20201-05-2Relevant academic research and scientific papers
Synthesis and evaluation of N-(methylthiophenyl)picolinamide derivatives as PET radioligands for metabotropic glutamate receptor subtype 4
Kil, Kun-Eek,Poutiainen, Pekka,Zhang, Zhaoda,Zhu, Aijun,Kuruppu, Darshini,Prabhakar, Shilpa,Choi, Ji-Kyung,Tannous, Bakhos A.,Brownell, Anna-Liisa
, p. 133 - 139 (2016)
In recent years, mGlu4 has received great research attention because of the potential benefits of mGlu4 activation in treating numerous brain disorders, such as Parkinson's disease (PD). A specific mGlu4 PET radioligand could be an important tool in understanding the role of mGlu4 in both healthy and disease conditions, and also for the development of new drugs. In this study, we synthesized four new N-(methylthiophenyl)picolinamide derivatives 11-14. Of these ligands, 11 and 14 showed high in vitro binding affinity for mGlu4 with IC50 values of 3.4 nM and 3.1 nM, respectively, and suitable physicochemical parameters. Compound 11 also showed enhanced metabolic stability and good selectivity to other mGluRs. [11C]11 and [11C]14 were radiolabeled using the [11C]methylation of the thiophenol precursors 20a and 20c with [11C]CH3I in 19.0% and 34.8% radiochemical yields (RCY), and their specific activities at the end of synthesis (EOS) were 496 ± 138 GBq/μmol (n = 6) and 463 ± 263 GBq/μmol (n = 4), respectively. The PET studies showed that [11C]11 accumulated fast into the brain and had higher uptake, slower washout and 25% better contrast than [11C]2, indicating improved imaging characteristics as PET radiotracer for mGlu4 compared to [11C]2. Therefore, [11C]11 will be a useful radioligand to investigate mGlu4 in different biological applications.
ARYL SULFIDE DERIVATIVES AND ARYL SULFOXIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES
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Paragraph 1009; 1010; 1011, (2015/12/23)
The present invention relates to aryl sulphide and aryl sulphoxide derivatives, to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation. The aryl sulphide and aryl sulphoxide derivatives have the general structure (I) in which the respective radicals have the meanings given in the description.
N-ARYLAMIDINE-SUBSTITUTED TRIFLUOROETHYL SULFIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES
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Paragraph 0445-0447, (2014/10/29)
The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
Synthesis of aryl perfluoroalkyl sulfides from aromatic disulfides
Sipyagin,Enshov,Kashtanov,Potemkin,Thrasher,Waterfeld
, p. 420 - 434 (2007/10/03)
Thermolysis of xenon(II) bis(perfluoroalkanecarboxylates) in the presence of diaryl disulfides occurs through the S-S bond cleavage to form dihalo-, halonitro-, and halodinitrophenyl perfluoroalkyl sulfides. The latter type of compounds was obtained for the first time. The main side process is the perfluoroalkylation of the aromatic ring.
Preparation of the first ortho-substituted pentafluorosulfanylbenzenes
Sipyagin, Alexey M.,Bateman, Colin P.,Tan, Ying-Teck,Thrasher, Joseph S.
, p. 287 - 295 (2007/10/03)
The preparation of the first ortho-substituted pentafluorosulfanylbenzenes was achieved. Oxidative fluorination (AgF2) of a series of aromatic disulfides containing different substituents ortho to the disulfide moiety gave only one ortho-substi
SYNTHESIS OF 2,7-DINITRO- AND 2,7-DIAMINOTHIANTHRENE
Lisitsyn, V. N.,Zaitsev, S. A.
, p. 181 - 182 (2007/10/02)
The previously undescribed 2,7-dinitrothioanthrene was obtained by the reduction of bis(5-nitro-2-chlorophenyl) disulfide.Its reduction to the corresponding diamine and its diacetyl derivative was investigated.
