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Toxicological Screening of 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one: A New Potential Candidate for Alzheimer's Treatment.
Anwar, Fareeha; Saleem, Uzma; Rehman, Atta Ur; Ahmad, Bashir; Ismail, Tariq; Mirza, Muhammad Usman; Kee, Lee Yean; Abdullah, Iskandar; Ahmad, Sarfraz.
Affiliation
  • Anwar F; Riphah Institute of Pharmaceutical Sciences, Riphah International University, Lahore 54000 Pakistan.
  • Saleem U; Riphah Institute of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences, Riphah International University, Islamabad 44000, Pakistan.
  • Rehman AU; Department of Pharmacology, Faculty of Pharmaceutical Sciences, Govt. College University, Faisalabad 38040, Pakistan.
  • Ahmad B; Department of Pharmacy, Forman Christian College, Lahore 54600, Pakistan.
  • Ismail T; Riphah Institute of Pharmaceutical Sciences, Riphah International University, Lahore 54000 Pakistan.
  • Mirza MU; Riphah Institute of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences, Riphah International University, Islamabad 44000, Pakistan.
  • Kee LY; Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad Campus, Abottabad 22060, Pakistan.
  • Abdullah I; Department of Pharmaceutical and Pharmacological Sciences, Rega Institute for Medical Research, Medicinal Chemistry, University of Leuven, Leuven B-3000, Belgium.
  • Ahmad S; Department of Chemistry and Biochemistry, University of Windsor, Windsor, Ontario N9B 3P4, Canada.
ACS Omega ; 6(16): 10897-10909, 2021 Apr 27.
Article in En | MEDLINE | ID: mdl-34056243
Toxicity studies are necessary for the development of a new drug. Naphthalene is a bicyclic molecule and is easy to derivatize. In our previous study, a derivative of naphthalene (4-phenyl,3,4-dihydrobenzoquinoline-2(H)one) was synthesized and reported its in vitro activity on different enzymes. This study was a probe to investigate the toxicity potential of that compound (SF3). Acute oral (425), subacute (407), and teratogenicity (414) studies were planned according to their respective guidelines given by organization of economic cooperation and development (OECD). Acute oral, subacute, and teratogenicity studies were carried out on 2000, 5-40, and 40 mg/kg doses. Blood samples were collected for hematological and biochemical analyses. Vital organs were excised for oxidative stress (superoxide dismutase, catalase, glutathione, and malondialdehyde) and histopathological analysis. LD 50 of SF3 was higher than 2000 mg/kg. In acute and subacute studies, levels of alkaline phosphates and aspartate transaminase were increased. Teratogenicity showed no resorptions, no skeletal or soft tissue abnormalities, and no cleft pallet. Oxidative stress biomarkers were close to the normal, and no increase in the malondialdehyde level was seen. Histopathological studies revealed normal tissue architecture of the selected organs, except kidney, in acute oral and subacute toxicity studies at 40 mg/kg. The study concluded that SF3 is safer if used as a drug.

Full text: 1 Collection: 01-internacional Database: MEDLINE Type of study: Diagnostic_studies / Screening_studies Language: En Journal: ACS Omega Year: 2021 Document type: Article Country of publication: United States

Full text: 1 Collection: 01-internacional Database: MEDLINE Type of study: Diagnostic_studies / Screening_studies Language: En Journal: ACS Omega Year: 2021 Document type: Article Country of publication: United States