CONFORMAL RESTRICTION MEASURES ON LOOPS SURROUNDING AN INTERIOR POINT

A conformal restriction measure is a probability measure which is used to describe the law of a random connected subset in a simply connected domain that satisfies a certain conformal restriction property. Usually there are three kinds of conformal restriction measures: one (called the chordal restriction measure) has two given boundary points of the random set, the second (called the radial restriction measure) has one boundary point and one interior point in the random set, and the third (called the tri-chordal restriction measure) has three boundary points in the random set. In this article, we will define a new probability measure such that the random set associated to it contains one given interior point and does not intersect with the boundary. Furthermore, we will show that this measure can be characterized by one parameter;we will also construct this one-parameter family of measures in two ways and obtain several properties.

Coumarin Based Neutral Sensor for Biologically Important Anions

A coumarin Shiff-base derivative, salicylaldehyde-N-（6-phenylazo-coumarin-3-formyl）-hydrazone（1）, was obtained by simple organic synthesis from cheap and commercially available starting materials. Sensor 1 exhibits a very weak fluorescence emission, however, in the presence of acetate ions ＂turn-on＂ fluorescence is observed, which results from binding-induced conformational restriction of the fluorophore. Importantly, sensor 1 can also be used as colorimetric chemosensor for the anions with strong basicity, which is easily observed from yellow to red by naked eyes. Consequently, compound 1 can behave as a colorimetric and fluorescence sensor for biologically important F-, CH3COO- and H2PO4- in the presence of the other anions tested such as Cl-, Br- and I- in dimethyl sulfoxide（DMSO）.

Intelligent design and construction of novel APN-based theranostic probe driven by advanced computational methods

Multifunctional molecules with both optical signal and pharmacological activity play an important role in drug development,disease diagnosis,and basic theoretical research.Aminopeptidase N(APN),as a representative tumor biomarker with anti-tumor potential,still lacks a high-precision theranostic probe specifically targeting it.In this study,a novel quaternity design strategy for APN theranostic probe was developed.This proposed strategy utilizes advanced machine learning and molecular dynamics simulations,and cleverly employs the strategy of conformation-induced fluorescence recovery to achieve multi-objective optimization and integration of functional fragments.Through this strategy,a unique“Off-On”theranostic probe,ABTP-DPTB,was ingeniously constructed to light up APN through fluorescence restoration,relying on conformation-induced effects and solvent restriction.Differ from the common diagnostic probes,the intelligent design with non-substrated linkage makes ABTP-DPTB for long-term in-situ imaging.The fabricated probe was used for detecting and inhibiting APN in various environments,with a better in vitro inhibitory than golden-standard drug bestatin.

Enantiospecific Synthesis of All Four Stereoisomers of Novel Bicyclic Arylacetamides as κ-Opioid Agonists

Conformationally constrained bicyclic derivatives of the potent and selective κ-opioid receptor agonist 2-(3,4-dichlorophenyl)-N-methyl-N- [(1S)-1-phenyl-2- (1-pyrrolidinyl)-ethyl] acetam^ide (3, ICI-199, 441) were designed to explore the effect of the conformational restriction and stereochemistry of the pharmacophoric ethylenediamine incorporated into the pyrrolidine on the affinity and κ-selectivity. A facile enantiospecific synthetic route was established to afford all four stereoisomers starting from readily available amino acids through mild cyclization and amide formation.