Category: 39267-05-5

Yang, Yanchun published the artcileAn Efficient Synthesis of Quinoxalinone Derivatives as Potent Inhibitors of Aldose Reductase, SDS of cas: 39267-05-5, the main research area is oxoquinoxalinylacetic acid phenoxy anilino preparation aldose reductase inhibitor; quinoxalinone phenoxy anilino preparation aldose reductase inhibitor.

A novel and facile synthesis of quinoxalinone derivatives was developed in which a wide range of 3-chloroquinoxalin-2(1H)-ones as key intermediates can be generated chemo- and regioselectively in good yields from corresponding quinoxaline-2,3(1H,4H)-diones. This new protocol is arguably superior, as it allows the design and preparation of a variety of bioactive quinoxaline-based compounds, which are particularly effective in the treatment of diabetes and its complications. Through this procedure, a new class of quinoxalinone-based aldose reductase inhibitors were synthesized successfully. Most of the inhibitors, with an N1-acetic acid head group and a substituted C3-phenoxy side chain, proved to be potent and selective. Their IC50 values ranged from 11.4 to 74.8 nM. Among them, 2-(3-(4-bromophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid and 2-(6-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid were the most active. Structure-activity relationship and mol. docking studies highlighted the importance of the ether spacer in the C3-phenoxy side chains, and provided clear guidance on the contribution of substitutions both at the core structure and the side chain to activity.

ChemMedChem published new progress about Molecular docking. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, SDS of cas: 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Lee, Young Bok published the artcileSynthesis and anticancer activity of new 1-[(5 or 6-substituted 2-alkoxyquinoxalin-3-yl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives, Related Products of quinoxaline, the main research area is anticancer quinoxalinyl piperazine derivative preparation SAR.

A series of novel quinoxalinyl-piperazine compounds, 1-[(5 or 6-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives were synthesized and evaluated as an anticancer agent. From screening of quinoxalinyl-piperazine compound library, we identified that many compounds inhibited proliferation of various human cancer cells at nanomolar concentrations Among them, one of the fluoro quinoxalinyl-piperazine derivatives, 25 (I), showed its IC50 values ranging from 11 to 21 nΜ in the growth inhibition of cancer cells. This compound also displayed a more potent effect than paclitaxel against paclitaxel resistant HCT-15 colorectal carcinoma cells. The potency of this novel compound was further confirmed with the synergistic cytotoxic effect with several known cancer drugs such as paclitaxel, doxorubicin, cisplatin, gemcitabine or 5-fluorouracil in cancer cells. This strong cell killing effect was derived from the induction of apoptosis. Mechanistic studies have shown that this quinoxalinyl-piperazine compound is a G2/M-specific cell cycle inhibitor and inhibits anti-apoptotic Bcl-2 protein with p21 induction. Thus the results suggest that our compound has potential use in the growth inhibition of drug resistant cancer cells and the combination therapy with other clin. approved anticancer agents as well.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Related Products of quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Nakhi, Ali published the artcileTransition metal free hydrolysis/cyclization strategy in a single pot: synthesis of fused furo N-heterocycles of pharmacological interest, SDS of cas: 39267-05-5, the main research area is chloroquinoxaline alkynyl hydrolysis cyclization; furoquinoxaline preparation sirtuins inhibitory activity; furopyrazine preparation sirtuins inhibitory activity.

A transition metal free tandem two-step strategy has been developed involving hydrolysis of 2-chloro-3-alkynyl quinoxalines/pyrazines followed by in situ cyclization of the corresponding 2-hydroxy-3-alkynyl intermediates in a single pot leading to fused furo N-heterocycles as potential inhibitors of sirtuins. A representative compound I showed promising pharmacol. properties in vitro and in vivo.

Organic & Biomolecular Chemistry published new progress about Antitumor agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, SDS of cas: 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Thabit, Mohamed G. published the artcileSynthesis and biological evaluation of new 3-(4-substituted phenyl)aminoquinoxaline derivatives as anticancer agents, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline, the main research area is phenylaminoquinoxaline preparation anticancer mol modeling human.

