Sulfonamides SOSA approach

Fig. 1.16 A successful SOSA approach allowed the identification of the antibacterial sulfonamide sulfathiazole as a ligand of the endothelin ETfl receptor and its optimization to the selective and potent compounds BMS-182874, BMS-193884, and BMS-207940 [34,35],...

Among them, a typical illustration of the SOSA approach is shown by the development of a selective ligand for the endotheline ETa receptors by scientists from Bristol-Myers-Squibb. " Starting from an in-house library, the antibacterial compound sulfathiazole (Fig. 5.13) was an initial, but weak, hit (IC50 = 69 p,M). Testing of related sulfonamides identified the more potent sulfisoxazole (IC50 = 0.78 xM). Systematic variations led finally to the potent and selective... 

---