Khan Khalid Mohammed, Khan Muhammad Zarrar, Taha Muhammad, Maharvi Ghulam Murtaza, Saify Zafar Saeed, Parveen Shahnaz, Choudhary Muhammad Iqbal
HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
Nat Prod Res. 2009;23(5):479-84. doi: 10.1080/14786410802090359.
A series of N-substituted morpholines 2-20 was synthesised by reacting various acid chlorides and alkyl halides with morpholine (1). All of the synthesised compounds 2-20 were screened for their leishmanicidal effects using amphotericin B (IC(50) = 0.24 microg L(-1)) and pentamidine (IC(50) = 2.56 microg mL(-1)) as standards and a structure-activity relationship (SAR) study was established. The compounds 2 (IC(50) = 48 microg mL(-1)), 3 (IC(50) = 30.0 microg mL(-1)), 10 (IC(50) = 41.0 microg mL(-1)), 15 (IC(50) = 33.0 microg mL(-1)), 16 (IC(50) = 35.0 microg mL(-1)) and 20 (IC(50) = 47.0 microg mL(-1)) showed weak leishmanicidal activities.
通过使各种酰氯和卤代烷与吗啉（1）反应，合成了一系列N-取代吗啉2 - 20。以两性霉素B（IC50 = 0.24μg L-1）和喷他脒（IC50 = 2.56μg mL-1）作为标准，对所有合成的化合物2 - 20进行了杀利什曼原虫效果筛选，并建立了构效关系（SAR）研究。化合物2（IC50 = 48μg mL-1）、3（IC50 = 30.0μg mL-1）、10（IC50 = 41.0μg mL-1）、15（IC50 = 33.0μg mL-1）、16（IC50 = 35.0μg mL-1）和20（IC50 = 47.0μg mL-1）显示出较弱的杀利什曼原虫活性。
