50548-46-4Relevant articles and documents
2-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity
Cardoso, Marcos Veríssimo de Oliveira,de Oliveira Filho, Gevanio Bezerra,de Siqueira, Lucianna Rabelo Pessoa,Espíndola, José Wanderlan Pontes,Silva, Elany Barbosa da,Mendes, Andresa Pereira de Oliveira,Pereira, Valéria Rêgo Alves,de Castro, Maria Carolina Accioly Brelaz,Ferreira, Rafaela Salgado,Villela, Filipe Silva,Costa, Francielly Morais Rodrigues da,Meira, Cássio Santana,Moreira, Diogo Rodrigo Magalh?es,Soares, Milena Botelho Pereira,Leite, Ana Cristina Lima
, p. 191 - 203 (2019/07/16)
Chagas disease is an illness caused by the protozoan parasite Trypanosoma cruzi. The current chemotherapy is based on benznidazole, and, in some countries, Nifurtimox, which is effective in the acute phase of the disease, but its efficacy in the chronic p
Dioxazolones as masked ester surrogates in the Pd(ii)-catalyzed direct C-H arylation of 6,5-fused heterocycles
Saxena, Paridhi,Maida, Neha,Kapur, Manmohan
supporting information, p. 11187 - 11190 (2019/09/30)
A simple and effective Pd(ii)-catalyzed regioselective C(2)-H arylation of 6,5-fused heterocycles with dioxazolones as a masked ester surrogate under mild conditions is reported. The significance of the arylation is highlighted by the new reactivity demonstrated in dioxazolones via proximal C-H activation of the cyclic carbonate of the hydroxamic acid functionality under protic conditions.
The phosphorescent compounds and organic light emitting diode device
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Paragraph 0048-0051, (2017/02/28)
A phosphorescent compound is disclosed. The phosphorescent compound represented by the following Chemical Formula 1, where X, Y, and Z are each selected from the group consisting of carbon and nitrogen, and when x, y, and z are all carbon, R is any one selected from the group consisting of carbazole, α-carboline, β-carboline, γ-carboline, fluorine, dibenzothiophene, dibenzofuran, triphenylsilane, tetraphenylsilane, pyridine, quinoline, isoquinoline, pyrimidine, diphenylphosphineoxide, and substituents thereof.
Synthesis, docking, and in vitro activity of thiosemicarbazones, aminoacyl-thiosemicarbazides and acyl-thiazolidones against Trypanosoma cruzi
Leite, Ana Cristina Lima,de Lima, Renata Souza,Moreira, Diogo Rodrigo de M.,Cardoso, Marcos Verissimo de O.,Gouveia de Brito, Ana Carolina,Farias dos Santos, Luciene Maria,Hernandes, Marcelo Zaldini,Kiperstok, Alice Costa,de Lima, Ricardo Santana,Soares, Milena B.P.
, p. 3749 - 3757 (2007/10/03)
A novel series of thiosemicarbazone and aminoacyl-thiazolidones derivatives were synthesized. Their structure suggests that these compounds could have anti-Trypanosoma cruzi activity. Biological evaluation indicates that some of these compounds are able t
Novel inhibitors of chymase
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Page/Page column 54, (2008/06/13)
The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
C17,20-lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors.
Matsunaga, Nobuyuki,Kaku, Tomohiro,Itoh, Fumio,Tanaka, Toshimasa,Hara, Takahito,Miki, Hiroshi,Iwasaki, Masahiko,Aono, Tetsuya,Yamaoka, Masuo,Kusaka, Masami,Tasaka, Akihiro
, p. 2251 - 2273 (2007/10/03)
Novel nonsteroidal C(17,20)-lyase inhibitors were synthesized using de novo design based on its substrate, 17 alpha-hydroxypregnenolone, and several compounds exhibited potent C(17,20)-lyase inhibition. However, in vivo activities were found to be short-lasting, and in order to improve the duration of action, a series of benzothiophene derivatives were evaluated. As a result, compounds 9h, (S)-9i, and 9k with nanomolar enzyme inhibition (IC(50)=4-9 nM) and 9e (IC(50)=27 nM) were identified to have powerful in vivo efficacy with extended duration of action. The key structural determinants for the in vivo efficacy were demonstrated to be the 5-fluoro group on the benzothiophene ring and the 4-imidazolyl moiety. Superimposition of 9k and 17 alpha-hydroxypregnenolone demonstrated their structural similarity and enabled rationalization of the pharmacological results. In addition, selected compounds were also identified to be potent inhibitors of human enzyme with IC(50) values of 20-30 nM.