title: Synthesis and Biological Evaluation of New N-(4-Substituted phenyl)glycine Derivatives as Potential Anti-inflammatory Agents.
abstract: Designing new anti-inflammatory agents possessing safe therapeutic
  profiles and devoid of potential undesirable side effects is an active field in medicinal chemistry.
  Thus, a series of N-(4-substituted phenyl)glycine derivatives was designed and synthesized.
  The idea behind the design is to utilize the bifunctionality of 4-aminoacetophenone via
  converting the amino group into glycine derivative as a side arm to mimic the glycine amino
  acid enhancing the overall physicochemical and biological characteristics. In addition, the
  opposite acetyl group was used as a center for modification and derivatization.
  
  
  
  The starting N-(4-acetylphenyl)glycine was converted into two intermediates: the
  chalcone analog 2 and the thiosemicarbazone derivative 8. Both 2 and 8 were derivatized
  and/or cyclized into different heterocyclic target derivatives (3-7 and 9-12). The target compounds
  were screened for anti-inflammatory activity using carrageenan-induced rat paw
  edema assay.
  
  
  
  The results showed that compounds 6, 7, and 3, were the most active among the
  tested compounds at 50 mg/kg dose level with % inhibition of edema of 51.82, 43.80, and
  40.39, respectively.
  
  
  
  The authors succeeded to introduce a simple and versatile skeleton with a side
  arm resembling the glycine amino acid; imparting a potential improvement in physicochemical
  properties. We utilize the other side of the skeleton’s aromatic ring as a center for derivatization.
  The chalcone analog and its cyclized heterocyclic derivatives were of remarkably
  higher anti-inflammatory activity than the thiosemicarbazone and its derivatives.
authors.affiliation: Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University,
  Mansoura 35516, Egypt
authors.forename: Waleed A
authors.initials: WA
authors.lastname: Bayoumi
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
authors.forename: Mariam A
authors.initials: MA
authors.lastname: Ghaly
authors.affiliation: Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
authors.forename: Mohamed E
authors.initials: ME
authors.lastname: Shaker
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002351:Carrageenan; D004008:Diclofenac / Q000494:pharmacology; D004195:Disease Models, Animal; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control*; D005998:Glycine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D008297:Male; D015394:Molecular Structure; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D000893:Anti-Inflammatory Agents; D004008:Diclofenac; D002351:Carrageenan; D005998:Glycine