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Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity

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

Affiliations 

  • 1 Chemistry Department, College of Science, King Saud University, Riyadh 11362, Saudi Arabia
  • 2 Pharmacognosy Department, College of Pharmacy, Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia
  • 3 Department of Chemistry, Kulliyyah of Science, International Islamic University Malaysia, Malaysia
  • 4 Aromatic and Medicinal Plants Department, Desert Research Center, Cairo, Egypt
  • 5 Department of Pharmacognosy, College of Pharmacy, King Saud University, KSA
Saudi Pharm J, 2018 Jan;26(1):138-143.
PMID: 29379346 DOI: 10.1016/j.jsps.2017.09.011

Abstract

Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl-3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4-aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & Anti-Ulcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P 

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

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