Quinoxaline derivatives e.g. I, were synthesized and evaluated for their in vitro growth inhibitory activities against liver carcinoma cell line (HEPG2) using the sulforhodiamine B assay. The synthesis was achieved by reaction of 2,3-dichloroquinoxalines with 4-aminoacetophenone to give the corresponding 2-(4-acetylphenylamino)-3-quinoxaline derivatives Claisen-Schmidt condensation reaction of these quinoxaline derivatives with furfuraldehyde gave enones, which were transformed into pyridines, isoxazolines, pyrazolines, and pyrimidines via several synthetic routes. Virtual screening was carried out by mol. modeling evaluation of the designed compounds Biol. evaluation of the prepared compounds showed that most of the synthesized compounds exhibit more than 50% growth inhibitory.

Heterocyclic Communications published new progress about Antitumor agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Kumar, K. Shiva published the artcileAlCl3-mediated heteroarylation-cyclization strategy: one-pot synthesis of fused quinoxalines containing the central core of Lamellarin D, Application of 2,3-Dichloro-6-methylquinoxaline, the main research area is pyranoindole quinoxaline preparation enzyme antitumor; indole acid quinoxaline heteroarylation cyclization.

An inexpensive, practical and one-pot method has been developed for the synthesis of quinoxalines fused with pyrano[3,4-b]indole, I (R = H, CH3; R1 = H, CH3; R2 = H, CH3; R3 = H, F, CH3; R4 = H, CH3, CH2CH3, CH2=CHCH2) the central core of Lamellarin D. The methodol. involved construction of the central pyranone ring via an AlCl3-mediated heteroarylation-cyclization method. A number of compounds I are prepared by using this methodol., some of which were converted to the corresponding indol-3-ylquinoxaline derivatives II (R = H, CH3; R1 = H; R2 = H, CH3; R3 = H, CH3; R4 = H, CH2CH3). Several of the pyrano[3,4-b]indole fused quinoxalines I showed promising growth inhibition of cervical and lung cancer cells and good interactions with topoisomerase I in silico.

RSC Advances published new progress about Antitumor agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Application of 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Srinivas, B. published the artcileSynthesis of some new tetrazolo[1,5-a]quinazolino[2,3-c]imidazo[4,5-b]quinoxaline derivatives as antimicrobial agents, HPLC of Formula: 39267-05-5, the main research area is quinoxalinoimidazoquinazoline preparation antibacterial antifungal activity; tetrazoloquinazolinoimidazoquinoxaline preparation antibacterial antifungal activity.

A series of 6,7-dimethoxy-2-chloroquinazolo-[3,4-c]-imidazo-[4,5-6]-quinoxalines I [R = H, Me, Cl, Br, O2N] and 7,8-dimethoxytetrazolo-[1,5-a]-quinazolo-[2,3-c]-imidazo-[4,5-b]-quninoxalines II were synthesized by the reaction of 6,7-dimethoxy-2-chloroquinazolin-4-amine and 7,8-dimethoxytetrazolo-[1,5-a]-quinazolin-5-amine in acetic acid/DMF. The chem. structures of the newly synthesized compounds were characterized by IR, NMR, mass spectral and CHN anal. All the title compounds were subjected to in-vitro antibacterial testing against two pathogenic strains and antifungal screening against two fungi. Among the tested compounds, II [R = Me,Cl] showed significant antibacterial and antifungal activities. Also the compound I [R = Me] showed significant antifungal activity against Candida albicans.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Antibacterial agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, HPLC of Formula: 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Lian, Xu published the artcileAnti-MRSA drug discovery by ligand-based virtual screening and biological evaluation, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline, the main research area is virtual screening biol evaluation Staphylococous aureus resistant methicillin ligand; Antibacterial agent; Antibiotic resistance; DNA Gyrase inhibitors; MRSA; Virtual screening.

S. aureus resistant to methicillin (MRSA) is one of the most-concerned multidrug resistant bacteria, due to its role in life-threatening infections. There is an urgent need to develop new antibiotics against MRSA. In this study, we firstly compiled a data set of 2,3-diaminoquinoxalines by chem. synthesis and antibacterial screening against S. aureus, and then performed cheminformatics modeling and virtual screening. The compound with the Specs ID of AG-205/33156020 was discovered as a new antibacterial agent, and was further identified as a Gyrase B (GyrB) inhibitor. In light of the common features, we hypothesized that the 6c as the representative of 2,3-diaminoquinoxalines also inhibited GyrB and eventually proved it. Via mol. docking and mol. dynamics simulations, we identified binding modes of AG-205/33156020 and 6c to the ATPase domain of GyrB. Importantly, these GyrB inhibitors inhibited the MRSA strains and showed selectivity to HepG2 and HUVEC. Taken together, this research work provides an effective ligand-based computational workflow for scaffold hopping in anti-MRSA drug discovery, and discovers two new GyrB inhibitors that are worthy of further development.

