24539-87-5Relevant academic research and scientific papers
Implication of sulfonylurea derivatives as prospective inhibitors of human carbonic anhydrase II
Idrees, Danish,Hadianawala, Murtuza,Mahapatra, Amarjyoti Das,Datta, Bhaskar,Roy, Sonam,Ahamad, Shahzaib,Khan, Parvez,Imtaiyaz Hassan, Md.
, p. 961 - 969 (2018/05/23)
Selective carbonic anhydrase (CA) inhibitors have gained a lot of importance owing to the implication of specific isoforms of CA in certain diseases like glaucoma, leukemia, cystic fibrosis, and epilepsy. A novel class of sulfonylurea derivatives was synthesized from corresponding sulfonyl chlorides and amines. Compounds with different pendant moieties in the sulfonylurea derivatives show significant interactions with human carbonic anhydrase II (CAII). In vitro evaluation of the sulfonylurea derivatives revealed that three compounds possess admirable inhibitory activity against CAII. Compounds containing methyl (G2), isopropyl (G4) and o-tosyl (G5) groups displayed IC50 (109-137 μm) for CAII. Fluorescence binding and cytotoxicity studies revealed that these compounds are showing good binding affinity (18-34 μM) to CAII and non- toxic to human cells. Further, molecular docking studies of G2, G4 and G5 with CAII showed that these compounds fit nicely in the active site of CAII. Molecular dynamics simulation studies of these compounds complexed with CAII showed that essential interactions were maintained up to 50 ns of simulation. These results indicate the promising nature of the sulfonylurea scaffold towards CAII inhibition and opens scope of hit to-lead optimization for discovery of effective drugs against CAII-associated disorders.
The aqueous-phase synthesis of sulfonylthioureas and a study of their properties as anion receptors
Ding, Cong-Wen,Yu, Hai-Feng,Li, Rui-Min,Jiang, Xiang-Fu,Luo, Bin
, p. 254 - 261 (2013/02/25)
A series of mono- or bis-sulfonylthioureas has been synthesized via nucleophilic substitution of potassium sulfonamides and sodium dithiocarbamate in water under mild conditions, and their properties as anion receptors in the absence and presence of K+ have been investigated by 1H NMR spectroscopy. It was found that calix[4]crown-5 derivative 10 shows much higher selective complexation capability with H2PO4 - in the presence of K+ than in the absence of K +, which indicates the physical dimension of K+ and H 2PO4-, respectively, matched the corresponding cavity of the host compound. ARKAT-USA, Inc.
Substituted Sulfonylthioureas as Broad-Band Complexing Agents
Koenig, Karl-Heinz,Holzner, Christoph,Bosslet, Joachim
, p. 1771 - 1772 (2007/10/02)
Compounds 1 form neutral metal complexes, which are insoluble in water and extractable with CHCl3.Due to the high N-H acidity of 1, complexation occurs with more than 20 metals even in strongly acidic solution.
