Abstract
N-Alkylation and N-acylation of the prostaglandin-F2α allosteric modulator l-PDC31 were performed to install various alkyl, PEG and isoprenoid groups onto the l-enantiomer of the peptide. Among the different bio-conjugates studied, the N-dodecyl analog reduced prostaglandin-F2α-induced mouse myometrium contractions ex vivo. Furthermore, N-dodecyl-l-PDC31 exhibited improved stability in a mouse serum assay, likely due to protection from protease degradation by the lipid chain.
Highlights
Preterm labor is a challenging contemporary target of modern medicinal chemistry
Ineffective healthcare to treat mother and child in less affluent countries is associated with a higher percentage of neonatal and infantile mortality: 90% for very preterm babies of
Dodecanal and farnesol were purchased from commercial sources and used without further purification
Summary
Preterm labor is a challenging contemporary target of modern medicinal chemistry. Preterm birth (PTB), defined as less than 37 weeks of gestational age, accounts for 5–13% of all births [1].Responsible for an increased risk of neonatal and infantile mortality [2] PTB is associated with various other complications, including developmental disorders [3], vision and hearing impairments [4,5], and chronic metabolic conditions [6]. Preterm labor is a challenging contemporary target of modern medicinal chemistry. Preterm birth (PTB), defined as less than 37 weeks of gestational age, accounts for 5–13% of all births [1]. Responsible for an increased risk of neonatal and infantile mortality [2] PTB is associated with various other complications, including developmental disorders [3], vision and hearing impairments [4,5], and chronic metabolic conditions [6]. PTB is more problematic: >60% of PTBs occur in Africa and South-Asia. Ineffective healthcare to treat mother and child in less affluent countries is associated with a higher percentage of neonatal and infantile mortality: 90% for very preterm babies of
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