Synthesis of 5- and 7-hydroxy indolizidin-2-one prostaglandin-F2α modulators and activity on myometrial contractility towards development of agents for delaying preterm birth,Journal of Peptide Science

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Synthesis of 5- and 7-hydroxy indolizidin-2-one prostaglandin-F2α modulators and activity on myometrial contractility towards development of agents for delaying preterm birth
Journal of Peptide Science ( IF 1.8 ) Pub Date : 2022-10-02 , DOI: 10.1002/psc.3455
Ramakotaiah Mulamreddy ₁ , Xin Hou ₂ , Sylvain Chemtob ₂ , William D Lubell ₁

Affiliation

In pursuit of more effective-labor delaying tocolytic agents, the prostaglandin F2α (PGF2α) receptor (FP) modulator PDC113.824 [(6S)-2] represents a potent lead for developing therapy to treat preterm birth. Derivatives of FP modulator (6S)-2 were synthesized, possessing respectively 5- and 7-hydroxyl groups on the indolizidin-2-one amino acid (I²aa) residue. The effects of the alcohol substituents were examined in a PGF2α-induced myometrial contraction assay. Based on knowledge of dihedral angle values of model I²aa peptides from X-ray analyses, the results of the study indicate respectively encouraging and limited potential for creating improved tocolytic agents by modifications at the 5- and 7-positions.

中文翻译：

5- 和 7-羟基 indolizidin-2-one 前列腺素-F2α 调节剂的合成及其对子宫肌层收缩力的活性对延缓早产药物的开发

为了寻找更有效的分娩延迟宫缩抑制剂，前列腺素 F2α (PGF2α) 受体 (FP) 调节剂 PDC113.824 [(6 S )- 2 ] 代表了开发治疗早产疗法的有力先导。合成了FP 调节剂 (6 S )-2的衍生物，在 indolizidin-2-one 氨基酸 (I ² aa) 残基上分别具有 5- 和 7- 羟基。在 PGF2α 诱导的子宫肌层收缩试验中检查了醇取代基的影响。^{基于模型 I 2}的二面角值的知识aa 来自 X 射线分析的肽，该研究的结果分别表明通过在 5 位和 7 位进行修饰来产生改进的宫缩抑制剂的潜力是令人鼓舞的和有限的。

更新日期：2022-10-02

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