Synthesis of 3-Amino-l-CarboxymethyI-Benzodiazepine (BZA) Peptidomimetics
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Replacement of key structural or binding elements of a peptide lead with nonpeptide components can improve affinity and metabolic stability (1 –5 ). Such a strategy was successfully applied to the generation of potent, cell-permeable inhibitors of Ras famesyltransferase (FTase) (6 ,7 ). The central pair of amino acids in the CAAX tetrapeptide was replaced with the nonpeptide scaffold 3-methylamino-1-carboxymethyl-2,3-dihydro-5-phenyl-1H-1,4-benzodiazepin-2-one, (N -Me)BZA, shown below.
![1-(6-amino-3,5-difluoro-2-pyridyl)-7-[[3-[1-[1-(6-amino-3,5-difluoro-2-pyridyl)-3-carboxy-8-chloro-6-fluoro-4-oxo-7-quinolyl]azetidin-3-yl]oxy-2-hydroxy-propyl]amino]-8-chloro-6-fluoro-4-oxo-quinoline-3-carboxylic acid，1093185-35-3，阿拉丁](https://img1.dxycdn.com/p/s14/2024/0619/630/0420372030125733081.jpg!wh200)
