A new annular centrifugal contactor capable of rapid disassembly for inspection and cleaning is presented. The unique design enhances the utility of this liquid-liquid centrifuge in processes requiring cleaning and inspection of all wetted parts. This new model differs from previous designs in that it can be manufactured to meet the requirements of the pharmaceutical industry. Annular centrifugal contactors are vertical, direct-drive centrifuges providing an efficient mixing and separation device in a single unit. They can be directly coupled for multiple-stage processes. Other features include small hold up volume, rapid start-up and shutdown, variable speed control, interchangeable heavy phase weirs, and very compact size. Mixing and disengaging residence times of 3 and 20 s, respectively, are typical. Single stage efficiencies for processes with rapid kinetics are greater than 90%. Annular centrifugal contactors can be used to convert processes from batch to continuous due to their ability to handle intermittent feed flows and 100% phase ratio changes.
(E)-3-(2-Carboxy-2-phenylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acid, 1, is a potent and selective antagonist of the glycine site of the N-methyl-d-aspartate (NMDA) receptor. Using 3D comparative molecular field analysis (CoMFA) to guide the synthetic effort, a series of aryl diacid analogues of 1 were synthesized to optimize in vivo potency, duration of action, and binding activity. It was found that the incorporation of a substituted aromatic with an electron withdrawing group or a heterocyclic group at the 2-position of the 3-propenyl moiety of 1 gave compounds with better affinity and potency in the murine stroke model. Ultimately this led to the discovery of 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, 19, as a new potent selective glycine-site NMDA receptor antagonist.
The 4-Isoxazolyl-dihydropyridines (IDHPs) exhibit inhibition of the multidrug-resistance transporter (MDR-1), and exhibit an SAR distinct from their activity at voltage gated calcium channels (VGCC). Among the four most active IDHPs, three were branched at C-5 of the isoxazole, including the most active analog, 1k.
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