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Literature DB >> 16806925

Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase.

Martha De La Rosa¹, Hong Woo Kim, Esmir Gunic, Cheryl Jenket, Uyen Boyle, Yung-Hyo Koh, Ilia Korboukh, Matthew Allan, Weijian Zhang, Huanming Chen, Wen Xu, Shahul Nilar, Nanhua Yao, Robert Hamatake, Stanley A Lang, Zhi Hong, Zhijun Zhang, Jean-Luc Girardet.

Abstract

A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones.

Entities: Chemical Mutation Species

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Year: 2006 PMID： 16806925 DOI： 10.1016/j.bmcl.2006.06.048

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

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Cited

13 in total

1. The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.

Authors: Vigneshwaran Namasivayam; Murugesan Vanangamudi; Victor G Kramer; Sonali Kurup; Peng Zhan; Xinyong Liu; Jacob Kongsted; Siddappa N Byrareddy
Journal: J Med Chem Date: 2018-12-27 Impact factor: 7.446

2. 3,4,5-Trisubstituted-1,2,4-4H-triazoles as WT and Y188L mutant HIV-1 non-nucleoside reverse transcriptase inhibitors: docking-based CoMFA and CoMSIA analyses.

Authors: Elena Cichero; Laura Buffa; Paola Fossa
Journal: J Mol Model Date: 2010-10-05 Impact factor: 1.810

3. A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.

Authors: Zhijun Zhang; Wen Xu; Yung-Hyo Koh; Jae Hoon Shim; Jean-Luc Girardet; Li-Tain Yeh; Robert K Hamatake; Zhi Hong
Journal: Antimicrob Agents Chemother Date: 2006-11-20 Impact factor: 5.191

9. Three-dimensional pharmacophore design and biochemical screening identifies substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.

Authors: Tummala R K Reddy; Chan Li; Peter M Fischer; Lodewijk V Dekker
Journal: ChemMedChem Date: 2012-05-29 Impact factor: 3.466

Review 10. Triazole analogues as potential pharmacological agents: a brief review.

Authors: Sachin Kumar; Sukhbir Lal Khokra; Akash Yadav
Journal: Futur J Pharm Sci Date: 2021-05-25

Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase.

1. The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.

2. 3,4,5-Trisubstituted-1,2,4-4H-triazoles as WT and Y188L mutant HIV-1 non-nucleoside reverse transcriptase inhibitors: docking-based CoMFA and CoMSIA analyses.

3. A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.

4. From docking false-positive to active anti-HIV agent.

5. Synthesis and antiviral activities of new acyclic and "double-headed" nucleoside analogues.

6. Docking-based 3D-QSAR analyses of pyrazole derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.

7. Host-directed Inhibitors of Myxoviruses: Synthesis and in vitro Biochemical Evaluation.

8. Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1 NNRTIs.

9. Three-dimensional pharmacophore design and biochemical screening identifies substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.

Review 10. Triazole analogues as potential pharmacological agents: a brief review.