Day: January 5, 2023

Discovery of potent pteridine reductase inhibitors to guide antiparasite drug development was written by Cavazzuti, Antonio;Paglietti, Giuseppe;Hunter, William N.;Gamarro, Francisco;Piras, Sandra;Loriga, Mario;Alleca, Sergio;Corona, Paola;McLuskey, Karen;Tulloch, Lindsay;Gibellini, Federica;Ferrari, Stefania;Costi, Maria Paola. And the article was included in Proceedings of the National Academy of Sciences of the United States of America in 2008.Safety of Ethyl 3-chloroquinoxaline-2-carboxylate This article mentions the following:

Pteridine reductase (PTR1) is essential for salvage of pterins by parasitic trypanosomatids and is a target for the development of improved therapies. To identify inhibitors of Leishmania major and Trypanosoma cruzi PTR1, a rapid-screening strategy using a folate-based library was combined with structure-based design. Assays were carried out against folate-dependent enzymes including PTR1, dihydrofolate reductase (DHFR), and thymidylate synthase. Affinity profiling determined selectivity and specificity of a series of quinoxaline and 2,4-diaminopteridine derivatives, and nine compounds showed greater activity against parasite enzymes compared with human enzymes. Compound I [R = H, Me (II)] displayed a K_i of 100 nM toward LmPTR1, and the crystal structure of the LmPTR1:NADPH:I ternary complex revealed a substrate-like binding mode distinct from that previously observed for similar compounds A second round of design, synthesis, and assay produced a compound II with a significantly improved K_i (37 nM) against LmPTR1, and the structure of this complex was also determined Biol. evaluation of selected inhibitors was performed against the extracellular forms of T. cruzi and L. major, both wild-type and overexpressing PTR1 lines, as a model for PTR1-driven antifolate drug resistance and the intracellular form of T. cruzi. An additive profile was observed when PTR1 inhibitors were used in combination with known DHFR inhibitors, and a reduction in toxicity of treatment was observed with respect to administration of a DHFR inhibitor alone. The successful combination of antifolates targeting two enzymes indicates high potential for such an approach in the development of previously undescribed antiparasitic drugs. In the experiment, the researchers used many compounds, for example, Ethyl 3-chloroquinoxaline-2-carboxylate (cas: 49679-45-0Safety of Ethyl 3-chloroquinoxaline-2-carboxylate).

Ethyl 3-chloroquinoxaline-2-carboxylate (cas: 49679-45-0) belongs to quinoxaline derivatives. Condensed heterocycles of quinoxalines have become attractive targets in synthetic and medicinal chemistry due to their significant biological activities. Quinoxalines are used as dyes, pharmaceuticals, and antibiotics such as echinomycin, levomycin exhibiting antitumoral properties. Quinoxalines establish also the basis of anthelmintics and receptor antagonists.Safety of Ethyl 3-chloroquinoxaline-2-carboxylate

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Electrochemical reactions. XV. Factors which determine the rate of carbon-halogen bond fragmentation in radical anions illustrated by halogenated derivatives of quinoline, quinoxaline, and phenazine was written by Alwair, Khaled;Grimshaw, James. And the article was included in Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999) in 1973.Electric Literature of C8H5ClN2 This article mentions the following:

Halo derivatives of quinoline, quinoxaline, and phenazine in the potential region of the 1st reduction waves were examined by polarog. and cyclic voltammetry in DMF at an Hg cathode. The stability of the C-halogen bond in a halogenated radical anion depended on bond strength and the redox potential of the substrate-radical anion couple. In the experiment, the researchers used many compounds, for example, 6-Chloroquinoxaline (cas: 5448-43-1Electric Literature of C8H5ClN2).

6-Chloroquinoxaline (cas: 5448-43-1) belongs to quinoxaline derivatives. Quinoxalines are important class of heterocyclic compounds, associated with wider pharmacological applications. The parent substance of the group, quinoxaline, results when glyoxal is condensed with 1,2-diaminobenzene. Substituted derivatives arise when α-ketonic acids, α-chlorketones, α-aldehyde alcohols and α-ketone alcohols are used in place of diketones.Electric Literature of C8H5ClN2

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

One-pot synthesis of substituted bistetrazolo[1,5-a:5′,1′-c]quinoxalines was written by Srinivas, B.;Prasanna, B.;Ravinder, M.. And the article was included in Chemical Science Transactions in 2013.Safety of 6-Bromoquinoxaline-2,3(1H,4H)-dione This article mentions the following:

A novel methodol. was developed for synthesis of substituted bis tetrazolo[1,5-a;5′,1′-c]quinoxalines via one pot three-component condensation of quinoxaline-2,3-diones, phosphorous oxychloride and sodium azide. The ambient conditions, excellent product yields, easy work up procedures and short reaction time make this synthetic strategy a better protocol for the synthesis of newer bistetrazoloquinoxalines. The structures of all these compounds were confirmed by their IR, ¹H NMR, ¹³C NMR and mass spectral anal. In the experiment, the researchers used many compounds, for example, 6-Bromoquinoxaline-2,3(1H,4H)-dione (cas: 1910-90-3Safety of 6-Bromoquinoxaline-2,3(1H,4H)-dione).

6-Bromoquinoxaline-2,3(1H,4H)-dione (cas: 1910-90-3) belongs to quinoxaline derivatives. Compounds possessing quinoxaline derivatives were bestowed with a variety of significant biological properties such as antiviral, antimalarial, anticancer, DNA intercalation, DNA duplex stabilization, and many others. They are well-known for application in organic light emitting devices, polymers and pharmaceutical agents. The quinoxaline-containing polymers are applicable in optical devices due to their thermal stability and low band gap.Safety of 6-Bromoquinoxaline-2,3(1H,4H)-dione

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Proton magnetic resonance spectra in aromatic systems. XIII. Heteroaromatic series. 5. 6-Substituted quinoxalines was written by Sasaki, Yoshio;Hatanaka, Minoru;Suzuki, Miyoko. And the article was included in Yakugaku Zasshi in 1969.Category: quinoxaline This article mentions the following:

The chem. shifts of the ring 1H of 6-quinoxalines have been corrected for N anisotropy, N elec. field, and ring current effects. The corrected shifts have also been correlated with the substituent constants σπ, and those corresponding to the π-electron charge density-ρ-distributions were estimated, and converted to ρ values. In the experiment, the researchers used many compounds, for example, 6-Methoxyquinoxaline (cas: 6639-82-3Category: quinoxaline).

6-Methoxyquinoxaline (cas: 6639-82-3) belongs to quinoxaline derivatives. Compounds possessing quinoxaline derivatives were bestowed with a variety of significant biological properties such as antiviral, antimalarial, anticancer, DNA intercalation, DNA duplex stabilization, and many others. Quinoxalines are used as dyes, pharmaceuticals, and antibiotics such as echinomycin, levomycin exhibiting antitumoral properties. Quinoxalines establish also the basis of anthelmintics and receptor antagonists.Category: quinoxaline

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Organic Base Enabled Nickel-Catalyzed Mono-α-Arylation of Feedstock Solvents was written by MacMillan, Joshua W. M.;McGuire, Ryan T.;Stradiotto, Mark. And the article was included in Chemistry – A European Journal in 2022.Application of 5448-43-1 This article mentions the following:

Authors report on authors’ successful development of the first metal-catalyzed mono-α-arylation of carbonyl compounds employing a soluble organic base. The scope of these Ni/DalPhos-catalyzed transformations encompasses a range of (hetero)aryl halides (Cl, Br, I) and phenol-derived electrophiles (sulfonates, carbonates, carbamates, sulfamates), including active pharmaceutical ingredients (chloroquine, clozapine), in combination with the typically problematic feedstock small mol. substrates acetone, dimethylacetamide, and for the first time with any metal catalyst/base, Et acetate. In the experiment, the researchers used many compounds, for example, 6-Chloroquinoxaline (cas: 5448-43-1Application of 5448-43-1).

6-Chloroquinoxaline (cas: 5448-43-1) belongs to quinoxaline derivatives. Quinoxalines have received a significant amount of attention due to their potential use in fighting various pathophysiological conditions like epilepsy, Parkinson’s, and Alzheimer’s diseases. Modifying quinoxaline structure it is possible to obtain a wide variety of biomedical applications, namely antimicrobial activities and chronic and metabolic diseases treatment.Application of 5448-43-1

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider