Literature DB >> 12217356

Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.

Veerle Vanheusden1, Hélène Munier-Lehmann, Sylvie Pochet, Piet Herdewijn, Serge Van Calenbergh.   

Abstract

A number of 2'- and 3'-modified thymidine 5'-O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate kinase showed that a 2'-halogeno substituent and a 3'-azido function are the most favorable leads for further development of potent inhibitors of this enzyme.

Entities:  

Mesh：

Substances：

Year:  2002        PMID： 12217356     DOI： 10.1016/s0960-894x(02)00551-6

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  10 in total

1.  Mechanisms of substrate selectivity for Bacillus anthracis thymidylate kinase.

Authors:  Cecilia Carnrot; Liya Wang; Dimitri Topalis; Staffan Eriksson
Journal:  Protein Sci       Date:  2008-06-03       Impact factor: 6.725

2.  3D-Pharmacophore mapping of thymidine-based inhibitors of TMPK as potential antituberculosis agents.

Authors:  Carolina Horta Andrade; Kerly F M Pasqualoto; Elizabeth I Ferreira; Anton J Hopfinger
Journal:  J Comput Aided Mol Des       Date:  2010-03-10       Impact factor: 3.686

3.  Structural and chemical basis for enhanced affinity to a series of mycobacterial thymidine monophosphate kinase inhibitors: fragment-based QSAR and QM/MM docking studies.

Authors:  Renata V Bueno; Ney R Toledo; Bruno J Neves; Rodolpho C Braga; Carolina H Andrade
Journal:  J Mol Model       Date:  2012-07-31       Impact factor: 1.810

4.  Computer-assisted combinatorial design of bicyclic thymidine analogs as inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.

Authors:  Vladimir Frecer; Pierfausto Seneci; Stanislav Miertus
Journal:  J Comput Aided Mol Des       Date:  2010-11-17       Impact factor: 3.686

5.  Structure-based in-silico rational design of a selective peptide inhibitor for thymidine monophosphate kinase of mycobacterium tuberculosis.

Authors:  Manoj Kumar; Sujata Sharma; Alagiri Srinivasan; Tej P Singh; Punit Kaur
Journal:  J Mol Model       Date:  2010-08-11       Impact factor: 1.810

6.  Phosphorus Pentachloride Promoted gem-Dichlorination of 2'- and 3'-Deoxynucleosides.

Authors:  Fabio da Paixao Soares; Elisabetta Groaz; Piet Herdewijn
Journal:  Molecules       Date:  2018-06-15       Impact factor: 4.411

7.  Synthesis and evaluation of 3'-[18F]fluorothymidine-5'-squaryl as a bioisostere of 3'-[18F]fluorothymidine-5'-monophosphate.

Authors:  D Brickute; A Beckley; L Allott; M Braga; C Barnes; K J Thorley; E O Aboagye
Journal:  RSC Adv       Date:  2021-03-29       Impact factor: 4.036

Review 8.  Analogues of Pyrimidine Nucleosides as Mycobacteria Growth Inhibitors.

Authors:  Liudmila A Alexandrova; Anastasia L Khandazhinskaya; Elena S Matyugina; Dmitriy A Makarov; Sergey N Kochetkov
Journal:  Microorganisms       Date:  2022-06-27

9.  Chemotherapeutic interventions against tuberculosis.

Authors:  Neeraj Shakya; Gaurav Garg; Babita Agrawal; Rakesh Kumar
Journal:  Pharmaceuticals (Basel)       Date:  2012-06-28

10.  In silico Design and Synthesis of Tetrahydropyrimidinones and Tetrahydropyrimidinethiones as Potential Thymidylate Kinase Inhibitors Exerting Anti-TB Activity Against Mycobacterium tuberculosis.

Authors:  Katharigatta N Venugopala; Christophe Tratrat; Melendhran Pillay; Sandeep Chandrashekharappa; Omar Husham Ahmed Al-Attraqchi; Bandar E Aldhubiab; Mahesh Attimarad; Osama I Alwassil; Anroop B Nair; Nagaraja Sreeharsha; Rashmi Venugopala; Mohamed A Morsy; Michelyne Haroun; Hezekiel M Kumalo; Bharti Odhav; Koleka Mlisana
Journal:  Drug Des Devel Ther       Date:  2020-03-09       Impact factor: 4.162
  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.