doi: 10.1016/j.bmcl.2006.12.066.
Epub 2006 Dec 22.
New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents
Affiliations
- PMID: 17239593
- DOI: 10.1016/j.bmcl.2006.12.066
Item in Clipboard
New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents
Bioorg Med Chem Lett.
.
Abstract
The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to 2mug/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.
Similar articles
-
Synthesis and biological evaluation of substituted 4,6-diarylpyrimidines and 3,5-diphenyl-4,5-dihydro-1H-pyrazoles as anti-tubercular agents.Bioorg Med Chem Lett. 2014 Jul 1;24(13):2892-6. doi: 10.1016/j.bmcl.2014.04.094. Epub 2014 May 4. Bioorg Med Chem Lett. 2014. PMID: 24835631
-
Structure-based design, synthesis and biological evaluation of a newer series of pyrazolo[1,5-a]pyrimidine analogues as potential anti-tubercular agents.Bioorg Chem. 2019 Jun;87:240-251. doi: 10.1016/j.bioorg.2019.02.044. Epub 2019 Mar 16. Bioorg Chem. 2019. PMID: 30908967
-
Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.Eur J Med Chem. 2011 Jun;46(6):2290-4. doi: 10.1016/j.ejmech.2011.03.010. Epub 2011 Mar 15. Eur J Med Chem. 2011. PMID: 21450375
-
5-tert-butyl-N-pyrazol-4-yl-4,5,6,7-tetrahydrobenzo[d]isoxazole-3-carboxamide derivatives as novel potent inhibitors of Mycobacterium tuberculosis pantothenate synthetase: initiating a quest for new antitubercular drugs.J Med Chem. 2008 Apr 10;51(7):1999-2002. doi: 10.1021/jm701372r. Epub 2008 Mar 13. J Med Chem. 2008. PMID: 18335974 Review.
-
Recent advances of pyrazole-containing derivatives as anti-tubercular agents.Eur J Med Chem. 2017 Oct 20;139:429-440. doi: 10.1016/j.ejmech.2017.07.059. Epub 2017 Aug 3. Eur J Med Chem. 2017. PMID: 28818767 Review.
Cited by
-
4-Benzyl-sulfanyl-1H-pyrazolo-[3,4-d]pyrimidine.Acta Crystallogr Sect E Struct Rep Online. 2013 Oct 16;69(Pt 11):o1650. doi: 10.1107/S160053681302789X. eCollection 2013 Oct 16. Acta Crystallogr Sect E Struct Rep Online. 2013. PMID: 24454091 Free PMC article.
-
Novel coumarin derivatives containing 1,2,4-triazole, 4,5-dicyanoimidazole and purine moieties: synthesis and evaluation of their cytostatic activity.Molecules. 2012 Sep 12;17(9):11010-25. doi: 10.3390/molecules170911010. Molecules. 2012. PMID: 22971585 Free PMC article.
-
Efficient Synthesis, SC-XRD, and Theoretical Studies of O-Benzenesulfonylated Pyrimidines: Role of Noncovalent Interaction Influence in Their Supramolecular Network.ACS Omega. 2020 Jun 18;5(25):15115-15128. doi: 10.1021/acsomega.0c00975. eCollection 2020 Jun 30. ACS Omega. 2020. PMID: 32637784 Free PMC article.
-
Synthesis and antimicrobial activity of some new pyrazoles, fused pyrazolo[3,4-d]-pyrimidine and 1,2-dihydroimidazo-[2,1-c][1,2,4]triazin-6-one derivatives.Molecules. 2011 Aug 4;16(8):6549-60. doi: 10.3390/molecules16086549. Molecules. 2011. PMID: 21818058 Free PMC article.
-
Crystal structure of 1-ethyl-pyrazolo[3,4-d]pyrimidine-4(5H)-thione.Acta Crystallogr Sect E Struct Rep Online. 2014 Aug 16;70(Pt 9):o1005-6. doi: 10.1107/S160053681401825X. eCollection 2014 Sep 1. Acta Crystallogr Sect E Struct Rep Online. 2014. PMID: 25309193 Free PMC article.
Publication types
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources
Other Literature Sources
Miscellaneous
