Category: 1885-29-6

White, Kris published the artcileAryl Sulfonamide Inhibits Entry and Replication of Diverse Influenza Viruses via the Hemagglutinin Protein, Application of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is aryl sulfonamide preparation influenza virus entry replication hemagglutinin.

Influenza viruses cause approx. half a million deaths every year worldwide. Vaccines are available but partially effective, and the number of antiviral medications is limited. Thus, it is crucial to develop therapeutic strategies to counteract this major pathogen. Influenza viruses enter the host cell via their hemagglutinin (HA) proteins. The HA subtypes of influenza A virus are phylogenetically classified into groups 1 and 2. Here, we identified an inhibitor of the HA protein, a tertiary aryl sulfonamide, that prevents influenza virus entry and replication. This compound shows potent antiviral activity against diverse H1N1, H5N1, and H3N2 influenza viruses encoding HA proteins from both groups 1 and 2. Synthesis of derivatives of this aryl sulfonamide identified moieties important for antiviral activity. This compound may be considered as a lead for drug development with the intent to be used alone or in combination with other influenza A virus antivirals to enhance pan-subtype efficacy.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Application of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Hwu, Jih Ru published the artcileSynthesis and antiviral activities of quinazolinamine-coumarin conjugates toward chikungunya and hepatitis C viruses, HPLC of Formula: 1885-29-6, the main research area is quinazolinamine coumarin preparation antiviral chikungunya hepatitis C virus; Broad-spectrum; Chikungunya virus; Coumarin; Hepatitis C virus; Quinazolin-4-amine; Structure–activity relationship.

Development of new drugs with broad-spectrum to combat RNA viruses would be beneficial to mankind but faces a great challenge. Authors designed and efficiently synthesized a series of quinazolin-4-amine-SCH2-coumarin conjugated compounds Authors data of the virus-cell-based assay show five new conjugates inhibit chikungunya virus with EC50 values as potent as 1.96μM and two conjugates inhibit hepatitis C virus with EC50 values as low as 16.6μM. These conjugates possess a xylene substituent at the C-4 amino group of quinazoline and a t-Bu substituent at the C-6′ position of coumarin.

European Journal of Medicinal Chemistry published new progress about Antiviral agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Kakoulidou, Chrisoula published the artcileZn(II) complexes of (E)-4-(2-(pyridin-2-ylmethylene)hydrazinyl)quinazoline in combination with non-steroidal anti-inflammatory drug sodium diclofenac: Structure, DNA binding and photo-cleavage studies, antioxidant activity and interaction with albumin, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks), the main research area is preparation zinc pyridinylmethylenehydrazinylquinazoline diclofenac complex; crystal structure zinc pyridinylmethylenehydrazinylquinazoline diclofenac complex; DNA cleavage zinc pyridinylmethylenehydrazinylquinazoline diclofenac complex; Free radical scavenging; Interaction with albumin; Interaction with calf-thymus DNA; Plasmid DNA-photocleavage; Quinazoline derivatives; Zn(II) complexes.

The interaction of the novel quinazoline (E)-4-(2-(pyridin-2-ylmethylene)hydrazinyl)quinazoline (L) with Zn2+ was performed in the absence or presence of the non-steroidal antiinflammatory drug sodium diclofenac (Nadicl) and gave complexes [Zn(L)2](NO3)2·MeOH (1·MeOH) and [Zn(L)(dicl-O)2]·MeOH (2·MeOH), resp. The two complexes were characterized by IR and 1H NMR spectroscopy and by single-crystal x-ray crystallog. In these complexes, L was tridentately coordinated to Zn(II) via the quinazoline, hydrazone and pyridine nitrogen atoms. Further studies concerning the behavior of the compounds towards calf-thymus (CT) DNA and supercoiled circular pBluescript KS II plasmid DNA (pDNA) were performed. The complexes may bind to CT DNA via intercalation, with complex 1 showing higher binding affinity than 2. The complexes may cleave pDNA in the absence or presence of irradiation with UVA, UVB or visible light and the most active pDNA-cleavager is compound 1. The binding constants of the compounds for bovine serum albumin were calculated and the subdomain of the albumin where the compounds prefer to bind was determined The free radical scavenging ability of the compounds was evaluated towards 1,1-diphenyl-picrylhydrazyl and 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radicals with complex 2 being the most active compound Thus, complex of type 1 maybe a lead compound for the development of novel DNA-binders and DNA-cleavers or photo-cleavers for medical and biotechnol. “”on demand”” applications, whereas the structure of complex type 2 may provide novel antioxidants and radical scavengers.

Journal of Inorganic Biochemistry published new progress about Crystal structure. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Recommanded Product: 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Qurban, Jihan published the artcileSynthesis, characterization and reactivity of novel pseudocyclic hypervalent iodine reagents with heteroaryl carbonyl substituents, Safety of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is heteroaryl hydroxy benzoiodaoxolium triflate preparation crystal structure oxidative reaction.

