326-69-2Relevant articles and documents
Discovery of novel oral protein synthesis inhibitors of mycobacterium tuberculosis that target leucyl-tRNA synthetase
Palencia, Andrés,Li, Xianfeng,Bu, Wei,Choi, Wai,Ding, Charles Z.,Easom, Eric E.,Feng, Lisa,Hernandez, Vincent,Houston, Paul,Liu, Liang,Meewan, Maliwan,Mohan, Manisha,Rock, Fernando L.,Sexton, Holly,Zhang, Suoming,Zhou, Yasheen,Wan, Baojie,Wang, Yuehong,Franzblau, Scott G.,Woolhiser, Lisa,Gruppo, Veronica,Lenaerts, Anne J.,O'Malley, Theresa,Parish, Tanya,Cooper, Christopher B.,Waters, M. Gerard,Ma, Zhenkun,Ioerger, Thomas R.,Sacchettini, James C.,Rullas, Joaquín,Angulo-Barturen, I?igo,Pérez-Herrán, Esther,Mendoza, Alfonso,Barros, David,Cusack, Stephen,Plattner, Jacob J.,Alley
supporting information, p. 6271 - 6280 (2016/11/06)
The recent development and spread of extensively drug-resistant and totally drug-resistant resistant (TDR) strains of Mycobacterium tuberculosis highlight the need for new antitubercular drugs. Protein synthesis inhibitors have played an important role in
2-AMINOINDOLE COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA
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Page/Page column 90-91, (2011/05/11)
The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)- The values and preferred values of the variables in Structural Formula I are defined herein.
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs
Cantrell, Amanda S.,Engelhardt, Per,H?gberg, Marita,Jaskunas, S. Richard,Johansson, Nils Gunnar,Jordan, Christopher L.,Kangasmets?, Jussi,Kinnick, Michael D.,Lind, Peter,Morin Jr., John M.,Muesing,Noreén, Rolf,?berg, Bo,Pranc, Paul,Sahlberg, Christer,Ternansky, Robert J.,Vasileff, Robert T.,Vrang, Lotta,West, Sarah J.,Zhang, Hong
, p. 4261 - 4274 (2007/10/03)
Phenylethylthiazolylthiourea (PETT) derivatives have been identified as a new series of nonnucleoside inhibitors of HIV-1 RT. Structure-activity relationship studies of this class of compounds resulted in the identification of N-[2-(2-pyridyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea hydrochloride (trovirdine; LY300046.HCl) as a highly potent anti-HIV-1 agent. Trovirdine is currently in phase one clinical trials for potential use in the treatment of AIDS. Extension of these structure-activity relationship studies to identify additional compounds in this series with improved properties is ongoing. A part of this work is described here. Replacement of the two aromatic moleties of the PETT compounds by various substituted or unsubstituted heteroaromatic rings was investigated. In addition, the effects of multiple substitution in the phenyl ring were also studied. The antiviral activities were determined on wild-type and constructed mutants of HIV-1 RT and on wild-type HIV-1 and mutant viruses derived thereof, Ile100 and Cys181, in cell culture assays. Some selected compounds were determined on double- mutant viruses, HIV-1 (Ile100/Asn103) and HIV-1 (Ile100/Cys181). A number of highly potent analogs were synthesized. These compounds displayed IC50's against wild-type RT between 0.6 and 5 nM. In cell culture, these agents inhibited wild-type HIV-1 with ED50's between I and 5 nM in MT-4 cells. In addition, these derivatives inhibited mutant HIV-1 RT (Ile 100) with IC50's between 20 and 50 nM and mutant HIV-1 RT (Cys 181) with IC50's between 4 and 10 nM, and in cell culture they inhibited mutant HIV-1 (Ile100) with ED50's between 9 and 100 nM and mutant HIV-1 (Cys181) with ED50's between 3 and 20 nM.