891854-16-3Relevant academic research and scientific papers
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses
Tang, Guozhi,Kertesz, Denis J.,Yang, Minmin,Lin, Xianfeng,Wang, Zhanguo,Li, Wentao,Qiu, Zongxing,Chen, Junli,Mei, Jianghua,Chen, Li,Mirzadegan, Taraneh,Harris, Seth F.,Villase?or, Armando G.,Fretland, Jennifer,Fitch, William L.,Hang, Julie Qi,Heilek, Gabrielle,Klumpp, Klaus
scheme or table, p. 6020 - 6023 (2010/11/05)
Further investigation of the recently reported piperidine-4-yl- aminopyrimidine class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been carried out. Thus, preparation of a series of N-phenyl piperidine analogs resulted in the identification of 3-carboxamides as a particularly active series. Analogs such as 28 and 40 are very potent versus wild-type HIV-1 and a broad range of NNRTI-resistant mutant viruses. Synthesis, structure-activity relationship (SAR), clearance data, and crystallographic evidence for the binding motif are discussed.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 31; 32, (2008/12/06)
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
Tricyclic pharmacophore-based molecules as novel integrin αvβ3 antagonists. Part IV: Preliminary control of αvβ3 selectivity by meta-oriented substitution
Kubota, Dai,Ishikawa, Minoru,Ishikawa, Midori,Yahata, Naokazu,Murakami, Shoichi,Fujishima, Kazuyuki,Kitakaze, Masafumi,Ajito, Keiichi
, p. 4158 - 4181 (2007/10/03)
To establish the in vivo efficacy of αvβ3/αIIbβ3 dual antagonists possessing a tricyclic pharmacophore, a corresponding αvβ3-selective antagonist was required as a control. We initially too
