- Nickel complexes with phosphines and N-R-sulfonyldithiocarbimates ligands: New antifungals for the control of Hemileia vastatrix and Phakopsora pachyrhizi
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Nickel(II) complexes of general formula [Ni(RSO2N = CS2)(PPh3)2] (2a–h) or [Ni(RSO2N = CS2)dppe] (3a–h), where R = methyl (a), ethyl (b), butyl (c), octyl (d), phenyl (e), 4-isopropylphenyl (f), 4-tert-butylphenyl (g), 2-naphthyl (h), PPh3 = triphenylphosphine and dppe = 1,2-bis(diphenylphosphine)ethane were prepared, from which six are new substances (2f–h and 3f–h). The new compounds were characterized by elemental analysis of C, H, N and Ni, and by IR, UV–Vis and 1H, 13C and 31P NMR spectroscopies. The data were consistent with the formation of square planar nickel(II) complexes with mixed ligands, what was confirmed by single crystal X-ray diffraction studies on compounds 2f and 2h. These complexes present intramolecular Ni–H–C anagostic interactions. All complexes inhibited the germination of Hemileia vastatrix and Phakopsora pachyrhizi, the causal agents of devastating diseases on soybean and coffee cultures. The most active compounds presented IC90 values as low as 405 μM against H. vastatrix, and 280 μM against P. pachyrhizi. Thus, the title compounds are target molecules for the development of new agrochemicals against the Asian soybean rust and Coffee leaf-rust diseases.
- Vidigal, Antonio E.C.,Rubinger, Mayura M.M.,de Queiroz, Luan F.,da Silva, Lucas F.,Zambolim, Laércio,Guilardi, Silvana,Souza, Rafael A.C.,Ellena, Javier,Wetler, Emiliana B.,Oliveira, Marcelo R.L.
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p. 724 - 732
(2018/12/11)
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- Implication of sulfonylurea derivatives as prospective inhibitors of human carbonic anhydrase II
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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.
- Idrees, Danish,Hadianawala, Murtuza,Mahapatra, Amarjyoti Das,Datta, Bhaskar,Roy, Sonam,Ahamad, Shahzaib,Khan, Parvez,Imtaiyaz Hassan, Md.
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p. 961 - 969
(2018/05/23)
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- Identification of the first potent, selective and bioavailable PPARα antagonist
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The discovery and SAR of a novel series of potent and selective PPARα antagonists are herein described. Exploration of replacements for the labile acyl sulfonamide linker led to a biaryl sulfonamide series of which compound 33 proved to be suitable for further profiling in vivo. Compound 33 demonstrated excellent potency, selectivity against other nuclear hormone receptors, and good pharmacokinetics in mouse.
- Bravo, Yalda,Baccei, Christopher S.,Broadhead, Alex,Bundey, Richard,Chen, Austin,Clark, Ryan,Correa, Lucia,Jacintho, Jason D.,Lorrain, Daniel S.,Messmer, Davorka,Stebbins, Karin,Prasit, Peppi,Stock, Nicholas
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p. 2267 - 2272
(2014/05/20)
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- AZABICYCLO[3.1.0] HEXYLPHENYL DERIVATIVE AS MODULATORS OF DOPAMINE D3 RECEPTORS
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The present invention relates to novel compounds of formula (IA) or a salt thereof: Formula (IA), wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consis
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Page/Page column 38
(2008/06/13)
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- Sulfonamides and uses
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Sulfonamides of formula I, in which the symbols R1 -R6, X, Y and n have the significance given in the description and which are in part novel compounds, and salts thereof, which can be used as active ingredients for the manufacture of medicaments for the treatment of circulatory disorders, especially hypertension, ischemia, vasospasms and angina pectoris, are described.
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