title: Synthesis and biological evaluation of strained unusual amino acid containing tetrapeptides as potential antidepressant agents.
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.
authors.affiliation: Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Prathama S
authors.initials: PS
authors.lastname: Mainkar
authors.affiliation: Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Sumana
authors.initials: S
authors.lastname: Chakravarty
authors.affiliation: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Balanagar, Hyderabad 500037, India.
authors.forename: Takkallapally
authors.initials: T
authors.lastname: Srujana
authors.affiliation: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Balanagar, Hyderabad 500037, India.
authors.forename: Libi Anandi
authors.initials: LA
authors.lastname: Vishwanathan
authors.affiliation: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Balanagar, Hyderabad 500037, India.
authors.forename: Santosh Kumar
authors.initials: SK
authors.lastname: Prajapti
authors.affiliation: Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Karisetty Bhanu
authors.initials: KB
authors.lastname: Chandra
authors.affiliation: Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
authors.forename: Lenin
authors.initials: L
authors.lastname: Veeraval
authors.affiliation: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Balanagar, Hyderabad 500037, India. Electronic address: bathini@niperhyd.ac.in.
authors.forename: Bathini Nagendra
authors.initials: BN
authors.lastname: Babu
mesh_terms: D000596:Amino Acids / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D051379:Mice; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D000928:Antidepressive Agents; D018696:Neuroprotective Agents; D009842:Oligopeptides; C507283:GLYX-13 peptide
keywords: GRIN2B; NMDA receptor; Neurotrophic; Norbornane amino acid