective D5 receptor agonists.
- Researchers designed and tested forty new pyrimidine derivatives, finding four that act as selective partial agonists for the D5 receptor, with compound 5j showing the most promising activity.
- Compound 5j demonstrated stability and the ability to improve memory in mice without toxicity, suggesting it could be a viable therapeutic option for cognitive impairment.
The synthesis of 5-formyl-6-aryl-6H-indolo[3,2,1-de][1,5] naphthyridine-2-carboxylates by reaction between 1-formyl-9H-β-carbolines and cinnamaldehydes in the presence of pyrrolidine in water with microwave irradiation is described. Pharmacophoric modification of the formyl group offered several new fused β-carboline derivatives, which were investigated for their κ-opioid receptor (KOR) agonistic activity. Two compounds 4 a and 4 c produced appreciable agonist activity on KOR with EC values of 46±19 and 134±9 nM, respectively.
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