863111-54-0Relevant academic research and scientific papers
Structure-Based Design and Synthesis of Piperidinol-Containing Molecules as New Mycobacterium abscessus Inhibitors
Biot, Christophe,Blaise, Micka?l,Dubar, Faustine,Dupont, Christian,Grassin-Delyle, Stanislas,Guérardel, Yann,Herrmann, Jean-Louis,Kremer, Laurent,Lamy, Elodie,Le Moigne, Vincent,de Ruyck, Jér?me
, p. 351 - 365 (2020/04/15)
Non-tuberculous mycobacterium (NTM) infections, such as those caused by Mycobacterium abscessus, are increasing globally. Due to their intrinsic drug resistance, M. abscessus pulmonary infections are often difficult to cure using standard chemotherapy. We previously demonstrated that a piperidinol derivative, named PIPD1, is an efficient molecule both against M. abscessus and Mycobacterium tuberculosis, the agent of tuberculosis, by targeting the mycolic acid transporter MmpL3. These results prompted us to design and synthesize a series of piperidinol derivatives and to determine the biological activity against M. abscessus. Structure-activity relationship (SAR) studies pointed toward specific sites on the scaffold that can tolerate slight modifications. Overall, these results identified FMD-88 as a new promising active analogue against M. abscessus. Also, we determined the pharmacokinetics properties of PIPD1 and showed that intraperitoneal administration of this compound resulted in promising serum concentration and an elimination half-life of 3.2 hours.
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity
Ashraf-Uz-Zaman, Md,Sajib, Md Sanaullah,Cucullo, Luca,Mikelis, Constantinos M.,German, Nadezhda A.
supporting information, p. 3652 - 3657 (2018/11/03)
Several recent reports have highlighted the feasibility of the use of penfluridol, a well-known antipsychotic agent, as a chemotherapeutic agent. In vivo experiments have confirmed the cytotoxic activity of penfluridol in triple-negative breast cancer model, lung cancer model, and further studies have been proposed to assess its anticancer activity and viability for the treatment of glioblastomas. However, penfluridol anticancer activity was observed at a dosage significantly higher than that administered in antipsychotic therapy, thus raising the concern for the potential onset of CNS side effects in patients undergoing intensive pharmacological treatment. In this study, we evaluate the potential CNS toxicity of penfluridol side by side with a set of analogs.
DIPHENYLBUTYPIPERIDINE AUTOPHAGY INDUCERS
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Page/Page column 7; 84-85, (2011/12/02)
Autophagy inducing compounds, methods of their preparation and use, and kits containg said compounds are disclosed herein.
DISUBSTITUTED PHENYLPIPERIDINES AS MODULATORS OF CORTICAL CATECHOLAMINERGIC NEUROTRANSMISSION
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Page/Page column 33, (2010/11/27)
The present invention relates to compounds of the formulae (4), (5) or (6), and their use in the treatment of central nervous system disorders.
NEW SUBSTITUTED PIPERIDINES AS MODULATORS OF DOPAMINE NEUROTRANSMISSION
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Page/Page column 31, (2008/06/13)
The present invention relates to compounds having therapeutic effects against disorders in the central nervous system, and in particular substituted hydroxypiperidines of the formula 1: wherein R1, R2, and R3 are as defined herein.