Two new hypervalent iodine reagents containing furan and thiophene moieties in addition to a carbonyl group in the vicinity of the iodine atom were synthesized and characterized. The X-ray anal. of both compounds revealed a strong intramol. contact between the carbonyl oxygen and the hypervalent iodine atom with tosylate as a counter ion. The two reagents showed a broad range of synthetic applications and proved to be versatile oxidizing agents.

Chemical Communications (Cambridge, United Kingdom) published new progress about Crystal structure. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Safety of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Rozhkova, Yuliya S. published the artcileSynthesis of novel racemic 3,4-dihydroferroceno[c]pyridines via the Ritter reaction, Safety of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is dihydroferroceno pyridine preparation crystal mol structure; Ritter reaction methyl ferrocenylpropanol nitrile methansulfonic acid.

A new approach for the synthesis of functionalized racemic 3,4-dihydroferroceno[c]pyridines via the Ritter reaction of 2-methyl-1-ferrocenylpropan-1-ol with nitriles in the presence of methansulfonic acid was developed. The scope and limitations of the reaction were evaluated. Selected racemic 3,4-dihydroferroceno[c]pyridines were successfully separated by preparative HPLC on a Chiralcel OD-H column. The absolute configuration of the enantiomers was determined by x-ray crystal structure anal.

Tetrahedron Letters published new progress about Crystal structure. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Safety of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Gao, Zeng published the artcileBronsted Acid Catalyzed Cyclization of Inert N-Substituted Pyrroles to Benzo[ f ]pyrrolo[1,2-a][1,4]diazepines, HPLC of Formula: 1885-29-6, the main research area is benzopyrrolodiazepine preparation; substituted pyrrole tandem intramol dehydroxylation cyclization Bronsted Acid catalyzed; enantioselective preparation benzopyrrolodiazepine; pyrrolylphenyl methanamine chiral phosphoric acid catalyzed intermol addition.

Two approaches involving intramol. and intermol. cyclization, resp., were developed for the direct and practical construction of a series of important benzo[f]pyrrolo[1,2-a][1,4]azepines such as I [R = H, Me, Ph, etc.; R1 = H, Me, Cl] by using Bronsted acid catalysts. Upon catalysis by TsOH, the intramol. dehydroxylation/ring closure of 3-hydroxy-2-[2-(1 H-pyrrol-1-yl)benzyl]isoindolin-1-ones provided various racemic benzo[f]pyrrolo[1,2-a][1,4]azepines in high yields. Furthermore, enantioenriched benzo[f]pyrrolo[1,2-a][1,4]azepines II [R = H, Me; R1 = H, Cl; R2 = H, Cl, F] were also obtained by chiral phosphoric acid catalyzed intermol. addition of [2-(1 H-pyrrol-1-yl)phenyl]methanamines to 2-formylbenzoates under mild conditions.

Synlett published new progress about Addition reaction. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Rossi, Michele published the artcileSustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer’s Disease, HPLC of Formula: 1885-29-6, the main research area is sustainable drug multitarget ligand Alzheimer disease Anacardium neuroprotective.

The multifactorial nature of Alzheimer’s disease (AD) is a reason for the lack of effective drugs as well as a basis for the development of “”multi-target-directed ligands”” (MTDLs). As cases increase in developing countries, there is a need of new drugs that are not only effective but also accessible. With this motivation, we report the first sustainable MTDLs, derived from cashew nutshell liquid (CNSL), an inexpensive food waste with anti-inflammatory properties. We applied a framework combination of functionalized CNSL components and well-established acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) tacrine templates. MTDLs were selected based on hepatic, neuronal, and microglial cell toxicity. Enzymic studies disclosed potent and selective AChE/BChE inhibitors (5, 6, and 12), with subnanomolar activities. The X-ray crystal structure of 5 complexed with BChE allowed rationalizing the observed activity (0.0352 nM). Investigation in BV-2 microglial cells revealed antineuroinflammatory and neuroprotective activities for 5 and 6 (already at 0.01μM), confirming the design rationale.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Macha, Baswaraju published the artcileDesign and Friedlander Reaction Based Synthesis of New Cycloalkyl Ring Fused Quinolines as Multifunctional Agents for Alzheimer’s Treatment: In Silico Studies, Safety of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is cycloalkyl ring fused quinoline preparation acetylcholinesterase butyrylcholinesterase inhibitor.

A new series of acetylcholinesterase and butyrylcholinesterase inhibitors were designed based on the structure of tacrine and synthesized in multicomponent Friedlander reaction between 2-aminobenzonitrile and cycloalkanones. The synthesized tacrine analogs were characterized by spectral data and evaluated for acetylcholinesterase and butyryl cholinesterase inhibitory activity by following Ellman method. Compound I and II with piperazine containing acetamide and butyrylamide chains have shown equal potency to that of tacrine with IC50 values 0.71 +/= 0.04 and 1.01 +/= 0.03μM, and 0.52 +/= 0.03 and 0.73 +/= 0.04μM, against AChE and BuChE resp. when compared to standard tacrine with IC50 of 0.23 +/= 0.4μM and 0.31 +/= 0.03, whereas rivastigmine showed 0.47 +/= 0.2 and 0.65 +/= 0.02μM against AChE and BuChE, resp. Also, some of the potent compounds were tested for liver toxicity and were found to be much safer than tacrine. Thus, these new tacrine analogs with five, six and seven membered ‘C’ rings have emerged as new cholinesterase inhibitors for further exploitation as anti-Alzheimer’s agents. Docking studies of all the mols. disclosed close hydrogen bond interactions within the binding site.

ChemistrySelect published new progress about Alzheimer disease. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Safety of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Cheng, Xiao-jing published the artcileTacrine-Hydrogen Sulfide Donor Hybrid Ameliorates Cognitive Impairment in the Aluminum Chloride Mouse Model of Alzheimer’s Disease, HPLC of Formula: 1885-29-6, the main research area is tacrine hydrogen sulfide Alzheimer antiAlzheimer acetylcholinesterase; AChE; HS donor; Tacrine; hepatotoxicity; neuroinflammation; synaptic plasticity.

Alzheimer’s disease (AD) is a neurodegenerative disorder, characterized by progressive loss of memory and cognitive function, and is associated with the deficiency of synaptic acetylcholine, as well as chronic neuroinflammation. Tacrine, a potent acetylcholinesterase (AChE) inhibitor, was previously a prescribed clin. therapeutic agent for AD, but was recently withdrawn because it caused widespread hepatotoxicity. Hydrogen sulfide (H2S) has neuroprotective, hepatoprotective and anti-inflammatory effects. In this study, we synthesized a new compound, a tacrine- H2S donor hybrid (THS) by introducing H2S-releasing moieties (ACS81) to tacrine. Subsequently, pharmacol. and biol. evaluations of THS were conducted in the aluminum trichloride (AlCl3)-induced AD mice model. We found that THS (15mmol/kg) improved cognitive and locomotor activity in AD mice in the step-through test and open field test resp. THS showed strong AChE inhibitory activity in the serum and hippocampus of AD mice and induced increased hippocampal H2S levels. Furthermore, THS reduced mRNA expression of the proinflammatory cytokines, TNF-α, IL-6, and IL-1β and increased synapse-associated proteins (synaptophysin and postsynaptic d. protein 95) in the hippocampus of AD mice. Importantly, THS, unlike tacrine, did not increase liver transaminases (alanine transaminase and aspartate transaminase) or proinflammatory cytokines, indicating THS is much safer than tacrine. Therefore, the multifunctional effects of this new hybrid compound of tacrine and H2S indicate it is a promising compound for further research into the treatment of AD.

ACS Chemical Neuroscience published new progress about Alzheimer disease. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Maspero, Marco published the artcileTacrine-xanomeline and tacrine-iperoxo hybrid ligands: Synthesis and biological evaluation at acetylcholinesterase and M1 muscarinic acetylcholine receptors, Application of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is xanomeline tacrine iperoxo hybrid preparation acetylcholinesterase muscarinic acetylcholine receptor; Allosteric modulation; Bitopic ligands; Ellman’s assay; Inositol monophosphate; Iperoxo; M(1) muscarinic acetylcholine receptor; Multitarget compounds; Phospholipase C; Tacrine; Xanomeline.

A set of new hybrid derivatives, in which apolymethylene spacer chain of variable length connected the pharmacophoric moiety of xanomeline are synthesized ,anM1/M4preferring orthosteric muscarinic agonist, with that of tacrine, a well-known acetylcholinesterase (AChE) inhibitor abletoallosterically modulatemuscarinicacetylcholinereceptors(mAChRs). When tested in vitro in a colorimetric assay for their ability to inhibit AChE, the new compounds showed higher or similar potency compared to that of tacrine. Docking analyses were performed on the most potent inhibitors to rationalize their exptl. inhibitory power against AChE. Next, the signaling cascade at M1 mAChRs by exploring the interaction of Gαq-PLC-β3 proteins through split luciferase assays and the myo-Inositol 1 phosphate (IP1) accumulation in cells is evaluated. The results were compared with those obtained on the known derivatives, two quite potent AChE inhibitors in which tacrine is linked to iperoxo, an exceptionally potent muscarinic orthosteric activator. Interestingly, it was found that iprexo tacrine hybrids behaved as partial agonists of the M1 mAChR, at variance with hybrids containing xanomeline as the orthosteric mol. fragment, which were all unable to activate the receptor subtype response.

Bioorganic Chemistry published new progress about Alzheimer disease. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Application of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts