30746-54-4Relevant articles and documents
Design, synthesis, in vitro inhibition and toxicological evaluation of human carbonic anhydrases I, II and IX inhibitors in 5-nitroimidazole series
Aspatwar, Ashok,Parvathaneni, Nanda Kumar,Barker, Harlan,Anduran, Emilie,Supuran, Claudiu T.,Dubois, Ludwig,Lambin, Philippe,Parkkila, Seppo,Winum, Jean-Yves
, p. 109 - 117 (2020)
With the aim to obtain novel compounds possessing both strong affinity against human carbonic anhydrases and low toxicity, we synthesised novel thiourea and sulphonamide derivatives 3, 4 and 10, and studied their in vitro inhibitory properties against human CA I, CA II and CA IX. We also evaluated the toxicity of these compounds using zebrafish larvae. Among the three compounds, derivative 4 showed efficient inhibition against hCA II (KI = 58.6 nM). Compound 10 showed moderate inhibition against hCA II (KI = 199.2 nM) and hCA IX (KI = 147.3 nM), whereas it inhibited hCA I less weakly at micromolar concentrations (KI = 6428.4 nM). All other inhibition constants for these compounds were in the submicromolar range. The toxicity evaluation studies showed no adverse effects on the zebrafish larvae. Our study suggests that these compounds are suitable for further preclinical characterisation as potential inhibitors of hCA I, II and IX.
A rifamycin - nitro imidazole coupled molecular preparation method of (by machine translation)
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Paragraph 0027-0029, (2017/09/12)
The invention discloses a rifamycin - nitro imidazole coupling molecule of the preparation method. Preparation method of this invention to MTZ as raw materials, by changing the synthetic route, overcomes the reaction conditions must be controlled to the defect under the low temperature condition, and has improved the yield of target product. (by machine translation)
EXPANDED THERAPEUTIC POTENTIAL IN NITROHETEROARYL ANTIMICROBIALS
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Paragraph 0296, (2015/01/07)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to imidazole, thiazole, and furan derivatives and their use as therapeutic agents.
