Synthesis of intramolecular cross-coupling analogues of forskolin

Article Chemistry, Organic

Stereoselective Palladium-Catalyzed Arylation of Exo-Glycals with Aryl Iodides

Jeffery Regier et al.

Summary: A novel methodology for the arylation of exo-glycals has been developed, allowing for the formation of Z-isomers in a stereoselective manner. The transformation demonstrated excellent functional group tolerance.

JOURNAL OF ORGANIC CHEMISTRY (2022)

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Article Chemistry, Medicinal

Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin- resistant Staphylococcus aureus

Mohamed M. Elsebaie et al.

Summary: A series of diphenylurea derivatives with aminoguanidine moiety were synthesized and their antibacterial activity was evaluated. Two compounds showed better bacteriological profiles and prolonged post-antibiotic effect. Additionally, these compounds were able to resensitize vancomycin-resistant strains and exhibited comparable efficacy to a commercially available drug in a mouse model. Therefore, the diphenylurea scaffold has potential as an anti-staphylococcal treatment option.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Review Biochemistry & Molecular Biology

Recent ring distortion reactions for diversifying complex natural products

Yu Li et al.

Summary: Chemical diversification of natural products is an efficient approach for generating natural product-like compounds for modern drug discovery. Ring distortion reactions can alter the core ring structures of natural products, resulting in the production of structurally complex and diverse compounds suitable for various biological and medicinal applications. Despite the challenges and limitations, there are opportunities for future improvements in this rapidly expanding field.

NATURAL PRODUCT REPORTS (2022)

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Article Chemistry, Organic

Forskolin Editing via Radical Iodo- and Hydroalkylation

Elena Pruteanu et al.

Summary: The modification of highly oxygenated forskolin and two less functionalized model substrates was investigated via intermolecular carbon-centered radical addition, leading to highly regio- and reasonably stereoselective iodine atom transfer radical addition reactions. Unexpected cyclic ether derivative was obtained from unprotected forskolin, while in situ protection of the 1,3-diol moiety as a cyclic boronic ester occurred during the iodine ATRA process by changing the mode of radical process initiation. This mild radical-mediated in situ protection of 1,3-diol may have broad applications in radical and non-radical transformations.

SYNTHESIS-STUTTGART (2021)

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Article Chemistry, Organic

Synthesis of non-toxic anticancer active forskolin-indole-triazole conjugates along with their in silico succinate dehydrogenase inhibition studies

Devendar Ponnam et al.

Summary: A novel series of hybrid molecules combining forskolin, indole, and 1,2,3-triazoles were synthesized and evaluated for potential anticancer activity. Compound 5g showed the highest potency across various cell lines. In silico studies indicated that the synthesized compounds exhibited stronger binding affinity compared to forskolin.

JOURNAL OF HETEROCYCLIC CHEMISTRY (2021)

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Article Chemistry, Multidisciplinary