Tag: M.W=150-200

Taylor, Scott D. published the artcileA Fresh Look at the Staudinger Reaction on Azido Esters: Formation of 2H-1,2,3-Triazol-4-ols from α-Azido Esters Using Trialkyl Phosphines, Computed Properties of 27412-71-1, the main research area is triazolol preparation; azido acid ester preparation reaction phosphine.

Ph esters of α-azido acids react with trialkylphosphines in THF/H2O to give 5-substituted 2H-1,2,3-triazol-4-ols in good to excellent yields. In contrast, their reaction with PPh3 in THF/H2O give the amino esters as the major product and no triazoles. Reaction between an α-azido Ph ester and P(OEt)3 provided the corresponding phosphoramidate in excellent yield, but no triazole was formed. The authors warn that 5,5-diphenyl-3,5-dihydro-4H-1,2,3-triazol-4-one and 1,2,3-triazaspiro[4.4]non-1-en-4-one decompose explosively at higher temperatures

Organic Letters published new progress about Crystal structure. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Computed Properties of 27412-71-1.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Encinas, Lourdes published the artcileEncoded Library Technology as a Source of Hits for the Discovery and Lead Optimization of a Potent and Selective Class of Bactericidal Direct Inhibitors of Mycobacterium tuberculosis InhA, Formula: C9H14N2O2, the main research area is pyrrolidinylpyrazolecarboxamide benzofuranylcarbonyl derivative preparation tuberculostatic structure activity.

Tuberculosis (TB) is one of the world’s oldest and deadliest diseases, killing a person every 20 s. InhA, the enoyl-ACP reductase from Mycobacterium tuberculosis, is the target of the frontline antitubercular drug isoniazid (INH). Compounds that directly target InhA and do not require activation by mycobacterial catalase peroxidase KatG are promising candidates for treating infections caused by INH resistant strains. The application of the encoded library technol. (ELT) to the discovery of direct InhA inhibitors yielded compound I endowed with good enzymic potency but with low antitubercular potency. This work reports the hit identification, the selected strategy for potency optimization, the structure-activity relationships of a hundred analogs synthesized, and the results of the in vivo efficacy studies performed with the lead compound II.

Journal of Medicinal Chemistry published new progress about Crystal structure. 769132-77-6 belongs to class pyrazoles-derivatives, name is 3-Isobutyl-1-methyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C9H14N2O2, Formula: C9H14N2O2.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Mugnaini, Claudia published the artcileSynthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease, HPLC of Formula: 637336-53-9, the main research area is adamantanylcarboxamidothiophene preparation cannabinoid 2 receptor agonist skin inflammation; CB2R agonists; CBR ligands; Chemokine release; Skin inflammation.

A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist Me 2-[((adamantan-1-yl)carbonyl)amino]-4-ethyl-5-methylthiophene-3-carboxylate , showing the best balance between receptor affinity and selectivity, was tested in vitro in an exptl. model of allergic contact dermatitis and is able to block the release of MCP-2 in HaCaT cells at 10 μM concentration

European Journal of Medicinal Chemistry published new progress about Allergic contact dermatitis. 637336-53-9 belongs to class pyrazoles-derivatives, name is Methyl 4-amino-1-methyl-1H-pyrazole-3-carboxylate, and the molecular formula is C6H9N3O2, HPLC of Formula: 637336-53-9.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Elfahham, H. A. published the artcileSynthesis of heterocycles through the reactions of nitrilimines with amino and oxo diazoles, Safety of 5-Phenyl-1H-pyrazol-3(2H)-one, the main research area is pyrazoletriazole; pyrazolopyrazine; pyrazoloimidazole; nitrilimine cyclocondensation diazole; pyrazole amino hydroxy cyclocondensation nitrilimine.

