Awaad Amani S, Alafeefy Ahmed M, Alasmary Fatmah A S, El-Meligy Reham M, Zain M E, Alqasoumi Saleh I
Pharmacognosy Department, College of Pharmacy, Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
Department of Chemistry, Kulliyyah of Science, International Islamic University, Malaysia.
Saudi Pharm J. 2017 Nov;25(7):967-971. doi: 10.1016/j.jsps.2017.02.012. Epub 2017 Feb 27.
A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and anti- activity. The new molecule showed a dose dependent activity against absolute ethanol-induced ulcer in rats, it produced percent protection of control ulcer by 66.7 at dose 100 mg/kg. In addition it showed a potent anti- activity against 7 clinically isolated strains. The minimum inhibitory concentration (MIC) ranged from 12.5 to 50 μg/ml. The preliminary safety studies and toxicity profile are optimistic and encouraging.
合成了一种新型且安全的含磺胺的必需氨基酸（亮氨酸），并对其抗溃疡活性和抗菌活性进行了评估。新分子对大鼠绝对乙醇诱导的溃疡呈现剂量依赖性活性，在100mg/kg剂量时对对照溃疡的保护率达66.7%。此外，它对7株临床分离菌株显示出强效抗菌活性。最低抑菌浓度（MIC）范围为12.5至50μg/ml。初步安全性研究和毒性概况令人乐观且鼓舞人心。
