210686-44-5Relevant academic research and scientific papers
N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480
Artico, Marino,Mai, Antonello,Sbardella, Gianluca,Massa, Silvio,Lampis, Giorgio,Deidda, Delia,Pompei, Raffaello
, p. 1493 - 1498 (1998)
Thiomorpholine analogues of U-100480 with the biphenylmethyl group replacing the acetamidomethyloxazolidinone moiety have been synthesized and tested as antimycobacterial agents together with various related derivatives. Some biphenyl derivatives were endowed with high activity against Mycobacterium tuberculosis and other non-tuberculous mycobacteria.
Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp3 values and favorable drug-like properties
Jiang, Xiangyi,Huang, Boshi,Olotu, Fisayo A.,Li, Jing,Kang, Dongwei,Wang, Zhao,De Clercq, Erik,Soliman, Mahmoud E.S.,Pannecouque, Christophe,Liu, Xinyong,Zhan, Peng
, (2020/12/07)
To yield potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with favorable drug-like properties, a series of novel diarylpyrimidine derivatives targeting the tolerant region I of the NNRTI binding pocket were designed, synthesized and b
Diarylpyrimidine derivative containing six-membered nitrogen heterocyclic ring as well as preparation method and application of diarylpyrimidine derivative
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, (2020/12/15)
The invention discloses a diarylpyrimidine compound containing a six-membered nitrogen heterocyclic ring as well as a preparation method and application of the diarylpyrimidine compound. The compoundhas a structure as shown in a general formula I in the s
Substituted indolines which inhibit receptor tyrosine kinases
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Page column 48, (2008/06/13)
Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
Substituted indolinones with kinase inhibitory activity
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, (2008/06/13)
Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-a
N-[4-(1,1'-biphenylyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines, a new class of synthetic antituberculosis agents active against Mycobacterium avium
Mai, Antonello,Sbardella, Gianluca,Artico, Marino,Massa, Silvio,Lampis, Giorgio,Deidda, Delia,Pompeit, Raffaello
, p. 149 - 161 (2007/10/03)
Various N-derivatives of 4-(4-thiomorpholinyl)aniline and 4-(4- thiomorpholinylmethyl)aniline were synthesized and tested for in vitro antibacterial activities against Mycobacterium avium CIP 103317 and other mycobacteria including M. tuberculosis CIP 103471. Appropriate substituents were introduced at the nitrogen of aniline portion in order to exploit their potential antimycobacterial activities. Only derivatives with the biphenylylmethyl group bound to the 4-(4-thiomorpholinylmethyl)aniline moiety were found to possess appreciable antibacterial activities against atypical mycobacteria and M. tuberculosis. Several compounds (7c-g and 7j) were two and sixteen times more potent than azithromycin and isoniazid, respectively, in the in vitro assays against M. avium.
Antimycobacterial activity of new ortho-, meta- and para-toluidine derivatives
Biava, Mariangela,Fioravanti, Rossella,Porretta, Giulio Cesare,Sleiter, Giancarlo,Deidda, Delia,Lampis, Giorgio,Pompei, Raffaello
, p. 721 - 727 (2007/10/03)
Novel toluidine derivatives are described. Some of them showed an interesting in vitro activity against Mycobacterium tuberculosis, M. smegmatis, M. marinum, M. gordonae, and M. avium. Some of them were more active than Streptomycin and Isoniazid, which were used as controls, against M. avium and M. gordonae. In particular, we confirm the good activity of biphenyl derivatives.
