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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

[Image: see text] 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 diff...

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Autores principales: Anwar, Fareeha, Saleem, Uzma, Rehman, Atta ur, Ahmad, Bashir, Ismail, Tariq, Mirza, Muhammad Usman, Kee, Lee Yean, Abdullah, Iskandar, Ahmad, Sarfraz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8153932/
https://www.ncbi.nlm.nih.gov/pubmed/34056243
http://dx.doi.org/10.1021/acsomega.1c00654
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author Anwar, Fareeha
Saleem, Uzma
Rehman, Atta ur
Ahmad, Bashir
Ismail, Tariq
Mirza, Muhammad Usman
Kee, Lee Yean
Abdullah, Iskandar
Ahmad, Sarfraz
author_facet Anwar, Fareeha
Saleem, Uzma
Rehman, Atta ur
Ahmad, Bashir
Ismail, Tariq
Mirza, Muhammad Usman
Kee, Lee Yean
Abdullah, Iskandar
Ahmad, Sarfraz
author_sort Anwar, Fareeha
collection PubMed
description [Image: see text] 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.
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spelling pubmed-81539322021-05-27 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 ACS Omega [Image: see text] 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. American Chemical Society 2021-04-16 /pmc/articles/PMC8153932/ /pubmed/34056243 http://dx.doi.org/10.1021/acsomega.1c00654 Text en © 2021 The Authors. Published by American Chemical Society Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Anwar, Fareeha
Saleem, Uzma
Rehman, Atta ur
Ahmad, Bashir
Ismail, Tariq
Mirza, Muhammad Usman
Kee, Lee Yean
Abdullah, Iskandar
Ahmad, Sarfraz
Toxicological Screening of 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one: A New Potential Candidate for Alzheimer’s Treatment
title Toxicological Screening of 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one: A New Potential Candidate for Alzheimer’s Treatment
title_full Toxicological Screening of 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one: A New Potential Candidate for Alzheimer’s Treatment
title_fullStr Toxicological Screening of 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one: A New Potential Candidate for Alzheimer’s Treatment
title_full_unstemmed Toxicological Screening of 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one: A New Potential Candidate for Alzheimer’s Treatment
title_short Toxicological Screening of 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one: A New Potential Candidate for Alzheimer’s Treatment
title_sort toxicological screening of 4-phenyl-3,4-dihydrobenzo[h]quinolin-2(1h)-one: a new potential candidate for alzheimer’s treatment
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8153932/
https://www.ncbi.nlm.nih.gov/pubmed/34056243
http://dx.doi.org/10.1021/acsomega.1c00654
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