Access to 8-Aminoindolizine Fused with Quinone via Cu(OAc)2-Catalyzed Domino [4+2] Annulation

Synthesis, Год журнала: 2024, Номер 56(11), С. 1799 - 1806

Опубликована: Фев. 1, 2024

Abstract Cu(OAc)2-catalyzed [4+2] annulation of N-substituted pyrrole-2-carbonitriles with quinones allowed access to a wide range 8-aminoindolizines fused through domino process involving sequence intermolecular Michael addition, Thorpe–Ziegler type cyclization, and aromatization. Biological evaluation the resulting quinone-8-aminoindolizine hybrids revealed significant anticancer effects these compounds in human hepatocellular cells (HepG2) prostate adenocarcinoma (PC-3).

Язык: Английский

---

Synthesis and Potential Dual Inhibitory Activity Against Acetylcholinesterase and Butyrylcholinesterase of Galactose‐Conjugated Isatin β‐Thiosemicarbazones

ChemistrySelect, Год журнала: 2023, Номер 8(22)

Опубликована: Июнь 6, 2023

Abstract A series of different isatin‐thiosemicarbazones 4 a – t derived from corresponding substituted isatins and N ‐(2,3,4,6‐tetra‐ O ‐acetyl‐β‐ d ‐galactopyranosyl)thiosemicarbazide had been synthesized. Their anti‐Alzheimer activity were studied through the inhibitions acetylcholinesterase (AChE) butyrylcholinesterase (BChE). Most these compounds exhibited inhibitory activities against enzymes. Of isatin ‐(2,3,4,6‐tetra‐O‐acetyl‐β‐ ‐galactoranosyl)thiosemicarbazones , in IC 50 range below 0.05 μM, some thiosemicarbazones potent AChE enzyme, including s (1‐benzyl)> (1‐phenthyl)> p (1‐allyl)> r (1‐ ‐butyl), others BChE, o (1‐propyl)> q (1‐butyl)> (1‐benzyl). Enzymic kinetics BChE inhibition studied. These with strong further investigated induced fit docking studies as well molecular dynamics simulations. The obtained resulting simulations indicate that ligand‐residues interactions decisive factors to enzymes, respectively.

Язык: Английский

---

Prediction by DFT and Synthesis of new Xanthene Derivatives: Evaluation of their Toxicity and Antihyperlipidemic Properties In-Vivo and In-Silico

Journal of Molecular Structure, Год журнала: 2024, Номер 1313, С. 138705 - 138705

Опубликована: Май 21, 2024

Язык: Английский

---

Design, Creation, and Biological Screening of Newer Coumarin-Coupled Heterocyclic Hybrids as Acetylcholinesterase Inhibitors that may be Useful in the Treatment of Alzheimer’s Disease

Pharmaceutical Chemistry Journal, Год журнала: 2024, Номер 58(7), С. 1069 - 1083

Опубликована: Окт. 1, 2024

Язык: Английский

---