Fused azoles such as pyrazolo[5,1-c][1,2,4]triazoles, pyrazolo[3,4-b]pyrazine and pyrazolo[1,5-a]imidazole have been prepared from the reactions of nitrilimines , produced from hydrazidoyl halides I (R = Cl, Me, MeO), or II (R1 = NO2, Me), with amino- and oxo-azoles. In some cases acyclic products are formed.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Cyclocondensation reaction. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Safety of 5-Phenyl-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Mugnaini, Claudia published the artcileDesign, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide Derivatives with Antiosteoarthritic Activity In Vivo, Quality Control of 637336-53-9, the main research area is hydroxy oxopyrazolopyridine carboxamide preparation antiosteoarthritic osteoarthritis cannabinoid type receptor.

The hallmark of joint diseases, such as osteoarthritis (OA), is pain, originating from both inflammatory and neuropathic components, and compounds able to modulate the signal transduction pathways of the cannabinoid type-2 receptor (CB2R) can represent a helpful option in the treatment of OA. In this perspective, a set of 18 cannabinoid type-2 receptor (CB2R) ligands was developed based on an unprecedented structure. With the aim of improving the physicochem. properties of previously reported 4-hydroxy-2-quinolone-3-carboxamides, a structural optimization program led to the discovery of isosteric 7-hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide derivatives These new compounds are endowed with high affinity for the CB2R and moderate to good selectivity over the cannabinoid type-1 receptor (CB1R), associated with good physicochem. characteristics. As to the functional activity at the CB2R, compounds able to act either as agonists or as inverse agonists/antagonists were discovered. Among them, compound I emerged as a potent CB2R agonist able to reduce pain in rats carrying OA induced by injection of monoiodoacetic acid (MIA).

Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 637336-53-9 belongs to class pyrazoles-derivatives, name is Methyl 4-amino-1-methyl-1H-pyrazole-3-carboxylate, and the molecular formula is C6H9N3O2, Quality Control of 637336-53-9.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Elfahham, Hassan A. published the artcileThe reactions of nitrile imines with amino- and oxo-substituted azoles, Name: 5-Phenyl-1H-pyrazol-3(2H)-one, the main research area is azole reaction nitrile imine hydrazonyl halide; pyrazole cyclization hydrazonyl chloride; pyrazolopyrazole; pyrazolotriazole; azatricycloundecanone; adamantanone oxime rearrangement.

The behavior of several amino and hydroxy azoles toward nitrile imines and hydrazonyl halides is reported. Thus, the pyrazoles I (R = Ph, R1 = H2N, OH) reacted with PhCCl:NNHPh to give the pyrazolopyrazole II. I (R = Me, R1 = OH) under identical conditions gave the pyrazolotriazole III. I (R = Ph, R1 = NH2) reacted with MeCOCCl:NNHPh to give the pyrazoloimidazole IV.

Chemistry Letters published new progress about Cycloaddition reaction. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Name: 5-Phenyl-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Elfahham, Hassan Attia published the artcileNovel synthesis of pyrazolo[5,1-c]-1,2,4-triazoles, imidazo[1,2-b]pyrazoles, and [1,2,4]-triazolo[4,3-a]benzimidazoles. Reaction of nitrile imines with amino- and oxo-substituted diazoles, Safety of 5-Phenyl-1H-pyrazol-3(2H)-one, the main research area is pyrazolotriazole; imidazopyrazole; triazolobenzimidazole; hydrazonyl chloride condensation cyclization diazole.

RCCl:NNHPh (I; R = Ph, COMe) reacted with cyclic amidines and azolones to give condensation products. In some cases intramol. cyclocondensation occurred to give the title heterocyclic compounds E.g., reaction of antipyrine II (R = H) with I (R = Ph) in refluxing EtOH containing Et3N for 3 h gave 86% II (R = CPh:NNHPh) whereas reaction of I (R = COMe) with pyrazole III under the above conditions gave 91% pyrazolotriazole IV.

Journal of the Chemical Society, Perkin Transactions 11: Organic and Bio-Organic Chemistry published new progress about Condensation reaction. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Safety of 5-Phenyl-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Kolodyazhna, Tatiana I. published the artcileSome Aspects of 4H-Pyrans Synthesis Based on 4-Chloro-1-ethyl-1H-benzo[c][1,2]thiazine-3-carbaldehyde 2,2-dioxide: Antimicrobial Activity of the Compounds Synthesized, Quality Control of 27412-71-1, the main research area is sigma linked benzopyrazolopyranothiazine dioxide preparation antibacterial antifungal.

A three-component interaction of 4-chloro-1-ethyl-1H-benzo[c][1,2]thiazine-3-carbaldehyde 2,2-dioxide with malononitrile and enol nucleophiles of heterocyclic nature has been studied. Depending on the nature of an enol nucleophile this reaction can lead either to heterocyclic ensemble of σ-linked 4-chloro-1-ethyl-1H-benzo[c][1,2]thiazine 2,2-dioxide and 2-amino-4H-pyran rings or condensed tetracyclic derivatives containing a new heterocyclic core of 7,10-dihydro-5H-benzo[c]pyrazolo[4′,3′:5,6]pyrano[2,3-e][1,2]thiazine 6,6-dioxide. The same result was obtained in the case of two-component approach involving 2-((4-chloro-1-ethyl-2,2-dioxido-1H-benzo[c][1,2]thiazin-3-yl)methylene)malononitrile. The structure of the tetracyclic derivatives has been confirmed by 2D NMR experiments A plausible mechanism of the three-component interaction resulting in the two possible products has been proposed. The synthesized compounds were screened for in vitro antibacterial and antifungal activities.

ChemistrySelect published new progress about Antibacterial agents. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Quality Control of 27412-71-1.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Xu, Peng published the artcileNovel pleuromutilin derivatives with excellent antibacterial activity against Staphylococcus aureus, Safety of 3-Isobutyl-1-methyl-1H-pyrazole-5-carboxylic acid, the main research area is pleuromutilin derivative antibacterial activity Staphylococcus.

Ten novel pleuromutilin derivatives with thioether moiety and heterocyclic carboxamide or chloroformate group in the side chain were synthesized and confirmed by 1H NMR, IR and HRMS. The results of the antibacterial activity showed that the title compounds had excellent antibacterial activity against Staphylococcus aureus, among which the MIC of 5f reached 0.03125 μg/mL.

Chemical Biology & Drug Design published new progress about Antibacterial agents. 769132-77-6 belongs to class pyrazoles-derivatives, name is 3-Isobutyl-1-methyl-1H-pyrazole-5-carboxylic acid, and the molecular formula is C9H14N2O2, Safety of 3-Isobutyl-1-methyl-1H-pyrazole-5-carboxylic acid.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Johnson, Matthew P. published the artcileAzo dienophiles. Diels-Alder reactions of 4-phenyl-1,2,4-triazole-3,5-dione and 5-phenylpyrazol-3-one with functionalized dienes, Recommanded Product: 5-Phenyl-1H-pyrazol-3(2H)-one, the main research area is Diels Alder phenyltriazoledione phenylpyrazolone diene; triazoledione phenyl Diels Alder diene; pyrazolone phenyl Diels Alder diene; regioselectivity Diels Alder phenylpyrazolone acetoxybutadiene.

The title triazoledione (I) underwent Diels-Alder reactions with a variety of dienes. E.g., reaction of [ICH2C(:CH2)]2 with I in CH2Cl2 at -50° for 15 min then -20° overnight gave 60% adduct II (R = R3 = iodo, R1R2 = bond) (III). Reduction of III with a Zn-Cu couple gave 97% II (RR1 = R2R3 = bond) which in turn reacted with a variety of dienophiles, including I, in a tandem Diels-Alder reaction. 5-Phenylpyrazol-3-one, generated in situ by oxidation of the corresponding pyrazolinone with Pb(OAc)4, also underwent a variety of Diels-Alder reactions, including regioselective reaction with AcOCH:CHCH:CH2 in CH2Cl2 to give 67% pyrazolopyridazine IV.

Journal of the Chemical Society, Perkin Transactions 12: Organic and Bio-Organic Chemistry published new progress about Diels-Alder reaction. 27412-71-1 belongs to class pyrazoles-derivatives, name is 5-Phenyl-1H-pyrazol-3(2H)-one, and the molecular formula is C9H8N2O, Recommanded Product: 5-Phenyl-1H-pyrazol-3(2H)-one.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics