Literature DB >> 17643991

A novel approach to cyclin-dependent kinase 5/p25 inhibitors: A potential treatment for Alzheimer's disease.

Mahendra Ramesh Shiradkar1, Mallikarjuna Bandrehally Padhalingappa, Sastry Bhetalabhotala, Kalyan Chakravarthy Akula, Dattu Anna Tupe, Raghotham Reddy Pinninti, Suman Thummanagoti.   

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.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 17643991     DOI: 10.1016/j.bmc.2007.06.053

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  6 in total

1.  A 24-residue peptide (p5), derived from p35, the Cdk5 neuronal activator, specifically inhibits Cdk5-p25 hyperactivity and tau hyperphosphorylation.

Authors:  Ya-Li Zheng; Niranjana D Amin; Ya-Fang Hu; Parvathi Rudrabhatla; Varsha Shukla; Jyotshnabala Kanungo; Sashi Kesavapany; Philip Grant; Wayne Albers; Harish C Pant
Journal:  J Biol Chem       Date:  2010-08-18       Impact factor: 5.157

2.  Discovery of thienoquinolone derivatives as selective and ATP non-competitive CDK5/p25 inhibitors by structure-based virtual screening.

Authors:  Arindam Chatterjee; Stephen J Cutler; Robert J Doerksen; Ikhlas A Khan; John S Williamson
Journal:  Bioorg Med Chem       Date:  2014-09-28       Impact factor: 3.641

3.  Docking and 3D-QSAR modeling of cyclin-dependent kinase 5/p25 inhibitors.

Authors:  Zaheer Ul Haq; Reaz Uddin; Lam Kok Wai; Abdul Wadood; Nordin Haji Lajis
Journal:  J Mol Model       Date:  2010-08-05       Impact factor: 1.810

4.  Silencing of CDK5 reduces neurofibrillary tangles in transgenic alzheimer's mice.

Authors:  Diego Piedrahita; Israel Hernández; Alejandro López-Tobón; Dmitry Fedorov; Boguslaw Obara; B S Manjunath; Ryan L Boudreau; Beverly Davidson; Frank Laferla; Juan Carlos Gallego-Gómez; Kenneth S Kosik; Gloria Patricia Cardona-Gómez
Journal:  J Neurosci       Date:  2010-10-20       Impact factor: 6.167

5.  Synthesis of Oxadiazolyl, Pyrazolyl and Thiazolyl Derivatives of Thiophene-2-Carboxamide as Antimicrobial and Anti-HCV Agents.

Authors:  Ola H Rizk; Omaima G Shaaban; Abeer E Abdel Wahab
Journal:  Open Med Chem J       Date:  2017-04-28

6.  Synthesis and antimicrobial activity of new 5-(2-thienyl)-1,2,4-triazoles and 5-(2-thienyl)-1,3,4-oxadiazoles and related derivatives.

Authors:  Mohamed A Al-Omar
Journal:  Molecules       Date:  2010-01-22       Impact factor: 4.411

  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.