Cheng, Hua; Shen, Yan-Qing; Pan, Xia-Yan; Hou, Yi-Ping; Wu, Qiong-You; Yang, Guang-Fu published the artcile< Discovery of 1,2,4-triazole-1,3-disulfonamides as dual inhibitors of mitochondrial complex II and complex III>, Reference of 35852-58-5, the main research area is triazoledisulfonamide preparation inhibitor mitochondria complex II III; antibacterial activity Xanthomonas.
Respiratory chain succinate-ubiquinone oxidoreductase (SQR or complex II) and ubihydroquinone-cytochrome (cyt) c oxidoreductase (cyt bc1 or complex III) have been demonstrated as the promising targets of numerous antibiotics and fungicides. As a continuation of our research work on the development of new fungicides, a series of 1,2,4-triazole-1,3-disulfonamide derivatives with dual functions targeting both SQR and cyt bc1 were designed and synthesized by coupling diverse di-Ph ether moieties with triazolesulfonamide units. These newly synthesized compounds were characterized by elemental analyses, 1H NMR and ESI-MS spectrometry. The in vitro assay indicated that most of the synthesized compounds displayed good inhibition against porcine succinate-cytochrome reductase (SCR) with IC50 values ranging from 3.2 to 81.8 μM, revealing much higher activity than that of the com. control amisulbrom whose IC50 value is 93.0 μM. Further evaluation against the resp. SQR and cyt bc1 indicated that most compounds exhibited SQR-inhibiting activity as well as cyt bc1-inhibiting activity, but the inhibition potency against SQR is much higher than that against cyt bc1, showing that the SCR inhibition might be contributed greatly by the SQR inhibition. The further antibacterial evaluation against Xanthomonas oryzae pv. oryzae revealed that four compounds showed excellent potency at the concentration of 20 μg mL-1. In particular, compounds (I) and (II) exhibited much better antibacterial activity than the com. control bismerthiazol in terms of their EC50. Impressively, II has an EC90 of 33.62 μg mL-1, more than 10-fold higher than that of bismerthiazol.
New Journal of Chemistry published new progress about Antibacterial agents. 35852-58-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3O, Reference of 35852-58-5.
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