Tag: M.W=200-250

Li, Yan published the artcileStereoselective synthesis and fungicidal activities of (E)-α-(methoxyimino)-benzeneacetate derivatives containing 1,3,4-oxadiazole ring, Application In Synthesis of 35112-27-7, the main research area is stereoselective synthesis fungicidal activity methoxyiminobenzeneacetate oxadiazolyl.

Fifteen novel (E)-α-(methoxyimino)benzeneacetate derivatives, the analogs of strobilurins, which contain two pharmacophoric substructures of (E)-Me methoxyiminoacetate moiety and 1,3,4-oxadiazole ring were stereoselectively synthesized. It was first found that the coupling reaction could give stereoselectively the key intermediate (E)- and (Z)-Me 2-(hydroxyimino)-2-o-tolylacetate with a ratio of 14:1. The preliminary bioassays indicated that all the compounds I (R = H, 4-MeO, 2,3-Cl2, 2-I, etc.) showed potent fungicidal activity against Rhizoctonia solani, Botrytis cinereapers, Gibberella zeae, Physalospora piricola and Bipolaris mayclis, and all of the tested compounds had more potent fungicidal activities against R. solani than Kresoxim-Me.

Bioorganic & Medicinal Chemistry Letters published new progress about Agrochemical fungicides. 35112-27-7 belongs to class chlorides-buliding-blocks, name is Ethyl 2,5-dichlorobenzoate, and the molecular formula is C9H8Cl2O2, Application In Synthesis of 35112-27-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Okuzumi, Tatsuya published the artcileEfficient solid-phase synthesis of diverse 1,2,3-benzotriazin-4-ones using tert-butyl nitrite, HPLC of Formula: 3032-32-4, the main research area is solid phase combinatorial synthesis benzotriazinone derivative aminobenzamide diazotization cyclization.

The solid-phase synthesis of 1,2,3-benzotriazin-4-ones, e.g. I, via the intramol. cyclization of 2-aminobenzamides through diazotization using tert-Bu nitrite is reported. Addnl., a small library of 1,2,3-benzotriazin-4-ones was combinatorially prepared utilizing this methodol. In view of the fact that this library contains three points of diversity, the preparation of a large number of compounds is possible.

Tetrahedron Letters published new progress about Combinatorial chemistry. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, HPLC of Formula: 3032-32-4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Lee, Jun Young published the artcileDesign, synthesis and biological evaluation of 2-aminoquinazolin-4(3H)-one derivatives as potential SARS-CoV-2 and MERS-CoV treatments, Recommanded Product: 2-Amino-3,6-dichlorobenzoic acid, the main research area is arylaminoquinazolinone preparation anticoronaviral activity; structure arylaminoquinazolinone inhibition SARS CoV2 MERS; pharmacokinetics metabolism toxicity hERG cytochrome inhibition dichlorophenylaminoquinazolinone; 2-aminoquinazolinone; Antiviral; Coronavirus; MERS-CoV; SARS-CoV-2.

Despite the rising threat of fatal coronaviruses, there are no general proven effective antivirals to treat them. 2-Aminoquinazolin-4(3H)-one derivatives were newly designed, synthesized, and investigated to show the inhibitory effects on SARS-CoV-2 and MERS-CoV. Among the synthesized derivatives, 7-chloro-2-((3,5-dichlorophenyl)amino)quinazolin-4(3H)-one I (R = Cl; R1 = H) and 2-((3,5-dichlorophenyl)amino)-5-hydroxyquinazolin-4(3H)-one I (R = H; R1 = HO) showed the most potent anti-SARS-CoV-2 activities (IC50 < 0.25μM) and anti-MERS-CoV activities (IC50 < 1.1μM) with no cytotoxicity (CC50 > 25μM). In addition, both compounds showed acceptable results in metabolic stabilities, hERG binding affinities, CYP inhibitions, and preliminary PK studies.

Bioorganic & Medicinal Chemistry Letters published new progress about Anticoronaviral agents. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Recommanded Product: 2-Amino-3,6-dichlorobenzoic acid.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kersten, Philip published the artcileEnzymic release of halogens or methanol from some substituted protocatechuic acids, Synthetic Route of 62936-23-6, the main research area is protocatechuate metabolism bacteria halogen methanol.

