Salicyl-AApicolamide Foldameric Peptides Exhibit Quorum Sensing Inhibition of (PA14).

An organic acid, salicylic acid, and its derivatives are constituents of various natural products possessing remarkable bioactivity. -Acetyl salicylate (aspirin) is a well-known life-saving drug. Its peptide derivative salicylamide has also been explored in the designing of peptide-based therapeutic drugs.

A new transient directing group diethoxyethyl-L-proline facilitates -arylation of aryl-amines/-amino acids Pd-catalyzed C(sp)-H activation.

Mono--arylated arylamines are constituents of various natural products but their syntheses are challenging. This report describes a new synthetic methodology for the -arylation of arylamines and α-aromatic amino acids (phenylglycine and phenylalanine) through a Pd-catalyzed C(sp)-H activation using the synthetic transient directing group diethoxyethyl-L-proline (DEP). A catalytic amount of diethoxyethyl-L-proline is sufficient to form mono-arylated arylamines as the major products using aryliodides.

Synthesis of Aminotroponyl-/Difluoroboronyl Aminotroponyl Deoxyuridine Phosphoramidites.

This report describes the chemical synthesis of aminotroponyl-conjugated deoxyuridine analog (at-dU) and its difluoroboron complex (dfbat-dU) and their phosphoramidites by using the versatile phosphorylating reagent 2-Cyanoethyl N,N-diisopropylchlorophosphoramidite. Tropolone is a non-benzenoid aromatic bioactive natural fluorescent molecule, possessing intramolecular charge transfer and metal chelating properties with transition metal ions such as Cu Zn Ni . Its synthetic derivatives, 2-aminotropones also exhibit unique bioactivities and are considered potential therapeutic drug candidate.

Fluorescent DNA analog: 2-aminotroponyl-pyrrolyl-2'-deoxyuridinyl DNA oligo enhance fluorescence in DNA-duplex as compared to 2-aminotroponyl-ethynyl-2'-deoxyuridinyl DNA oligo.

The nucleobase modified fluorescent DNA and RNA analogs are synthesized by the conjugation of aromatic scaffolds through linkers, comprising mostly ethyne/ethene or fused ring residues at the pyrimidine/purine ring. These scaffolds are mainly derived from the benzenoid aromatic molecules comprising electron withdrawing/donating characters. However, non-benzenoid aromatic scaffolds such as tropolone and related derivatives are constituents of various troponoid natural products.