679409-18-8Relevant articles and documents
Synthesis and antimalarial activity of 1,4-disubstituted piperidine derivatives
Seck, Rokhyatou,Gassama, Abdoulaye,Cojean, Sandrine,Cavé, Christian
, (2020/01/31)
In order to prepare, at low cost, new compounds active against Plasmodium falciparum, and with a less side-effects, we have designed and synthesized a library of 1,4-disubstituted piperidine derivatives from 4-aminopiperidine derivatives 6. The resulting compound library has been evaluated against chloroquine-sensitive (3D7) and chloroquine-resistant (W2) strains of P. falciparum. The most active molecules—compounds 12d (13.64 nM (3D7)), 13b (4.19 nM (3D7) and 13.30 nM (W2)), and 12a (11.6 nM (W2))—were comparable to chloroquine (22.38 nM (3D7) and 134.12 nM (W2)).
Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats
Duan, Maosheng,Kazmierski, Wieslaw M.,Chong, Pek Y.,DeAnda, Felix,Edelstein, Mark,Ferris, Rob,Peckham, Jennifer,Wheelan, Pat,Xiong, Zhiping,Zhang, Huichang,Nishizawa, Rena,Takaoka, Yoshikazu
scheme or table, p. 6470 - 6475 (2011/11/29)
A novel series of pyridyl carboxamide-based CCR5 inhibitors was designed, synthesized, and demonstrated to be highly potent against HIV-1 infection in both HOS and PBL assays. Attempts to evaluate this series of compounds in a rat PK model revealed its instability in rat plasma. A hypothesis for this liability was proposed, and strategies to overcome this issue were pursued, leading to discovery of highly potent 40 and 41, which featured dramatically improved rat PK profiles. 2011 Elsevier Ltd. All rights reserved.
CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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Page/Page column 11-12, (2009/07/17)
The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acq