Skip to content
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
pharmacology, toxicology and pharmaceutics
Isoxazole analogues of dibenzazepine as possible leads against ulcers and skin disease: In vitro and in silico exploration
Saudi Pharmaceutical Journal, Volume 31, No. 12, Article 101877, Year 2023
Notification
URL copied to clipboard!
Description
Utilizing multi-target drugs shows great promise as an effective strategy against polygenic diseases characterized by intricate patho-mechanisms, such as ulcers, skin dermatitis, and cancers. The current research centers around the creation of hybrid compounds, connecting dibenzazepine and isoxazole, with the aim of exploring their potential as inhibitors for urease and tyrosinase enzymes. Analogs 6a, 6b, 6d, 6 h-6j, and 6 l demonstrated strong inhibitory potential against tyrosinase enzyme with IC50 values of 4.32 ± 0.31–12.36 ± 0.48. Whereas analogs 6a, 6c, 6e, 6f, 6h-6m, and 6r exhibited potent inhibitory activities against urease enzyme with IC50 values of 3.67 ± 0.91–15.60 ± 0.18 μM. Furthermore, compounds 6i, 6n, and 6r showed weak toxic effect in BJ-cell line, whereas the remaining compounds were found non-toxic to normal cell line. The mechanistic studies of potent inhibitors of both the enzymes showed competitive mode of inhibition. Molecular docking was employed to establish the relationship between structure and activity and to elucidate the interaction mechanism. This analysis revealed that the active analogs exhibited crucial interactions with the active site residues of urease and tyrosinase, thus corroborating our experimental results. Hence, the generated derivatives of dibenzazepine-linked isoxazoles present intriguing starting points for further investigations into their potential as inhibitors of urease and tyrosinase, with the potential for future modification and enhancement. © 2023 The Authors
Authors & Co-Authors
Khan, Majid Riaz
Pakistan, Chakdara
University of Malakand
Oman, Nizwa
University of Nizwa
Halim, Sobia Ahsan
Oman, Nizwa
University of Nizwa
Shah, Luqman Ali
Pakistan, Mansehra
Hazara University Pakistan
Khan, Ajmal
Oman, Nizwa
University of Nizwa
Ahmed, Izzaddinn Elawad
Saudi Arabia, Tabuk
University of Tabuk
Abdalla, Ashraf N.
Saudi Arabia, Makkah
Umm Al-qura University
Jan, Afnan M.
Saudi Arabia, Makkah
Umm Al-qura University
Khalid, Asaad
Saudi Arabia, Jazan
Jazan University
Al-Harrasi, Ahmed Sulaiman
Saudi Arabia, Tabuk
University of Tabuk
Statistics
Authors: 9
Affiliations: 7
Identifiers
Doi:
10.1016/j.jsps.2023.101877
ISSN:
13190164
Research Areas
Environmental