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Bioorg Chem ; 63: 53-7, 2015 Dec.
Article in English | MEDLINE | ID: mdl-26433904

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.


Subject(s)
Amino Acids/pharmacology , Antidepressive Agents/chemistry , Antidepressive Agents/pharmacology , Neuroprotective Agents/chemistry , Neuroprotective Agents/pharmacology , Oligopeptides/pharmacology , Amino Acids/chemistry , Animals , Antidepressive Agents/chemical synthesis , Cell Line, Tumor , Dose-Response Relationship, Drug , Mice , Molecular Docking Simulation , Molecular Structure , Neuroprotective Agents/chemical synthesis , Oligopeptides/chemical synthesis , Oligopeptides/chemistry , Structure-Activity Relationship
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