期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 62, 期 9, 页码 4500-4525出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b00056
关键词
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资金
- Canadian Institutes of Health Research (CIHR) [337381]
- Natural Sciences and Engineering Research Council of Canada (NSERC) [337381]
- Shastri Indo-Canadian Institute, India
Peptide mimicry employing a combination of aza-amino acyl proline and indolizidinone residues has been used to develop allosteric modulators of the prostaglandin F2a receptor. The systematic study of the N-terminal phenylacetyl moiety and the conformation and side chain functions of the central turn dipeptide residue has demonstrated the sensitive relationships between modulator activity and topology. Examination of aza-Gly-Pro and aza-Phe-Pro analogs 2a and 2b in a murine preterm labor model featuring treatment with lipopolysaccharide demonstrated their capacity to extend significantly (>20 h) the average time of delivery offering new prototypes for delaying premature birth.
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