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Discovery of novel and potent heterocyclic carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors.
Basu, Sujay; Prasad, Uppuleti Viplava; Barawkar, Dinesh A; De, Siddhartha; Palle, Venkata P; Menon, Suraj; Patel, Meena; Thorat, Sachin; Singh, Umesh P; Das Sarma, Koushik; Waman, Yogesh; Niranjan, Sanjay; Pathade, Vishal; Gaur, Ashwani; Reddy, Satyanarayana; Ansari, Shariq.
Bioorg Med Chem Lett ; 22(8): 2843-9, 2012 Apr 15.
Article in English | MEDLINE | ID: mdl-22424978

ABSTRACT

A series of novel heterocyclic carboxylic acid based protein tyrosine phosphatase 1B (PTP1B) inhibitors with hydrophobic tail have been synthesized and characterized. Structure-activity relationship (SAR) optimization resulted in identification of several potent, selective (over the highly homologous T-cell protein tyrosine phosphatase, TCPTP) and metabolically stable PTP1B inhibitors. Compounds 7a, 19a and 19c showed favorable cell permeability and pharmacokinetic properties in mouse with moderate to very good oral (% F=13-70) bio-availability.


Subject(s)
Carboxylic Acids/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Heterocyclic Compounds/chemical synthesis , Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors , Administration, Oral , Animals , Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , Enzyme Activation/drug effects , Heterocyclic Compounds/chemistry , Heterocyclic Compounds/pharmacology , Hydrophobic and Hydrophilic Interactions , Male , Mice , Mice, Inbred C57BL , Structure-Activity Relationship
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