Nanodiamond-Enabled Thin-Film Nanocomposite Polyamide Membranes for High-Temperature Water Treatment.

Despite growing demands for high-temperature wastewater treatment, most available polymeric membranes are limited to mild operating temperatures (<50 °C) and become less efficient at high temperatures. Herein we show how to make thermally stable reverse osmosis thin-film nanocomposite (TFN) membranes by embedding nanodiamond (ND) particles. Polyamide composite layers containing different loadings of surface-modified ND particles were synthesized through interfacial polymerization. The reactive functional groups and the hydrophilic surface of the NDs intensified the interactions of the nanoparticles with the polymer matrix and increased the surface wettability of the TFN membranes. Contact angle measurement showed a maximum decrease from 88.4° for the pristine membrane to 58.3° for the TFN membrane fabricated with 400 ppm ND particles. The addition of ND particles and ethyl acetate created larger surface features on the polyamide surface of TFN membranes. The average roughness of the membranes increased from 108.4 nm for the pristine membrane to 177.5 nm for the TFN membrane prepared with highest ND concentration. The ND-modified TFN membranes showed a higher pure water flux (up to 76.5 LMH) than the pristine membrane (17 LMH) at ambient temperature at 220 psi and room temperature. The TFN membrane with the highest loading of ND particles overcame the trade-off relation between the water flux and NaCl rejection with 76.5 LMH and 97.3% when 2000 ppm of NaCl solution was filtered at 220 psi. Furthermore, with increasing ND concentration, the TFN membrane showed a lower flux decline at high temperatures over time. The TFN400 prepared with 400 ppm of m-phenylene diamine functionalized ND particles had a 13% flux decline over a 9 h filtration test at 75 °C. This research provides a promising path to the development of high-performance TFN membranes with enhanced thermal stability for the treatment of wastewaters at high temperatures.

Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.

Optimization of pyridine-based noncatalytic site integrase inhibitors (NCINIs) based on compound 2 has led to the discovery of molecules capable of inhibiting virus harboring N124 variants of HIV integrase (IN) while maintaining minimal contribution of enterohepatic recirculation to clearance in rat. Structure-activity relationships at the C6 position established chemical space where the extent of enterohepatic recirculation in the rat is minimized. Desymmetrization of the C4 substituent allowed for potency optimization against virus having the N124 variant of integrase. Combination of these lessons led to the discovery of compound 20, having balanced serum-shifted antiviral potency and minimized excretion in to the biliary tract in rat, potentially representing a clinically viable starting point for a new treatment option for individuals infected with HIV.

Potent triazolyl-proline-based inhibitors of HCV NS3 protease.

The design and synthesis of tripeptide-based inhibitors of the HCV NS3 protease containing a novel P2-triazole is described. Replacement of the P2 quinoline with a triazole moiety provided a versatile handle which could be expediently modified to generate a diverse series of inhibitors. Further refinement by the incorporation of an aryl-substituted triazole and replacement of the P1 acid with an acyl sulfonamide ultimately provided inhibitors with interesting cellular activity.