The diphenylsulfonyl sulfonamide scaffold represented by 1 (WAY-316606) are small molecule inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. Modulators of the Wnt pathway have been proposed as anabolic agents for the treatment of osteoporosis or other bone-related disorders. Details of the structure-activity relationships and biological activity from the first structural class of this scaffold will be discussed.
The synthesis and in vitro antibacterial profile of several novel C-4 substituted monobactam analogs are reported.Continuing efforts in these laboratories have focused on the design and synthesis of novel 4-substituted monobactamderivatives.^Our interest in this area was in response to the excellent activity displayed from the monobactamantibiotic azthreonam,2) and more recently carumonam.3) Herein is reported the results of our detailed study concerning the synthesis and antibacterial profile Scheme 1.
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