El-Naggar Mai H, Elgaml Abdelaziz, Abdel Bar Fatma M, Badria Farid A
a Department of Pharmacognosy, Faculty of Pharmacy , Sohag University , Sohag , Egypt.
b Department of Pharmacognosy, Faculty of Pharmacy , Mansoura University , Mansoura , Egypt.
Nat Prod Res. 2019 Jun;33(11):1556-1562. doi: 10.1080/14786419.2017.1423306. Epub 2018 Jan 15.
Ricinine (), a known major alkaloid in plant, was used as a starting compound for the synthesis of six ricinine derivatives; two new and four known compounds. The new derivatives; 3-amino-5-methyl-1-pyrazolo[4,3-c]pyridin-4(5)-one (), and 3-amino-5-methyl-1-(phenylsulfonyl)-1-pyrazolo[4,3-c]pyridin-4(5)-one (), as well as the previously prepared derivatives (-) were subjected for antimicrobial and antiquorum-sensing evaluation in comparison to different extracts. Acetyl ricininic acid derivative ( showed the highest antimicrobial activity among all tested derivatives against , , , and . However, compound (4-methoxy-1-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide) showed the highest antiquorum-sensing activity among all tested compounds and extracts. These findings proved the usefulness of ricinine as a good scaffold for the synthesis of new antimicrobial and antiquorum-sensing derivatives in spite of its poor contribution to the antimicrobial activity of the plant extracts.
蓖麻碱（），一种已知的植物主要生物碱，被用作合成六种蓖麻碱衍生物的起始化合物；两种新化合物和四种已知化合物。新衍生物；3-氨基-5-甲基-1-吡唑并[4,3-c]吡啶-4(5)-酮（）和3-氨基-5-甲基-1-(苯磺酰基)-1-吡唑并[4,3-c]吡啶-4(5)-酮（），以及先前制备的衍生物（-），与不同提取物相比，进行了抗菌和群体感应抑制评估。乙酰蓖麻酸衍生物（在所有测试衍生物中对、、、和显示出最高的抗菌活性。然而，化合物（4-甲氧基-1-甲基-2-氧代-1,2-二氢吡啶-3-甲酰胺）在所有测试化合物和提取物中显示出最高的群体感应抑制活性。这些发现证明了蓖麻碱作为合成新型抗菌和群体感应抑制衍生物的良好骨架的有用性，尽管它对植物提取物的抗菌活性贡献不大。
