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Bioorg Med Chem. 2010 May 1;18(9):3307-19. doi: 10.1016/j.bmc.2010.03.014. Epub 2010 Mar 11.

Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation.

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Pfizer Global Research and Development, La Jolla Laboratories, 10770 Science Center Drive, San Diego, CA 92121, USA.

Erratum in

  • Bioorg Med Chem. 2010 Oct 1;18(19):7144. Meador, James W 3rd [added]; Paz, Robert L [added].


A novel series of potent thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV was discovered using structure-based drug design. Synthesis, structure-activity relationship, and optimization of physicochemical properties are described. Low nanomolar potency was achieved, and selected compounds with improved thermodynamic solubility showed promising in vitro inhibition of carbonic anhydrase activity in rabbit iris ciliary body homogenate.

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