A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, SDS of cas: 19035-79-1, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 19035-79-1, Name is Potassium hexadecyl hydrogenphosphate, molecular formula is C16H34KO4P. In an article, author is Zhao, Tong,once mentioned of 19035-79-1.
Discovery of novel indolylarylsulfones as potent HIV-1 NNRTIs via structure-guided scaffold morphing
For more in-depth exploration of the chemical space around the entrance channel of HIV-1 reverse transcriptase (RT), a series of novel indolylarylsulfones (IASs) bearing different chiral N-substituted pyrrolidine, azetidine or substituted sulfonamide groups at indole-2-carboxamide were designed and synthesized as potent HIV NNRTIs by structure-guided scaffold morphing approach. All the IASs exhibited moderate to excellent potency against wild-type HIV-1 with EC50 values ranging from 0.0043 mu M to 4.42 mu M. Notably, compound 27 (EC50= 4.7 nM, SI = 5183) and 33 (EC50= 4.3 nM, SI = 7083) were identified as the most potent compounds, which were more active than nevirapine, lamivudine and efavirenz, and also reached the same order of etravirine. Furthermore, some compounds maintained excellent activity against various single HIV-1 mutants (L100I, K103 N, E138K, Y181C) as well as one double mutant (F227L/V106A) with EC50 values in low-micromolar concentration ranges. Notably, 34 displayed outstanding potency against F2271./V106A (EC50 = 0.094 M), and also showed exceptional activity against E138K (EC50 = 0.014 mu M), L100I (EC50 = 0.011 mu M) and K103 N (EC50 = 0.025 mu M). Additionally, most compounds showed markedly reduced cytotoxicity (CC50) compared to lead compounds, especially 36 (CC50> 234.91 mu M, SI > 18727) and 37 (CC50> 252.49 mu M, SI > 15152). Preliminary SARs and molecular modeling studies were also discussed in detail, which may provide valuable insights for further optimization. (C) 2019 Elsevier Masson SAS. All rights reserved.
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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
,Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis