Day: November 16, 2022

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

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

Srinivas, B. published the artcileSynthesis and Antimicrobial Screening of Novel Tetrazolo Triazolo Substituted Mercapto Quinoxalines, HPLC of Formula: 39267-05-5, the main research area is thio tetrazolotriazoloquinoxaline preparation antibacterial antifungal.

A novel and convenient synthesis of 6-thio-tetrazolo[1,5-a][1,2,4]triazolo[3,4-c]quinoxalines I [R = allyl, (CH2)2Br, prop-2-yn-1-yl, Bn; R1 = R2 = H, Me; R1 = Me, R2 = H] starting from 2,3-dichloroquinoxalines was reported. The newly synthesized compounds I were screened for their in vitro anti-microbial activity against Staphylococcus aureus and Bacillus subtilis as Gram-pos. bacteria, Escherichia coli and Pseudomonas aeruginosa as Gram-neg. bacteria. Among all the synthesized compounds, compounds I [R = (CH2)2Br, R1 = R2 = H; R = (CH2)2Br, R1 = Me, R2 = H; R = (CH2)2Br, R1 = R2 = Me] showed good activity and I [R = allyl; R1 = R2 = H, Me] showed moderate activity against B. subtilis and Gram-neg. bacterial strains E. coli and P. aeruginosa. They were also evaluated for their in vitro anti-fungal potential against Candida albicans and compounds I [R = (CH2)2Br, R1 = R2 = H; R = (CH2)2Br, R1 = Me, R2 = H; R = (CH2)2Br, R1 = R2 = Me] showed appreciable activity and I [R = allyl; R1 = R2 = H] showed moderate activity against tested fungal strains C. albicans organism.

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, HPLC of Formula: 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Alhayek, Alaa published the artcileDiscovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases, Name: 2,3-Dichloro-6-methylquinoxaline, the main research area is FDA approved inhibitor clostridia bacillus collagenase antibacterial.

In view of the worldwide antimicrobial resistance (AMR) threat, new bacterial targets and anti-infective agents are needed. Since important roles in bacterial pathogenesis have been demonstrated for the collagenase H and G (ColH and ColG) from Clostridium histolyticum, collagenase Q1 and A (ColQ1 and ColA) from Bacillus cereus represent attractive antivirulence targets. Furthermore, repurposing FDA-approved drugs may assist to tackle the AMR crisis and was addressed in this work. Here, we report on the discovery of two potent and chem. stable bacterial collagenase inhibitors: synthesized and FDA-approved diphosphonates and hydroxamates. Both classes showed high in vitro activity against the clostridial and bacillary collagenases. The potent diphosphonates reduced B. cereus-mediated detachment and death of cells and Galleria mellonella larvae. The hydroxamates were also tested in a similar manner; they did not have an effect in infection models. This might be due to their fast binding kinetics to bacterial collagenases.

Journal of 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, Name: 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Alhayek, Alaa published the artcileDiscovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases, SDS of cas: 25983-14-6, the main research area is FDA approved inhibitor clostridia bacillus collagenase antibacterial.

In view of the worldwide antimicrobial resistance (AMR) threat, new bacterial targets and anti-infective agents are needed. Since important roles in bacterial pathogenesis have been demonstrated for the collagenase H and G (ColH and ColG) from Clostridium histolyticum, collagenase Q1 and A (ColQ1 and ColA) from Bacillus cereus represent attractive antivirulence targets. Furthermore, repurposing FDA-approved drugs may assist to tackle the AMR crisis and was addressed in this work. Here, we report on the discovery of two potent and chem. stable bacterial collagenase inhibitors: synthesized and FDA-approved diphosphonates and hydroxamates. Both classes showed high in vitro activity against the clostridial and bacillary collagenases. The potent diphosphonates reduced B. cereus-mediated detachment and death of cells and Galleria mellonella larvae. The hydroxamates were also tested in a similar manner; they did not have an effect in infection models. This might be due to their fast binding kinetics to bacterial collagenases.

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, SDS of cas: 25983-14-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Obafemi, Craig A. published the artcileSynthesis and some reactions of 3-chloro-2-(cyanomethylene)-1,2-dihydroquinoxalines, Application In Synthesis of 39267-05-5, the main research area is dichloroquinoxaline malononitrile substitution; chloroquinoxaline cyanomethylene preparation.

2,3-Dichloroquinoxaline and some of its derivatives have been reacted with malononitrile and Et cyanoacetate to yield a variety of 3-chloro-2-(cyanomethylene)-1,2-dihydroquinoxaline derivatives, e.g., I. The reaction of 3-chloro-2-(dicyanomethylene)-1,2-dihydroquinoxaline (I) with pyridine and its Me derivatives led to zwitterionic structures, e.g., II. The structures of the newly synthesized compounds were assigned by spectroscopic data and elemental analyses.

Molecules published new progress about Substitution reaction. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Application In Synthesis of 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Ivanova, Bojidarka published the artcileQuinoxalines as potent selective CRFRs ligands for monitoring and brain diagnostic, HPLC of Formula: 25983-14-6, the main research area is quinoxaline CRFR ligand brain diagnostic; Brain diagnostic; CRFRs; Quinoxalines.

The paper highlighted quinoxalines as potent ligands to corticotropin-releasing factor receptor types 1 and 2. The content includes design and structure-activity relationship of 50 model substances to CRFR1, CRFR2α and CRF2β, resp. It is important to bear in mind, that our concept has based on challenging research task, designing for selective CRFRs ligands. Because,: (i) These macromols. can bond more than one ligand, thus causing for a distinct physiol. response; (ii) CRFRs also participate readily in protein-protein interactions; (iii) CRFRs have two step activation mechanism and; (iv) CRFR1 has low selectivity. In spite of, numerous research efforts, which have been devoted to the isolation of series peptidic and non-peptidic CRFRs agonists, the poor penetration across blood-brain barrier restricts, their wide application in the clin. practice. Furthermore, the biol. role of CRFR2 is not yet fully understood. For that reason, the studies of the structure-activity relationship have significant impact in the field. The great advantages of quinoxalines as prospective ligands are based on their: (a) One-step synthetic road, using mild exptl. conditions and, allowing to involve various functional groups in the mol. scaffold as well as good-to-excellent yields, employing Fischer and Hinsberg methods; (b) High selectivity to CRFRs sub-types and; (c) Tunable fluorescence emission within the frame of a large scale of the electromagnetic spectrum ∈ 500-700 nm.

Bioorganic Chemistry published new progress about Biological permeation. 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, HPLC of Formula: 25983-14-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider