Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights

Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights

Aim: Synthesis of novel bis-Schiff bases having potent inhibitory activity against phosphodiesterase (PDE-1 and -3) enzymes, potentially offering therapeutic implications for various conditions. Methods:Bis-Schiff bases were synthesized by refluxing 2,4-dihydroxyacetophenone with hydrazine hydrate,...

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Published in:Future Medicinal Chemistry
Main Author: Alam A.; Gul S.; Zainab; Khan M.; Elhenawy A.A.; Islam M.S.; Ali M.; Ali Shah S.A.; Latif A.; Ahmad M.
Format: Article
Language:English
Published: Taylor and Francis Ltd. 2024
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85193757947&doi=10.1080%2f17568919.2024.2342707&partnerID=40&md5=a0ba825c3df785e48af67556df92ecde
id 2-s2.0-85193757947
spelling 2-s2.0-85193757947
Alam A.; Gul S.; Zainab; Khan M.; Elhenawy A.A.; Islam M.S.; Ali M.; Ali Shah S.A.; Latif A.; Ahmad M.
Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
2024
Future Medicinal Chemistry
16
12
10.1080/17568919.2024.2342707
https://www.scopus.com/inward/record.uri?eid=2-s2.0-85193757947&doi=10.1080%2f17568919.2024.2342707&partnerID=40&md5=a0ba825c3df785e48af67556df92ecde
Aim: Synthesis of novel bis-Schiff bases having potent inhibitory activity against phosphodiesterase (PDE-1 and -3) enzymes, potentially offering therapeutic implications for various conditions. Methods:Bis-Schiff bases were synthesized by refluxing 2,4-dihydroxyacetophenone with hydrazine hydrate, followed by treatment of substituted aldehydes with the resulting hydrazone to obtain the product compounds. After structural confirmation, the compounds were screened for their in vitro PDE-1 and -3 inhibitory activities. Results: The prepared compounds exhibited noteworthy inhibitory efficacy against PDE-1 and -3 enzymes by comparing with suramin standard. To clarify the binding interactions between the drugs, PDE-1 and -3 active sites, molecular docking studies were carried out. Conclusion: The potent compounds discovered in this study may be good candidates for drug development. © 2024 Informa UK Limited, trading as Taylor & Francis Group.
Taylor and Francis Ltd.
17568919
English
Article
author Alam A.; Gul S.; Zainab; Khan M.; Elhenawy A.A.; Islam M.S.; Ali M.; Ali Shah S.A.; Latif A.; Ahmad M.
spellingShingle Alam A.; Gul S.; Zainab; Khan M.; Elhenawy A.A.; Islam M.S.; Ali M.; Ali Shah S.A.; Latif A.; Ahmad M.
Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
author_facet Alam A.; Gul S.; Zainab; Khan M.; Elhenawy A.A.; Islam M.S.; Ali M.; Ali Shah S.A.; Latif A.; Ahmad M.
author_sort Alam A.; Gul S.; Zainab; Khan M.; Elhenawy A.A.; Islam M.S.; Ali M.; Ali Shah S.A.; Latif A.; Ahmad M.
title Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
title_short Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
title_full Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
title_fullStr Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
title_full_unstemmed Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
title_sort Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights
publishDate 2024
container_title Future Medicinal Chemistry
container_volume 16
container_issue 12
doi_str_mv 10.1080/17568919.2024.2342707
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-85193757947&doi=10.1080%2f17568919.2024.2342707&partnerID=40&md5=a0ba825c3df785e48af67556df92ecde
description Aim: Synthesis of novel bis-Schiff bases having potent inhibitory activity against phosphodiesterase (PDE-1 and -3) enzymes, potentially offering therapeutic implications for various conditions. Methods:Bis-Schiff bases were synthesized by refluxing 2,4-dihydroxyacetophenone with hydrazine hydrate, followed by treatment of substituted aldehydes with the resulting hydrazone to obtain the product compounds. After structural confirmation, the compounds were screened for their in vitro PDE-1 and -3 inhibitory activities. Results: The prepared compounds exhibited noteworthy inhibitory efficacy against PDE-1 and -3 enzymes by comparing with suramin standard. To clarify the binding interactions between the drugs, PDE-1 and -3 active sites, molecular docking studies were carried out. Conclusion: The potent compounds discovered in this study may be good candidates for drug development. © 2024 Informa UK Limited, trading as Taylor & Francis Group.
publisher Taylor and Francis Ltd.
issn 17568919
language English
format Article
accesstype
record_format scopus
collection Scopus
_version_ 1814778502928400384

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