title: A novel approach to cyclin-dependent kinase 5/p25 inhibitors: A potential treatment for Alzheimer's disease.
abstract: Based on the earlier results of our in-house database and compound library, a series of novel clubbed thienyl triazoles was designed which may emerge as potential cdk5/p25 inhibitors, for the treatment of Alzheimer's disease. A benign synthesis was planned so as to take an advantage of MAOS (Microwave Assisted Organic Synthesis) method. Evaluation of the SAR of this series has allowed the identification of compounds 4, 5, 7 and 8 from series I while 13, 14, 16 and 17 from series II as significant cdk5/p25 inhibitors and thus have potential as possible treatments for Alzheimer's disease.
authors.affiliation: Dr. Reddy's Laboratories, 7-1-27, Ameerpet, Hyderabad 500016, Andhra Pradesh, India. rrshiradkar@rediffmail.com
authors.forename: Mahendra Ramesh
authors.initials: MR
authors.lastname: Shiradkar
authors.forename: Mallikarjuna Bandrehally
authors.initials: MB
authors.lastname: Padhalingappa
authors.forename: Sastry
authors.initials: S
authors.lastname: Bhetalabhotala
authors.forename: Kalyan Chakravarthy
authors.initials: KC
authors.lastname: Akula
authors.forename: Dattu Anna
authors.initials: DA
authors.lastname: Tupe
authors.forename: Raghotham Reddy
authors.initials: RR
authors.lastname: Pinninti
authors.forename: Suman
authors.initials: S
authors.lastname: Thummanagoti
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy / Q000473:pathology; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D051360:Cyclin-Dependent Kinase 5 / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D008872:Microwaves; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D013989:Ticrynafen / Q000737:chemistry*
chemical_list: D004791:Enzyme Inhibitors; D009419:Nerve Tissue Proteins; C118136:TPPP protein, human; D013844:Thiazoles; D051360:Cyclin-Dependent Kinase 5; D013989:Ticrynafen