title: Peptidomimetics as potent and selective PTP1B inhibitors.
abstract: A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms discovery of highly potent and selective PTP1B inhibitors.
authors.affiliation: Zydus Research Centre, Sarkhej-Bavla, N.H. 8A Moraiya, Ahmedabad-382210, India.
authors.forename: Dipam
authors.initials: D
authors.lastname: Patel
authors.forename: Mukul
authors.initials: M
authors.lastname: Jain
authors.forename: Shailesh R
authors.initials: SR
authors.lastname: Shah
authors.forename: Rajesh
authors.initials: R
authors.lastname: Bahekar
authors.forename: Pradip
authors.initials: P
authors.lastname: Jadav
authors.forename: Kiran
authors.initials: K
authors.lastname: Shah
authors.forename: Amit
authors.initials: A
authors.lastname: Joharapurkar
authors.forename: Mubeen
authors.initials: M
authors.lastname: Shaikh
authors.forename: Kalapatapu V V M
authors.initials: KV
authors.lastname: Sairam
mesh_terms: D000085:Acetates / Q000737:chemistry; D000577:Amides / Q000737:chemistry; D004151:Dipeptides / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D057786:Peptidomimetics; D010880:Piperidines / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000085:Acetates; D000577:Amides; D004151:Dipeptides; D004791:Enzyme Inhibitors; D057786:Peptidomimetics; D010880:Piperidines; C032727:piperidine; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1