Natural Product-Based Drugs Discovery: Semisynthesis and Biological Evaluation of Ester Derivatives from Pregn-5-ene-3β,17α,20(S)-triol

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  • Li Tian
    College of Plant Protection, Northwest A&F University
  • Hu Yuxiao
    College of Plant Protection, Northwest A&F University
  • Shi Baojun
    College of Plant Protection, Northwest A&F University Shaanxi Province Key Laboratory Research & Development on Botanical Pesticide, Northwest A&F University
  • Wu Wenjun
    College of Plant Protection, Northwest A&F University Shaanxi Province Key Laboratory Research & Development on Botanical Pesticide, Northwest A&F University

抄録

<p>There is no doubt that derivation of intermediates from natural product is a very efficient way to develop new environmentally friendly pesticide. We synthesis a succession of compounds esterified with pregn-5-ene-3β,17α,20(S)-triol to evaluate its insecticidal and bacteriostatic activity. Otherwise, their structure–activity relationships (SAR) are also discussed. As a result, compounds 7g, 7h, 7j, 7l and 7o exhibit more obvious insecticidal activity against 3rd Mythimna separata Walker (LC50 = 0.60, 0.68, 0.79, 0.85 and 0.78 mg/mL, respectively) than periplocoside F (PSF). Meanwhile, compounds 7g, 7h and 7i perform well inhibitory activity against Pseudomas syringae pv. actinidiae (Psa) in vitro (minimum inhibitory concentration (MIC) values: 0.10–0.25 mg/mL, minimum bactericidal concentration (MBC) values: 0.15–0.35 mg/mL). And SAR analysis indicates that the replacement and position of fluorine atom on benzoyl are highly vital to biological activity.</p>

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