4146-25-2Relevant academic research and scientific papers
The fight against the influenza A virus H1N1: Synthesis, molecular modeling, and biological evaluation of benzofurazan derivatives as viral RNA polymerase inhibitors
Pagano, Mafalda,Castagnolo, Daniele,Bernardini, Martina,Fallacara, Anna Lucia,Laurenzana, Ilaria,Deodato, Davide,Kessler, Ulrich,Pilger, Beatrice,Stergiou, Lilli,Strunze, Stephan,Tintori, Cristina,Botta, Maurizio
, p. 129 - 150 (2014/01/17)
The influenza RNA polymerase complex, which consists of the three subunits PA, PB1, and PB2, is a promising target for the development of new antiviral drugs. A large library of benzofurazan compounds was synthesized and assayed against influenza virus A/WSN/33 (H1N1). Most of the new derivatives were found to act by inhibiting the viral RNA polymerase complex through disruption of the complex formed between subunits PA and PB1. Docking studies were also performed to elucidate the binding mode of benzofurazans within the PB1 binding site in PA and to identify amino acids involved in their mechanism of action. The predicted binding pose is fully consistent with the biological data and lays the foundation for the rational development of more effective PA-PB1 inhibitors. In the fight against influenza virus A/WSN/33 (H1N1), the PA-PB1 protein-protein interaction is emerging as a new drug target. To identify small molecules able to inhibit the viral RNA polymerase complex, the benzofurazan scaffold was explored by synthesizing a large library of derivatives. Some compounds showed high anti-H1N1 activity and emerged as effective inhibitors of the PA-PB1 interaction, with IC50 values in the micromolar range. Copyright
Creating an antibacterial with in vivo efficacy: Synthesis and characterization of potent inhibitors of the bacterial cell division protein FTSZ with improved pharmaceutical properties
Haydon, David J.,Bennett, James M.,Brown, David,Collins, Ian,Galbraith, Greta,Lancett, Paul,MacDonald, Rebecca,Stokes, Neil R.,Chauhan, Pramod K.,Sutariya, Jignesh K.,Nayal, Narendra,Srivastava, Anil,Beanland, Joy,Hall, Robin,Henstock, Vincent,Noula, Caterina,Rockley, Chris,Czaplewski, Lloyd
supporting information; experimental part, p. 3927 - 3936 (2010/09/04)
3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.
HIV reverse transcriptase inhibitors
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Page/Page column 43, (2010/11/25)
Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
NOVEL HETEROCYCLIC COMPOUNDS AS HSP90-INHIBITORS
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Page/Page column 337, (2008/06/13)
Novel heterocyclic compounds are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agent. Method of synthesis and use of such compounds are also described.
Photochemical synthesis of s-triazolo[3,4-b]benzothiazole and mechanistic studies on benzothiazole formation
Jayanthi,Muthusamy,Paramasivam,Ramakrishnan,Ramasamy,Ramamurthy
, p. 5766 - 5770 (2007/10/03)
A general photochemical synthesis of s-triazolo[3,4-b]benzothizoles from 4,5-disubstituted 1,2,4-triazole-3-thione is described. Steady photolysis, quantum yield determination, and laser flash photolysis experiments have been carried out. An intermolecular electron transfer mechanism has been proposed.
Photochemical Synthesis of Benzothiazoles
Paramasivam, R.,Ramakrishnan, V. T.
, p. 930 - 934 (2007/10/02)
Irradiation of o-halothioacetanilides (1a-p) affords benzothiazoles (2a-p) in general.In methanol medium, polyhalogenated thioacetanilides yield benzothiazoles with the loss of bromine atom in the 4- or 6-position of the benzothiazole.Arylation of benzothiazoles occurs in benzene medium.