Four strains of gram-neg. bacteria capable of growing at the expense of 5-chlorovanillate were isolated from soil, and the metabolism of 1 strain was studied in particular detail. In the presence of α,α’-bipyridyl, a suspension of 5-chlorovanillate-grown cells accumulated 5-chloroprotocatechuate from 5-chlorovanillate; in the absence of inhibitor these compounds, and various other 5-substituted protocatechuates and vanillates, were oxidized to completion. Cell suspensions of this strain grown on 5-chlorovanillate or vanillate released Cl- quant. from 5-chlorovanillate and released MeOH from syringate. Extracts of cells grown with 4-hydroxybenzoate, vanillate, or syringate possessed high levels of both protocatechuate 4,5-dioxygenase and 2-pyrone-4,6-dicarboxylate hydrolase; extracts from acetate-grown cells did not. Protocatechuate 4,5-dioxygenase, purified from strains that could grow with 5-chlorovanillate, oxidized 5-halogeno-protocatechuates and 3-O-methylgallate with the formation of 2-pyrone-4,6-dicarboxylate. A crude extract converted 5-chloroprotocatechuate into pyruvate plus oxaloacetate. A meta-fission reaction sequence is proposed for the bacterial degradation of vanillate and protocatechuate substituted at C-5 of the benzene ring with halogen or methoxyl.

Journal of Bacteriology published new progress about Comamonas testosteroni. 62936-23-6 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-hydroxy-5-methoxybenzoic acid, and the molecular formula is C8H7ClO4, Synthetic Route of 62936-23-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Elkamhawy, Ahmed published the artcileThiazolidine-2,4-dione-based irreversible allosteric IKK-β kinase inhibitors: Optimization into in vivo active anti-inflammatory agents, Name: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is IKK beta modulators signaling pathway allosteric modulation antiinflammatory; Allosteric modulation; Anti-inflammatory; IKK-β modulators; NF-κB signaling pathway; Thiazolidine-2,4-diones.

Selective kinase inhibitors development is a cumbersome task because of ATP binding sites similarities across kinases. On contrast, irreversible allosteric covalent inhibition offers opportunity to develop novel selective kinase inhibitors. Previously, we reported thiazolidine-2,4-dione lead compounds eliciting in vitro irreversible allosteric inhibition of IKK-β. Herein, we address optimization into in vivo active anti-inflammatory agents. We successfully developed potent IKK-β inhibitors with the most potent compound eliciting IC50 = 0.20μM. Cellular assay of a set of active compounds using bacterial endotoxin lipopolysaccharide (LPS)-stimulated macrophages elucidated significant in vitro anti-inflammatory activity. In vitro evaluation of microsomal and plasma stabilities showed that the promising compound 7a is more stable than compound 7p. Finally, in vivo evaluation of 7a, which has been conducted in a model of LPS-induced septic shock in mice, showed its ability to protect mice against septic shock induced mortality. Accordingly, this study presents compound 7a as a novel potential irreversible allosteric covalent inhibitor of IKK-β with verified in vitro and in vivo anti-inflammatory activity.

European Journal of Medicinal Chemistry published new progress about Allosteric modulators. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Name: 4-(4-Chlorophenoxy)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yu, Haihua published the artcileControllable access to multi-substituted imidazoles via palladium(II)-catalyzed C-C coupling and C-N condensation cascade reactions, HPLC of Formula: 480438-56-0, the main research area is imidazole preparation; aminoacetonitrile boronic acid palladium catalyst cascade condensation cyclization.

A novel and efficient protocol for the synthesis of various 2,4-disubstituted, 1,2,4-trisubstituted and 1,2,4,5-tetra-substituted imidazoles I [R1 = Me, CF3, Ph, etc.; R2 = H, Ph, Bn; R3 = H, Me; R4 = Ph, 4-FC6H4, 2-MeC6H4, etc.] via cascade palladium catalyzed C-C coupling followed by intramol. C-N bond formation was developed. Readily accessible boronic acids and N-substituted-2-aminoacetonitriles were firstly reported as starting materials to construct di-, tri-, and tetra-substituted imidazoles in good to excellent yield. The protocol was the first report to prepare multi-substituted imidazoles from readily accessible aminoacetonitrile and boronic acid.

Chemical Communications (Cambridge, United Kingdom) published new progress about Condensation reaction. 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, HPLC of Formula: 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ruso, Jayaraman Sembian published the artcileOxidative cyclisation based one-pot synthesis of 3-substituted[1,2,4]triazolo[4,3-b]pyridazines using Me4NBr/oxone, Synthetic Route of 93118-03-7, the main research area is triazolopyridazine derivative preparation oxidative cyclization.

A facile one-pot synthesis of 3-substituted triazolopyridazine and thieno-triazolopyridazine derivatives is described. This protocol involves the preparation of heteroaryl hydrazone from the aldehyde and pyridazinohydrazine derivative followed by subjecting the intermediate directly to oxidative cyclization to assemble the desired 1,2,4-triazole moiety by employing the mixture of Me4NBr and oxone. This condition is efficient and is able to tolerate wide range of functional groups.

Journal of the Korean Chemical Society published new progress about Oxidative cyclization. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Synthetic Route of 93118-03-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Hu, Baihua published the artcileDiscovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRβ, Safety of 2-Chloro-3-(trifluoromethyl)benzaldehyde, the main research area is cinnoline quinoline derivative preparation structure liver X receptor agonist.

A series of cinnolines/quinolines was prepared and it was found that 4-phenyl-cinnoline/quinolines with either a 2′,3′ or 2′,5′-disubstituted benzyloxy moiety or the 1-Me-7-indole methoxy moiety on the meta position of the 4-Ph ring showed good binding selectivity for LXRβ over LXRα. The LXRβ binding selective modulators displayed good activity for inducing ABCA1 gene expression in J774 macrophage cell line and poor efficacy in the LXRα Gal4 functional assay. 26, 37 and 41 were examined for their ability to induce SREBP-1c gene expression in Huh-7 liver cell line and they were weak partial agonists.

Bioorganic & Medicinal Chemistry published new progress about Antiatherosclerotics. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Safety of 2-Chloro-3-(trifluoromethyl)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gopal Hegde, Subramanya published the artcileRegioselective synthesis and biological evaluation of novel dispiropyrrolidine derivatives via one-pot four-component reaction, COA of Formula: C13H9ClO2, the main research area is sarcosine barbituric acid ninhydrin benzaldehyde magnesium silicate four component; dispiro indeno pyrrolidine pyrimidine pentaone regioselective preparation microwave irradiation; antitumor antibacterial activity SAR.

A new series of regioselective dispiropyrrolidine analogs I [Ar = Ph, 4-pyridinyl, 2-methyl-4-chlorophenyl, etc] via efficient one-pot four-component tandem reaction was discovered. The reaction was carried out in the presence of four common reactants and magnesium silicate nanoparticles (NPs) in ethanol under microwave irradiation The reaction proceeded rapidly and was completed within 60-90 min. This methodol. offered several significant advantages such as high yield, mild catalyst and easy to perform. The synthesized compound was further screened for antibacterial and antiproliferative activities. The results showed that compound I [Ar = 4-nitrophenyl, phenyl] were potent antibacterials against Gram-pos. and Gram-neg. bacteria. Further, compound I [Ar = phenyl] showed best antiproliferative activity against tested cell lines.

Synthetic Communications published new progress about Antibacterial agents. 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, COA of Formula: C13H9ClO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kulathooran, S. published the artcileSynthesis and biological activities of novel heterocyclic chalcone derivatives by two different methods using anhydrous potassium carbonate as an efficient catalyst, Application In Synthesis of 93118-03-7, the main research area is acetyl dimethylfuran aryl aldehyde potassium carbonate catalyst microwave irradiation; chalcone preparation diastereoselective green chem antibacterial antifungal activity SAR.

A series of twenty 3-(aryl)-1-(2,5-dimethylfuran-3-yl)prop-2-en-1-one I [R = 2,5-(F)2-C6H3, 2-naphthyl, 2-biphenyl, etc.] were synthesized by using conventional and microwave irradiation methods in the presence of anhydrous potassium carbonate as an safe, inexpensive and efficient basic catalyst. Synthesized compounds were evaluated for their in-vitro antimicrobial activity against variety of microbial strains and it was characterized by IR, NMR (1H & 13C) and mass spectral anal. The biol. screening results indicated that some of the compounds showed significant antibacterial and antifungal activities. Compound I [R = 3-methyl-2-thiophenyl] displayed excellent antimicrobial activity against various microbial strains. The newly synthesized high potent compound I [R = 3-methyl-2-thiophenyl] was subjected to thermogravimetric anal. (TGA), differential scanning calorimetric (DSC) and single crystal XRD.

Pharma Chemica published new progress about Antibacterial agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Application In Synthesis of 93118-03-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics