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Metabolism of the aza-arenes quinoline, isoquinoline, quinazoline, and quinoxaline by a mutant strain of the bacterium Pseudomonas putida resulted in attack at the carbocyclic ring (to yield stable cis-dihydrodiols and phenols) and at the heterocyclic ring (to yield phenols and ring cleavage products).

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Proton-coupled electron-transfer (PCET) steps play a key role in energy conversion reactions. Molecular PCET reactions are well-described by “square schemes” in which the overall thermochemistry of the reaction is broken into its constituent proton-transfer and electron-transfer components. Although this description has been essential for understanding molecular PCET, no such framework exists for PCET reactions that take place at electrode surfaces. Herein, we develop a molecular square scheme framework for interfacial PCET by investigating the electrochemistry of molecularly well-defined acid/base sites conjugated to graphitic electrodes. Using cyclic voltammetry, we first demonstrate that, irrespective of the redox properties of the corresponding molecular analogue, proton transfer to graphite-conjugated acid/base sites is coupled to electron transfer. We then show that the thermochemistry of surface PCET events can be described by the pKa of the molecular analogue and the potential of zero free charge (zero-field reduction potential) of the electrode. This work provides a general framework for analyzing and predicting the thermochemistry of interfacial PCET reactions.

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Quinoxaline – Wikipedia,
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Photophysical properties and photochemical activity of 6-X-5- nitroquinoxalines with electron-donor substituents (X = H, CH3, Cl, OC2H5, NH2) ortho to the nitro group were studied. The quantum yield of the formation of 5-hydroxyquinoxaline from the corresponding nitro derivative depends on the nature of the substituent and irradiation conditions. Phototransformations can go through nitro-nitrite rearrangement with the participation of two alternative T(npi*) levels, depending on the size and electronic effects of the substituent. The latter factor is largely determined by the population on excitation of different charge-transfer states involving the nitro group.

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Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.

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The invention aims to allow a curable composition to have an extended working phase followed by a short time period in which said compound becomes fully cured. This is achieved by the provision of a curable composition comprising the following components: a) at least one polyether and/or at least one polyacrylic acid ester with at least one reactive silyl group as an end-group; b) at least one organotin compound; and c) at least one compound that does not contain any tin or silicon atoms and that has at least two functional groups. Said groups are selected from the following: carboxy, carbonyl or hydroxy groups, or nitrogen atoms that are part of a ring system with aromatic character. In addition, the invention relates to a method for producing such a composition, and to the use thereof as an adhesive, a sealant or as a coating material.

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The synthesis and structure-activity relationship of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound 36, a potent gp120-CD4 inhibitor which exhibited antiviral potency across a spectrum of 25 clade B isolates.

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Quinoxaline – Wikipedia,
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CERTAIN ARYL-ALIPHATIC AND HETEROARYL-ALIPHATIC PIPERAZINYL PYRAZINES AND THEIR USE IN THE TREATMENT OF SEROTONIN-RELATED DISEASES

Compounds of the general formula (I):wherein the variables are as defined in the specification are useful for the prophylaxis or treatment of serotonin-related, especially 5-HT 2 receptor-related, diseases in human beings or animals, particularly diseases related to the 5-HT2 c receptor, especially diseases such as eating disorders, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctionions, and urinary disorders.

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Quinoxaline – Wikipedia,
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Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists

A high throughput screening approach to the identification of selective cholecystokinin-2 receptor (CCK-2R) ligands resulted in the discovery of a novel series of antagonists, represented by 1-[2-[(2,1,3-benzothiadiazol-4- ylsulfonyl)amino]-5-chlorobenzoyl]-piperidine (1; CCK-2R, pKI = 6.4). Preliminary exploration of the structure-activity relationships around the anthranilic ring and the amide and sulfonamide moieties led to a nearly 50-fold improvement of receptor affinity and showed a greater than 1000-fold selectivity over the related cholecystokinin-1 receptor. Pharmacokinetic evaluation led to the identification of 4-[4-iodo-2-[(5-quinoxalinylsulfonyl)amino]benzoyl]- morpholine, 26d, a compound that demonstrates promising pharmacokinetic properties in the rat and dog with respect to plasma clearance and oral bioavailability and is a potent inhibitor in vivo of pentagastrin-stimulated acid secretion in the rat when dosed orally.

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Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis

Persistent bacteria, including persister cells within surface-attached biofilms and slow-growing pathogens lead to chronic infections that are tolerant to antibiotics. Here, we describe the structure-activity relationships of a series of halogenated phenazines (HP) inspired by 2-bromo-1-hydroxyphenazine 1. Using multiple synthetic pathways, we probed diverse substitutions of the HP scaffold in the 2-, 4-, 7-, and 8-positions, providing critical information regarding their antibacterial and bacterial eradication profiles. Halogenated phenazine 14 proved to be the most potent biofilm-eradicating agent (?99.9% persister cell killing) against MRSA (MBEC < 10 muM), MRSE (MBEC = 2.35 muM), and VRE (MBEC = 0.20 muM) biofilms while 11 and 12 demonstrated excellent antibacterial activity against M. tuberculosis (MIC = 3.13 muM). Unlike antimicrobial peptide mimics that eradicate biofilms through the general lysing of membranes, HPs do not lyse red blood cells. HPs are promising agents that effectively target persistent bacteria while demonstrating negligible toxicity against mammalian cells. I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 17056-99-4, help many people in the next few years.Application In Synthesis of Quinoxalin-5-ol

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Quinoline derivatives

Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

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