At 25 °C pyridine has a viscosity of 0.88 mPa/s and thermal conductivity of 0.166 W·m−1·K−1. 16133-25-8, formula is C5H4ClNO2S, Name is Pyridine-3-sulfonyl chloride. The enthalpy of vaporization is 35.09 kJ·mol−1 at the boiling point and normal pressure.The enthalpy of fusion is 8.28 kJ·mol−1 at the melting point. SDS of cas: 16133-25-8.
Fersing, Cyril;Boudot, Clotilde;Paoli-Lombardo, Romain;Primas, Nicolas;Pinault, Emilie;Hutter, Sebastien;Castera-Ducros, Caroline;Kabri, Youssef;Pedron, Julien;Bourgeade-Delmas, Sandra;Sournia-Saquet, Alix;Stigliani, Jean-Luc;Valentin, Alexis;Azqueta, Amaya;Muruzabal, Damian;Destere, Alexandre;Wyllie, Susan;Fairlamb, Alan H.;Corvaisier, Sophie;Since, Marc;Malzert-Freon, Aurelie;Di Giorgio, Carole;Rathelot, Pascal;Azas, Nadine;Courtioux, Bertrand;Vanelle, Patrice;Verhaeghe, Pierre research published 《 Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties》, the research content is summarized as follows. To study the antikinetoplastid 3-nitroimidazo[1,2-a]pyridine pharmacophore, a structure-activity relationship study was conducted through the synthesis of 26 original derivatives and their in vitro evaluation on both Leishmania spp and Trypanosoma brucei brucei. This SAR study showed that the antitrypanosomal pharmacophore was less restrictive than the antileishmanial one and highlighted positions 2, 6 and 8 of the imidazopyridine ring as key modulation points. None of the synthesized compounds allowed improvement in antileishmanial activity, compared to previous hit mols. in the series. Nevertheless, compound 8, the best antitrypanosomal mol. in this series (EC50 = 17 nM, SI = 2650 & E° = -0.6 V), was not only more active than all reference drugs and previous hit mols. in the series but also displayed improved aqueous solubility and better in vitro pharmacokinetic characteristics: good microsomal stability (T1/2 > 40 min), moderate albumin binding (77%) and moderate permeability across the blood brain barrier according to a PAMPA assay. Moreover, both micronucleus and comet assays showed that nitroarom. mol. 8 was not genotoxic in vitro. It was evidenced that bioactivation of mol. 8 was operated by T. b. brucei type 1 nitroreductase, in the same manner as fexinidazole. Finally, a mouse pharmacokinetic study showed that 8 displayed good systemic exposure after both single and repeated oral administrations at 100 mg/kg (NOAEL) and satisfying plasmatic half-life (T1/2 = 7.7 h). Thus, mol. 8 appears as a good candidate for initiating a hit to lead drug discovery program.
SDS of cas: 16133-25-8, Pyridine-3-sulfonyl chloride is a useful research compound. Its molecular formula is C5H4ClNO2S and its molecular weight is 177.61 g/mol. The purity is usually 95%.
Pyridine-3-sulfonyl chloride is a reagent used in the synthesis of pyrimidine derivatives with anti-proliferative activity against negative breast cancer cells.
Pyridine-3-sulfonyl chloride is a chemical compound that binds to the active site of cytochrome P450 enzymes. It can be used to study the effects of matrix effect on reaction solution. Pyridine-3-sulfonyl chloride has been shown to have an UV absorption spectrum with a maximum at 280 nm and a p450 activity that is proportional to the concentration of human serum. This compound has been shown to inhibit kinase domain in vitro assays, which may have clinical relevance in the treatment of obesity., 16133-25-8.