6314-40-5Relevant articles and documents
Discovery of Potent Inhibitors of Streptococcus mutans Biofilm with Antivirulence Activity
Nijampatnam, Bhavitavya,Ahirwar, Parmanand,Pukkanasut, Piyasuda,Womack, Holly,Casals, Luke,Zhang, Hua,Cai, Xia,Michalek, Suzanne M.,Wu, Hui,Velu, Sadanandan E.
supporting information, p. 48 - 55 (2020/12/21)
Dental caries is a bacterial infectious disease characterized by demineralization of the tooth enamel. Treatment of this disease with conventional antibiotics is largely ineffective as the cariogenic bacteria form tenacious biofilms that are resistant to such treatments. The main etiological agent for dental caries is the bacterium Streptococcus mutans. S. mutans readily forms biofilms on the tooth surface and rapidly produces lactic acid from dietary sucrose. Glucosyl transferases (Gtfs) secreted by S. mutans are mainly responsible for the production of exopolysaccharides that are crucial for the biofilm architecture. Thus, inhibiting S. mutans' Gtfs is an effective approach to develop selective biofilm inhibitors that do not affect the growth of oral commensals. Herein, we report a library of 90 analogs of the previously identified lead compound, G43, and exploration of its structure activity relationships (SAR). All compounds were evaluated for the inhibition of S. mutans biofilms and bacterial growth. Selected compounds from this library were further evaluated for enzyme inhibition against Gtfs using a zymogram assay and for growth inhibition against oral commensal bacterial species such as Streptococcus gordonii and Streptococcus sanguinis. This study has led to the discovery of several new biofilm inhibitors with enhanced potency and selectivity. One of the leads, IIIF1, showed marked reduction in buccal, sulcal, and proximal caries scores in a rat model of dental caries.
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes
Mahajan, Pravin S.,Nikam, Mukesh D.,Nawale, Laxman U.,Khedkar, Vijay M.,Sarkar, Dhiman,Gill, Charansingh H.
, p. 751 - 756 (2016/08/24)
In vitro and ex vivo efficacies of four series of benzo[b]thiophene-2-carboxylic acid derivatives were studied against Mycobacterium tuberculosis H37Ra (MTB). Benzo[b]thiophenes were also tested in vitro against multidrug resistant Mycobacterium tuberculosis H37Ra (MDR-MTB), and 7b was found to be highly active against A- and D-MDR-MTB/MTB (MIC ranges 2.73-22.86 μg/mL). The activity of all benzo[b]thiophenes against M. bovis BCG (BCG) was also assessed grown under aerobic and under conditions of oxygen depletion. Compounds 8c and 8g showed significant activity with MICs of 0.60 and 0.61 μg/mL against dormant BCG. The low cytotoxicity and high selectivity index data against human cancer cell lines, HeLa, Panc-1, and THP-1 indicate the potential importance of the development of benzo[b]thiophene-based 1,3-diketones and flavones as lead candidates to treat mycobacterial infections. Molecular docking studies into the active site of DprE1 (Decaprenylphosphoryl-β-d-ribose-2′-epimerase) enzyme revealed a similar binding mode to native ligand in the crystal structure thereby helping to understand the ligand-protein interactions and establish a structural basis for inhibition of MTB. In summary, its good activity in in vitro and ex vivo model, as well as its activity against multidrug-resistant M. tuberculosis H37Ra in a potentially latent state, makes 7b an attractive drug candidate for the therapy of tuberculosis.
Novel compound or pharmaceutically acceptable salt thereof and pharmaceutical composition for prevention or treatment of disease caused by influenza virus infection containing the same as an active ingredient
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Paragraph 0484; 0853-0856, (2016/10/07)
The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active component for preventing or treating diseases related with influenza virus infection. The novel compound represented by chemical formula 1 has remarkable antivirus activity against influenza virus without cytotoxicity to human cells and thus has little side effects to human bodies. Therefore, the pharmaceutical composition having the same as an active component can be usefully used for preventing or treating diseases which occur through influenza virus infection such as flu, cold, sore throat, bronchitis, pneumonia, avian influenza, swine flu, goat flu, etc.COPYRIGHT KIPO 2016
Novel compound or pharmaceutically acceptable salt thereof and pharmaceutical composition for prevention or treatment of disease caused by influenza virus infection containing the same as an active ingredient
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Paragraph 0484; 0853; 0854; 0855, (2016/10/07)
The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for preventing or treating diseases caused by influenza virus infection, comprising the same as an active ingredient. The nov
Novel compound or pharmaceutically acceptable salt thereof and pharmaceutical composition for prevention or treatment of disease caused by influenza virus infection containing the same as an active ingredient
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Paragraph 0484; 0853; 0854; 0855, (2016/10/08)
The present invention relates to a novel compound or pharmaceutically acceptable salt thereof, and to a pharmaceutical composition containing the same as an active ingredient for treating and preventing disease caused by influenza virus infection. The novel compound represented by chemical formula 1 according to the present invention not only has extremely excellent antivirus activity, but also has less side effects for a human body by not having cytotoxicity for a human cell. Therefore, a pharmaceutical composition containing the same as an active ingredient can be used in preventing or treating such as flu, colds, sore throats, bronchitis, pneumonia, bird flu, swine flu, and goat flu caused by influenza virus infection.COPYRIGHT KIPO 2015
Facile oxidation of electron-poor benzo[b]thiophenes to the corresponding sulfones with an aqueous solution of H2O2 and P 2O5
Antonow, Dyeison,Marrafa, Teresa,Dawood, Irfaan,Ahmed, Tauheed,Haque, Mohammad R.,Thurston, David E.,Zinzalla, Giovanna
supporting information; experimental part, p. 2289 - 2291 (2010/07/08)
A facile oxidation for the clean conversion of benzo[b]thiophenes to their corresponding sulfones is described employing an aqueous solution of H 2O2 and P2O5; the solution can be prepared and stored on a multi-
Carboxylic acid amide benzothiophenecarboxamide s-oxides
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, (2008/06/13)
New benzothiophenecarboxamide S-oxides of the formula (I) STR1 in which R1 represents optionally substituted alkyl, or represents alkenyl or alkinyl, or represents in each case optionally substituted cycloalkyl or cycloalkylalkyl, or represents
