作为HIV蛋白酶抑制剂的对称和不对称P1/P1'环脲的合成。
The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors.
作者信息
Patel M, Kaltenbach R F, Nugiel D A, McHugh R J, Jadhav P K, Bacheler L T, Cordova B C, Klabe R M, Erickson-Viitanen S, Garber S, Reid C, Seitz S P
机构信息
Department of Chemical & Physical Sciences, DuPont Merck Pharmaceutical Company, Wilmington, DE 19880-0500, USA.
出版信息
Bioorg Med Chem Lett. 1998 May 5;8(9):1077-82. doi: 10.1016/s0960-894x(98)00175-9.
Cyclic urea SD146, a potent HIV protease inhibitor bearing a flat resistance profile, possessed poor solubility and bioavailability, which precluded further development of the compound. In an effort to improve upon the pharmacokinetic profile of the compound, several analogs modified at the P1/P1' residues were prepared and evaluated. Several of those compounds displayed significant improvement of physical properties.
环状尿素SD146是一种具有平坦耐药性的强效HIV蛋白酶抑制剂，但其溶解度和生物利用度较差，这阻碍了该化合物的进一步开发。为了改善该化合物的药代动力学特性，制备并评估了几种在P1/P1'残基处进行修饰的类似物。其中几种化合物的物理性质有显著改善。
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