A new series of octadec-9-enoic acid schiff base entities (S1-S30) were designed and synthesized targeting peroxisome proliferator activated receptor-gamma for agonist action. Molinspiration software (online) was used to estimate drug like molecular properties of the metabolites. Docking disquisition on co-crystallized protein of PPAR-γ (PDB ID 1FM9) was carried out which showed S21, S10 and S7 as best situated in the vital sites of receptor having docking scores -9.19, -8.68 and -8.64 respectively. Free binding energy measured using model of Maestro 9.0 and was in range of from -40.01 and -80.54 kcal/mol, significant when compared with pioglitazone (-51.58 Kcal/mol). Seven best docked derivatives were assessed for in-vivo oral glucose tolerance on normal rats and anti-hyperglycaemic activity by streptozotocin induced diabetes model. S21 unveiled to be the best measured analogue among all the synthesized entities. Encouraging outcomes motivates fatty acids for further development of more effective and safer compounds.

中文翻译：

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十八烷基-9-烯酸中新型席夫碱衍生物的合成，ADME，对接研究和体内抗高血糖潜能估计。

设计并合成了一系列新的十八烷基-9-烯酸席夫碱实体（S1-S30），靶向过氧化物酶体增殖物激活的受体-γ，以产生激动剂作用。使用Molinspiration软件（在线）来估算代谢物的类药物分子性质。对PPAR-γ（PDB ID 1FM9）的共结晶蛋白进行了对接鉴定，结果表明S21，S10和S7分别位于对接分数分别为-9.19，-8.68和-8.64的受体的重要部位。使用Maestro 9.0模型测得的自由结合能在-40.01和-80.54 kcal / mol范围内，与吡格列酮相比是显着的（-51.58 Kcal / mol）。通过链脲佐菌素诱导的糖尿病模型评估了七种最佳对接衍生物的正常大鼠体内口服葡萄糖耐量和抗高血糖活性。S21被公认为是所有合成实体中测量最好的类似物。令人鼓舞的结果激励脂肪酸进一步开发更有效，更安全的化合物。