Bioorganic Chemistry published new progress about Antibacterial agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Revathi, T. published the artcileSynthesis of novel tetrazolo and triazolo [1,2-e] imidazolo [4,5-b] quinoxaline derivatives as antimicrobial agents, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline, the main research area is quinoxaline imidazolo preparation antibacterial antifungal activity; dichloroquinoxaline amine heterocyclization potassium carbonate catalyst.

An efficient general method has been described for the synthesis of novel tetrazolo and triazolo[1,2-e]imidazolo[4,5-b]quinoxaline derivatives I (R1 = R2 = H, CH3; R1 = NO2, Br, Cl) and II by the reaction of (1H)-tetrazol-5-amine and (3H)-1,2,3-triazol-4-amine with substituted 2,3-dichloroquinoxaline in DMF solvent and added a catalytic amount of K2CO3. The synthesized compounds I and II were evaluated for their antimicrobial activity against Bacillus subtilis, Staphylococcus aureus (Gram pos. bacteria), Escherichia coli (Gram Neg. bacteria) and Aspergillus niger, Candida albicans (fungi). The quinoxalines I [R1 = NO2, Cl; R2 = H] and II [R1 = NO2, Cl; R2 = H] were identified as potent antimicrobial agents.

World Journal of Pharmaceutical Research published new progress about Antibacterial agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Dasari, Gouthami published the artcileSynthesis and anti microbial activity of tetrazolo quinoxaline containing pyrazole analogues, Safety of 2,3-Dichloro-6-methylquinoxaline, the main research area is tetrazoloquinoxalinyl dihydropyrazolone preparation antibacterial antifungal; tetrazoloquinoxalinylpyrazolidinedione preparation antibacterial antifungal.

In the present work some novel substituted 5-methyl-2-(tetrazolo[1,5-a]quinoxalin-4-yl)-2,4-dihydro-3H-pyrazol- 3-ones and substituted 1-(tetrazolo[1,5-a] quinoxalin-4-yl) pyrazolidin-3,5- diones were synthesized. These derivatives were synthesized by treating 4- hydrazinyl tetrazolo[1,5-a]quinoxalines with ethylaceto acetate and di-Et malonate in acetic acid solution All the synthesized compounds were characterized by IR, 1H-NMR and Elemental Anal. All the newly synthesized derivatives were evaluated for anti-microbial activity on different micro-organisms (E.coli, S. aureus, A.niger, C.albicans) at the concentration of 10μg/mL and 20μg/mL by using agar disk-diffusion method. The activity was measured in terms of zone of inhibition and compared with standard drug ciprofloxacin for antibacterial and Flucanazole for antifungal activity.

Heterocyclic Letters published new progress about Antibacterial agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Safety of 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Srinivas, B. published the artcileSynthesis and anti-microbial activity of novel series of Substituted 2-(Tetrazolo[1,5-a]quinoxalin-4-yl)-2,3-dihydrophthalazine-1,4-dione derivatives, Formula: C9H6Cl2N2, the main research area is tetrazoloquinoxalinyl dihydrophthalazine dione preparation antibacterial antifungal.

A novel and efficient synthesis of 2-(substituted tetrazolo[1,5-a]quinoxalin-4-yl)-2,3-dihydrophthalazine-1,4-diones I (R1 = H, CH3, Cl, Br, NO2, OCH3; R2 = H, CH3) has been carried out. The substituted 4-hydrazinyl tetrazoloquinoxalines were treated with phthalic anhydride. All the synthesized compounds were screened for anti-microbial activity. Among all the synthesized compounds I (R1 = R2 = H, CH3) and I (R1 = Cl, Br, NO2, OCH3; R2 = H) showed moderate activity against gram-pos. bacterial strains S. aureus and gram-neg. bacterial strains E. coli. Compound I (R1 = NO2; R2 = H) showed appreciable activity against C. albicans and A. niger fungal strains.

Pharma Chemica published new progress about Antibacterial agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Formula: C9H6Cl2N2.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider