72857-85-3Relevant articles and documents
N-substituted 5-chloro-6-phenylpyridazin-3(2H)-ones: Synthesis, insecticidal activity against Plutella xylostella (L.) and SAR study
Wu, Jian,Kang, Shenghong,Yuan, Qinkun,Luo, Lijun,Ma, Juan,Shi, Qingcai,Yang, Song
, p. 9413 - 9420 (2012)
A series of N-substituted 5-chloro-6-phenylpyridazin-3(2H)-one derivatives were synthesized based on our previous work; all compounds were characterized by spectral data and tested for in vitro insecticidal activity against Plutella xylostella. The result
Design, synthesis, and In vitro antituberculosis activity of 2(5H)-Furanone derivatives
Ngwane, Andile H.,Panayides, Jenny-Lee,Chouteau, Franck,Macingwana, Lubabalo,Viljoen, Albertus,Baker, Bienyameen,Madikane, Eliya,de Kock, Carmen,Wiesner, Lubbe,Chibale, Kelly,Parkinson, Christopher J.,Mmutlane, Edwin M.,van Helden, Paul,Wiid, Ian
, p. 612 - 620 (2016)
A series of 2(5H)-furanone-based compounds were synthesized from commercially available mucohalic acids. From the first-generation compounds, three showed inhibitory activity (10 μg/mL) of at least 35% against Mycobacterium smegmatis mc2 155 growth (Bioscreen C system). In screening the active first-generation compounds for growth inhibition against Mycobacterium tuberculosis H37Rv, the most active compound was identified with a minimum inhibitory concentration (MIC99) of 8.07 μg/mL (15.8 μM) using BACTEC 460 system. No cross-resistance was observed with some current first-line anti-TB drugs, since it similarly inhibited the growth of multidrug resistant (MDR) clinical isolates. The compound showed a good selectivity for mycobacteria since it did not inhibit the growth of selected Gram-positive and Gram-negative bacteria. It also showed synergistic activity with rifampicin (RIF) and additive activity with isoniazid (INH) and ethambutol (EMB). Additional time-kill studies showed that the compound is bacteriostatic to mycobacteria, but cytotoxic to the Chinese Hamster Ovarian (CHO) cell line. From a second generation library, two compounds showed improved anti-TB activity against M. tuberculosis H37Rv and decreased CHO cell cytotoxicity. The compounds exhibited MIC values of 2.62 μg/mL (5.6 μM) and 3.07 μg/mL (5.6 μM) respectively. The improved cytotoxicity against CHO cell line of the two compounds ranged from IC50 = 38.24 μg/mL to IC50 = 45.58 μg/mL when compared to the most active first-generation compound (IC50 = 1.82 μg/mL). The two second generation leads with selectivity indices (SI) of 14.64 and 14.85 respectively, warrant further development as anti-TB drug candidates.
COMPOSITIONS AND METHODS FOR VIRAL SENSITIZATION
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Paragraph 0048; sheet 3, (2016/08/23)
Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.