Synthesis of Isoindoline-1,3-Dione Derivatives as Cyclooxygenase (Cox) S Inhibitors

Inflammation is the vital part of the immune system's response to injury and infection. It is the body's way of signaling the immune system to heal and repair damaged tissue. The objective of this paper is to design and synthesize a new isoindoline 1,3-dinoe derivative and investigate their selective anti inflammatory activity to COXs. As a potential anti-inflammatory compound, Isoindoline-1,3-dione derivatives were synthesized from the addition reaction of phthalimide, formaldehyde, catalytic amount of potassium hydroxide and cyclic amine in ethanol yielded the desired Isoindoline-1,3-dione compounds (ZJ1-ZJ6. 1H-NMR, ¹³C-NMR, FT-IR and elemental analysis were consistent with the assigned structures. Isoindoline-1,3-dione derivatives exhibited good inhibitory activity against the COX enzymes. To explain the result of our investigation to COX-1 and COX-2 and the selectivity of our compounds to either COX-1 or COX-2, the rationalization in COX-1, the amino group participate more effectively in binding with the ligand while in COX-2, the aryl group is more effective in binding to the ligand. The amino acetylenic compounds behave differently toward COXs from our compound. ZJ4 have shown some selective COX-1 ligand efficiency while ZJ1 promised a potent blockage and ligand efficiency toward the COX-2 enzyme which was found to be higher than the marketed drug Indomethacin and near potency score of Celecoxib. For the first time, this indicates the requirement of investigating the removal of acetylenic group in this study showed that it might be a different binding site in COXs which may result in effective compounds.

Light-driven carbon dioxide reduction coupled with conversion of acetylenic group to ketone by a functional Janus catalyst based on keplerate {Mo132}

A novel dual functional Janus catalyst {Mo132} for photocatalytic carbon dioxide reduction coupled with organic hydroxylation from phenylacetylene to acetophenone is reported.

Synthesis and Biological Activity of New 1,2,3-Triazole Acyclonucleosides Analogues of ACV

The synthesis of new 4,5-substituted 1-[(2-hydroxyethoxy)methyl]-1,2,3-triazole 3a–e is described. The key step is the 1,3-dipolar cycloaddition between the azido group and an acetylenic group. Biological evaluation show significant activity.

Palladium-catalysed Heteroannulation with Acetylenic Carbinols: Synthesis of 3-Acylmethylisoindolin-1-ones

Palladium-catalysed reactions of 2-iodobenzamides 1–6 with acetylenic carbinols 7–12 having a terminal acetylenic group and an adjacent carbinol functionality result in the formation of the 3-acylmethylisoindolin-1-ones 13–23 in one step.

The synthesis of cofacial porphyrin dimers

A cofacial dimeric porphyrin joined by two hydrocarbon chains has been prepared using a bis-porphyrin already linked by a single hydrocarbon chain. When each porphyrin bears an acetylenic group, copper catalyzed coupling followed by catalytic hydrogenation gives a doubly linked cofacial porphyrin. However, a far superior and more flexible route, involving the use of a dimeric biladiene-ac, gives in one step the same cofacial porphyrin. This latter route has been used to prepare dimeric porphyrins with hydrocarbon linkages of varying lengths.

Macrocyclic enol-ethers containing an acetylenic group from the red alga Phacelocarpus labillardieri

Four new acetate-derived metabolites have been isolated from two collections of the red alga Phacelocarpus labillardieri. Three of these metabolites were 2,6-disubstituted pyran-4-ones containing a macrocyclic enol-ether ring. The fourth compound was a 6-substituted pyran-2-one derivative.