Probing novel azole-sulfonamide urea/thiourea conjugates as multitarget inhibitors of AChE and hCAs (I and II): synthesis, in vitro, and in silico studies.
Overall, the experimental and computational findings identify azole-sulfonamide urea/thiourea conjugates as promising scaffolds for the further development of multitarget enzyme inhibitors and provide preliminary structure-activity insights for subsequent optimization.
Together with their dual cholinesterase inhibitory activities, compounds 6a and 6c represent promising multifunctional in vitro lead candidates for further development against neurodegenerative disorders associated with neurodegenerative disorders associated with neuroinflammation and oxidative stress.
A. Hussain, Rafaqat Hussain, Hina Sarfraz et al.· Journal of Computer-Aided Mo...· 0 citations
A novel series of seventeen carbazole–acrylamide–pyridinium-N-phenylacetamide hybrids (12a–q) was designed and synthesized as dual inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) for potential Alzheimer's disease therapy. Their inhibitory activity was evaluated against both enzymes using tacr...
A. Taherkhani, Halil Şenol, Y. Valizadeh et al.· RSC Medicinal Chemistry· 0 citations
AIM
To synthesize novel sulfonohydrazide derivatives and evaluate their physicochemical and enzyme‑inhibitory profiles, together with the corresponding structure-activity relationships.
METHODS
A series of six hydrazide derivatives (NLs1-NLs6) was synthesized and subjected to comprehensive in vitro enzymatic evaluati...
Lubabah Abdul Karim, Amara Mumtaz, S. Ejaz et al.· Future Medicinal Chemistry· 0 citations
Promising compounds like SBB-2, SBB-3, SBB-5, SBB-6, and SBB-7 exhibit favourable physicochemical properties, high drug-likeness, solubility, and a non-toxic profile, making them strong candidates for further development of a promising drug.
D. Upadhyay, Drashti Thanki, C. Somaiya· Current Organic Synthesis· 0 citations
Epilepsy remains a challenging neurological disorder, with a significant proportion of patients exhibiting resistance to current antiseizure medications. Herein, we report the rational design, synthesis, and biological evaluation of a new series of isatin-thiazolidine-2,4-dione hybrids bearing a pendant benzenesulfonam...
Wagdy M. Eldehna, M. A. Alkabbani, Andrea Ammara et al.· European journal of medicina...· 0 citations
The design and synthesis of ten disubstituted tetrazole derivatives (5a–5j) via a one-pot, four-component Ugi-azide reaction (UGI-4CR) employing 2-(4-chloro-2-formylphenoxy)acetonitrile, variously substituted primary aromatic amines, trimethylsilyl azide, and tert-butyl isocyanide in anhydrous methanol at ambient tempe...
R. Gohil, Anjalee R. Khoyanee, Hetal Ramani et al.· Discover Chemistry· 0 citations
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