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The incidence of preterm birth has been steadily increasing over the past thirty years, and presently, preterm delivery accounts for >75% of all neonatal deaths [1]. The prostaglandin F2α receptor (FP) is responsible for initiating labor and preterm labor [2]. In pursuit of drugs to delay uterine contractions and prolong pregnancy, FP has been targeted based on peptide leads using a peptidomimetic approach. For example, the indolizidin-2-one amino acid analogue PDC113.824 (1) [3] and aza-phenylalanine analogue 2 (Figure 1) [4], both reduced prostaglandin-F2α-induced myometrial contractions by modulating G protein signaling pathways. Studies of structure-activity relationships of aza-amino acyl proline modulators such as 2 have shown that biological activity was contingent on the aza-amino acyl residue side chain [4]. Considering that structural modification of the aza-residue may have consequences on function, we are exploring diversity-oriented synthesis featuring alkylation of the aza-glycinyl-proline residue to introduce different side chains onto the aza-peptide modulators. In this report, we describe the synthesis of aza-p-methylphenylalanine analogue 3.

Synthesis and Evaluation of Azapeptide Prostaglandin F2α Receptor Modulators in Pursuit of Inhibitors of Preterm Labor