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All total 26 Articles be found
All total 26 Articles be foundReagent-installed capsule network: Selective thiocarbamoylation of aromatic amines in crystals with preinstalled CH3NCS
Inokuma, Yasuhide,Ning, Guo-Hong,Fujita, Makoto
, p. 2379 - 2381 (2012)
Crystalline reagent capsules were prepared by installing CH3NCS into networked molecular capsules. While the tight encapsulation completely prevented leaching of reagent molecules into the supernatant, introduction of amines into the interstitial pores triggered reagent delivery. As a result, enhanced substrate selectivity was observed in crystalline-state thiocarbamoylation (see picture; 86:14 in favor of 2- vs. 1-naphthylamine). Copyright
Conformation of some N,N'-arylalkyl thioureas by 1H-NMR and infrared spectral analysis
Sudha, L. V.,Sathyanarayana, D. N.
, p. 751 - 756 (1984)
Several N,N'-arylalkyl thioureas were examined with 1H-NMR and i.r. spectra in order to study the conformation of the -NHCSNH- group.The influence of temperature and substituents on the chemical shift of the N-H protons has been investigated.Formation of a strong intramolecular hydrogen bond stabilizes the trans-cis conformation for most systems, while for the others the prevalence of different rotational isomers can be postulated.The influence of the steric effect on hydrogen bonding and molecular conformation is discussed.
CHEMICAL MODULATORS OF STORE-OPERATED CALCIUM CHANNELS AND THEIR THERAPEUTIC APPLICATIONS
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Paragraph 0130, (2019/04/14)
Methods of identification of inhibitors of calcium release-activated calcium (CRAC) channel and small molecule inhibitors of CRAC channel, including methods of their synthesis and pharmaceutical use, are disclosed.
Antileishmanial thioureas: Synthesis, biological activity and in Silico evaluations of new promising derivatives
Viana, Gil Mendes,Do Amaral, Lilian Henriques,Meireles, Paloma Wetler,Nunes, Raquel Pinto,Da Silva, Luiz Cláudio Rodrigues Pereira,De Sousa, Valeria Pereira,Sathler, Plínio Cunha,Cabral, Lucio Mendes,Soares, Deivid Costa,Saraiva, Elvira Maria,Santana, Marcos Vinicius,Castro, Helena Carla,De Sequeira Aguiar, Lúcia Cruz,Rodrigues, Carlos Rangel,Abreu, Paula Alvarez
, p. 911 - 919 (2018/10/31)
Leishmaniasis is a neglected tropical disease caused by protozoan parasites belonging to the genus Leishmania. Currently, the drugs available for treatment of this disease present high toxicity, along with development of parasite resistance. In order to overcome these problems, efforts have been made to search for new and more effective leishmanicidal drugs. The aim of this study was to synthesize and investigate the leishmanicidal effect of N,N′-disubstituted thioureas against Leishmania amazonensis, with evaluation of their in silico pharmacokinetics and toxicity profiles. Our results showed that different thioureas could be obtained in high to moderate yields using simple reaction conditions. Nine thiourea derivatives (3e, 3i, 3k, 3l, 3p, 3q, 3v, 3x and 3z) were active against parasite promastigotes (IC50 21.48–189.10μM), with low cytotoxicity on mice peritoneal macrophages (CC50>200μM), except for thiourea 3e (CC50=49.22μM). After that, the most promising thioureas (3k, 3l, 3p, 3q and 3v) showed IC50 ranging from 70 to 150μM against L. amazonensis amastigotes in infected macrophages. Except for thiourea 3p, the leishmanicidal activity of the derivatives were independent of nitric oxide (NO) production. Thioureas 3q and 3v affected promastigotes cell cycle without disturbing the mitochondrial membrane potential. Furthermore, our derivatives showed satisfactory theoretical absorption, distribution, metabolism, excretion, toxicity (ADMET) properties. These data indicate that thiourea derivatives are good candidates as leading compounds for the development of new leishmanicidal drugs.
