Biothiols are important species in physiological processes such as regulating protein structures, redox homeostasis and cell signalling Alternation in the biothiol levels is associated with various pathological processes, therefore non-invasive fluorescent probes with high specificity to biothiols are highly desirable research utilities Meanwhile, fluorescent probes with aggregation-induced emission properties (AIEgens) possess unique photophysical properties that allow modulation of the sensing process through controlling the aggregation-disaggregation or the intramolecular rotational motions of the fluorophores Herein we review the recent progress in the development of biothiol-specific AIEgens In particular, the molecular design principles to target different types of biothiols and the corresponding sensing mechanisms are discussed, along with the potential of the future design and development of multi-functional bioprobes

Biothiol-specific fluorescent probes with aggregation-induced emission characteristics

Heterocyclic compounds play a significant role in various biological processes of the human body and many of them are in clinical use due to their diverse, chemical and biological properties. Among these, indole is one of the most promising pharmacologically active molecules. Due to its chemical reactivity, indole has been willingly modified to obtain a variety of new lead molecules, which has been successfully utilized to obtained novel drug candidates for the treatment of different pharmacological diseases. Indole-based compounds such as vincristine (anticancer), reserpine (antihypertensive), amedalin (antidepressant) and many more describe the medicinal and pharmacological importance of the indole in uplifting human life. In this review, we compiled various reports on indole derivatives and their biological significance, including antifungal, antiprotozoal, antiplatelet, anti- Alzheimer's, anti-Parkinson's, antioxidant and anticancer potential from 2015 onwards. In addition, structure-activity relationship studies of the different derivatives have been included. We have also discussed novel synthetic strategies developed during this period for the synthesis of different indole derivatives. We believe that this review article will provide comprehensive knowledge about the medicinal importance of indoles and will help in the design and synthesis of novel indole-based molecules with high potency and efficacy.

Medicinal Perspective of Indole Derivatives: Recent Developments and Structure-Activity Relationship Studies.

A novel "turn-on" mitochondria-targeting near-infrared fluorescent probe for H2S detection and in living cells imaging.

The research of endogenous hydrogen sulfide (H2S) biology function, pathological and pharmacological effects has been active in the field of chemists and biologists in recent years. Especially, consequent H2S detection mechanisms and biological applications based on fluorescence probe emerged in endlessly, competing ideas, each had its advantage. In facts, the reaction mechanism and luminescence properties play a decisive role in the biology application of H2S fluorescence probe. In this despite booming season, in the process of research we still skillfully conceived, in view of H2S with small structure being able to do successive nucleophilic substitution in the same molecules, high selective H2S subcellular detection was realized. Specifically, we take the cyanine (Cy7) with positive charge as a red fluorophore, through the introduction of disulfide bond and carbonate to build the specific reaction sites of H2S, thus avoiding the interference of other sulfur-containing substances in biological systems. After reaction with H2S, the Probe released red fluorophore, realizing mitochondria target H2S detection. Because the advantages of red fluorescence emission probe, the Probe successfully was applied imaging in mice.

Based ‘successive’ nucleophilic substitution mitochondrial-targeted H2S red light emissive fluorescent probe and its imaging in mice

Cysteine plays a crucial role in physiological processes. Therefore, it is necessary to develop a method for detecting cysteine. Fluorimetry has the advantages of convenient detection, short response time, high sensitivity and good selectivity. In this review, fluorescent probes that detect cysteine over the past three years are summarized based on structural features of fluorophores such as coumarin, BODIPY, rhodamine, fluorescein, CDs, QDs, etc and reaction groups including acrylate, aldehyde, halogen, 7-nitrobenzofurazan, etc. Then, effects of different combinations between fluorophores and response groups on probe properties and detection performances are discussed.

https://iopscience.iop.org/article/10.1088/2050-6120/aad580/pdf

Fluorescent probes for detecting cysteine.

Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease.

A novel AIEE and EISPT fluorescent probe for selective detection of cysteine

The invention discloses 2-indolone derivatives and open-ring derivatives thereof, and synthetic method and a use thereof, belongs to the technical field of medicines, and relates to 2-indolone derivatives with the structure represented by general formula (I), and open-ring derivatives (II) thereof. In the formula (I) and formula (II), X is CO(CH2)n-1 and n is 1 to 10, or X is CO(CH2)n-1NH2 and n is 1 to 10; Y is CO or CH2; and R1, R2, R3, R4, R5, R6, R7 and R8 are different substituent groups. The invention also discloses structures, the synthetic methods and an in-vitro acetylcholinesterase and phosphodiesterase 5 inhibition activity, and can be further developed into new medicines for treating the Alzheimer's disease.

2-Indolone derivatives and open-ring derivatives, and synthetic methods and use thereof

The invention provides an aromatic amine acetylcholin esterase inhibitor containing amino side chains having a formula (I) or (II), a pharmaceutically acceptable salt thereof or a stereisomer thereof,preparation methods thereof, and application thereof in preparation of an acetylcholin esterase inhibitor and of drugs for treating alzheimer disease and/or myasthenia gravis, wherein the definitionof each group is shown in the description. As the acetylcholin esterase inhibitor, an aromatic amine derivative containing amino side chains has micromolar to nanomolar inhibitory activity, and has apossibility of further developing into a drug against alzheimer disease. The formula is shown in the description.

Li-yun Zhou

Papers

Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease.

A novel AIEE and EISPT fluorescent probe for selective detection of cysteine

2-Indolone derivatives and open-ring derivatives, and synthetic methods and use thereof

Synthesis and application of aromatic amine acetylcholin esterase inhibitor containing amino side chains