Extracurricular laboratory:new discovery of tert-Butyl piperidin-4-ylcarbamate

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Application of 73874-95-0, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 73874-95-0, Name is tert-Butyl piperidin-4-ylcarbamate, molecular formula is C10H20N2O2. In a Article£¬once mentioned of 73874-95-0

Exploiting the Tolerant Region i of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles

Diarylpyrimidine derivatives (DAPYs) exhibit robust anti-HIV-1 potency, although they have been compromised by E138K variant and severe side-effects and been suffering from poor water solubility. In the present work, hydrophilic morpholine or methylsulfonyl and sulfamide-substituted piperazine/piperidines were introduced into the right wing of DAPYs targeting the solvent-exposed tolerant region I. The anti-HIV-1 activities of 11c (EC50(WT) = 0.0035 muM, EC50(E138K) = 0.0075 muM) were the same as and 2-fold better than that of the lead etravirine against the wild-type and E138K mutant HIV-1, respectively, with a relative low cytotoxicity (CC50 ? 173 muM). Further test showed a significant improvement in the water solubility of 11c. Besides, 11c displayed no significant inhibition on main cytochrome P450 enzymes and exhibited no acute/subacute toxicities at doses of 2000 mg¡¤kg-1/50 mg¡¤kg-1 in mice. Taken together, we consider that 11c is a promising lead for further structural optimization.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H14261N – PubChem