1. Synthesis and biological evaluation of strained unusual amino acid containing tetrapeptides as potential antidepressant agents
- Author
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Libi Anandi Vishwanathan, Bathini Nagendra Babu, Lenin Veeraval, Karisetty Bhanu Chandra, Sumana Chakravarty, Prathama S. Mainkar, Takkallapally Srujana, and Santosh Kumar Prajapti
- Subjects
Neurite ,Stereochemistry ,Biochemistry ,Molecular Docking Simulation ,Mice ,Structure-Activity Relationship ,In vivo ,Cell Line, Tumor ,Drug Discovery ,Animals ,Structure–activity relationship ,Amino Acids ,Molecular Biology ,chemistry.chemical_classification ,Oligopeptide ,Dose-Response Relationship, Drug ,Molecular Structure ,Organic Chemistry ,Antidepressive Agents ,In vitro ,Amino acid ,Neuroprotective Agents ,chemistry ,Oligopeptides ,Behavioural despair test - Abstract
Strained unusual amino acid derived tetrapeptides were synthesized as mimics of GLYX-13, a clinical candidate for neuroprotective and anti-depressant properties, were studied. The synthesized compounds were screened for neurite growth and anti-depressant properties in vitro and in vivo respectively comparing with the parent GLYX-13 compound. Neurite growth property was assessed by neurite length and anti-depressant property by percentage of immobility in forced swim test, a behavioural assay. Mechanistic insights about protein-ligand interactions were obtained using molecular docking study. Based on the in vitro and in vivo screening data and molecular docking study, a new analogue of GLYX-13, Compound 11a has been found to be as good as the parent compound in all respects.
- Published
- 2015