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Novel essential amino acid-sulfanilamide hybrid as safe anti-ulcerogenic agent with anti-helicobacter pylori activity

Awaad AS 1 , Alafeefy AM 2 , Alasmary FAS 3 , El-Meligy RM 4 , Zain ME 5 , Alqasoumi SI 6

Affiliations 

  • 1 Pharmacognosy Department, College of Pharmacy, Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia
  • 2 Department of Chemistry, Kulliyyah of Science, International Islamic University, Malaysia
  • 3 Chemistry Department, College of Science, King Saud University, Riyadh 11362, Saudi Arabia
  • 4 Aromatic and Medicinal Plants Department, Desert Research Center, Cairo, Egypt
  • 5 Botany and Microbiology Department, Faculty of Science, Al-Azhar University, Cairo, Egypt
  • 6 Department of Pharmacognosy, College of Pharmacy, King Saud University, Saudi Arabia
Saudi Pharm J, 2017 Nov;25(7):967-971.
PMID: 29158702 DOI: 10.1016/j.jsps.2017.02.012

Abstract

A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and in vitro anti-Helicobacter pylori 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-Helicobacter pylori activity in vitro 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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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