Archives for Chemistry Experiments of 3-Phenyl-6-chloropyridazine

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Enzymatic enantioselective ester hydrolysis by carboxylesterase NP

The enzymatic hydrolysis of a series of carboxylic esters by carboxylesterase NP has been investigated in order to determine the scope and limitations of this enzyme. 2-Substituted propionates were hydrolyzed with high enantioselectivity when an aromatic moiety was part of the 2-substituent.Enantioselective hydrolysis could be accomplished with several 2-arypropionates, 2-(aryloxy)propionates and N-arylalanine esters.The propionate esters yielded propionic acids as (S) enantiomers, whereas the alanine esters yielded the (R) enantiomers.Without a 2-aryl substituent, the enzymatic hydrolysis of the propionates occurred at a lower rate without acceptable enantioselectivity.In addition to 2-substituted propionates, only a few other esters were hydrolyzed with high enantioselectivity by carboxylesterase NP, such as some prochiral disubstituted malonates. 1-Phenylethylacetate was the only substrate with chirality in the alcohol part of the ester that was found to be hydrolyzed enantioselectively.Carboxylesterase NP proved to be a powerful enzyme for kinetic resolution of propionate esters with an aromatic ring containing a 2-substituent.

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Pyridazine | C4H4N2744 – PubChem

 

Archives for Chemistry Experiments of 3-Phenyl-6-chloropyridazine

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A novel kinetically-controlled peptide synthesis – Dramatic increase of chemical yield with retention of chiral integrity

Peptide synthesis employing the highly selective reaction of isobutyl chloroformate at the carboxyl group of the N-protected amino acid, almost to the exclusion of the amino group of the C-protected amino acid, is described. This one-stage, kinetically-controlled strategy remarkably affords peptides with excellent optical purity in high chemical yields.

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Pyridazine | C4H4N2742 – PubChem

 

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 20375-65-9, name is 3-Phenyl-6-chloropyridazine, introducing its new discovery. Formula: C10H7ClN2

Biaryl-bridged macrocyclic peptides: Conformational constraint via carbogenic fusion of natural amino acid side chains

A general method for constraining peptide conformations via linkage of aromatic sidechains has been developed. Macrocyclization of suitably functionalized tri-, tetra- and pentapeptides via Suzuki-Miyaura cross-coupling has been used to generate side chain to side chain, biaryl-bridged 14- to 21-membered macrocyclic peptides. Biaryl bridges possessing three different configurations, meta-meta, meta-ortho, and ortho-meta, were systematically explored through regiochemical variation of the aryl halide and aryl boronate coupling partners, allowing fine-tuning of the resultant macrocycle conformation. Suzuki-Miyaura macrocyclizations were successfully achieved both in solution and on solid phase for all three sizes of peptide. This approach constitutes a means of constraining peptide conformation via direct carbogenic fusion of side chains of naturally occurring amino acids such as phenylalanine and tyrosine, and so is complementary to strategies involving non-natural, for example, hydrocarbon, bridges.

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Pyridazine | C4H4N2697 – PubChem

 

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STEREOSELECTIVE HYDROLYSIS OF AMINO ACID ESTERS BY MODIFIED POLY(ETHYLENIMINE)S WITH COVALENTLY-LINKED DIPEPTIDE CONTAINING A HISTIDYL RESIDUE

Stereoselective hydrolyses of chiral substrates were examined in poly(ethylenimine) derivatives with optically active groups.A high stereoselective effect, kL/kD = 3.6, is observed.The effect of the substrate structure influenced both the rate constant and the stereoselective ratio in the hydrolyses by poly(ethylenimine) derivatives.

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Synthesis and utilization of chiral alpha-methylated alpha-amino acids with a carboxyalkyl side chain in the design of novel Grb2-SH2 peptide inhibitors free of phosphotyrosine

The growth factor receptor-bound protein 2 (Grb2) is an SH2 domain-containing docking module that represents an attractive target for anticancer therapeutic intervention. To improve the potency and bioavailability of the Grb2-SH2 inhibitors, the chiral alpha-methyl-alpha-carboxyalkyl amino acid [(alpha-Me)Aa] was designed to cover dual structural and functional features separately contributed by 1-aminocyclohexanecarboxylic acid (Ac6c) and alpha-aminoadipic acid (Adi) in position Y + 1. The enantiopure L(or D)-(alpha-Me)Aa bearing various chain length carboxylalkyl side chain was conveniently synthesized by an optimized oxazolidinone methodology. The incorporation of (S)-(alpha-Me)Aa into the non-pTyr-containing peptide framework with a 5-amino acid sequence binding motif of X-2-Leu- (3?-substituted-Tyr)0-X+1-Asn really improved the inhibitory activity, affording potent (R)-sulfoxide-bridged cyclic and an open-chain series of pentapeptide inhibitors of Grb2-SH2 domain (IC50 = 1.1-5.8 muM). More significantly, these (alpha-Me)Aa incorporated peptide inhibitors showed excellent activities in inhibiting the growth of erbB2-dependent MDA-MB-453 tumor cell lines with low micromolar IC50 values, owing to the reduced peptidic nature and absence of pTyr or pTyr mimetics.

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Pyridazine | C4H4N2690 – PubChem

 

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Broadening of the substrate tolerance of alpha-chymotrypsin by using the carbamoylmethyl ester as an acyl donor in kinetically controlled peptide synthesis

In the kinetically controlled approach of peptide synthesis mediated by alpha-chymotrypsin, the broadening of the protease’s substrate tolerance is achieved by switching the acyl donor from the conventional methyl ester to the carbamoylmethyl ester. Thus, as a typical example, the extremely low coupling efficiency obtained by employing the methyl ester of an inherently poor amino acid substrate, Ala, is significantly improved by the use of this particular ester. Its ameliorating effect is observed also in the couplings of other amino acid residues such as Gly and Ser as carboxy components.

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Pyridazine | C4H4N2702 – PubChem

 

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New antituberculotics originated from salicylanilides with promising in vitro activity against atypical mycobacterial strains

A new series of 30 N-protected amino acid esters were prepared as a part of ongoing search for new anti-tuberculosis active salicylanilides. The esters possess high in vitro activity against Mycobacterium tuberculosis, Mycobacterium avium, and two strains of Mycobacterium kansasii, where one is an isolate from the patient, with MIC in the range 1-32 mumol/L for all tested strains. The prepared esters can be considered as prodrugs with better bio-availability and as more efficient transport forms through the mycobacterial cell membranes due to the higher lipophilicity. The experimental and calculated lipophilicity, stability, antituberculotic activity, cytotoxicity as well as the quantitative structure-activity relationships (QSARs) explored by the Intelligent Problem Solver (IPS) in Trajan Neural Network Simulator 6.0 are presented.

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Pyridazine | C4H4N2658 – PubChem

 

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Synthesis and pharmacological properties of ureidomethylcarbamoylphenylketone derivatives. A new potent and subtype-selective nonpeptide CCK-B/gastrin receptor antagonist, S-0509

A novel series of CCK-B/gastrin receptor antagonists – ureidomethylcarbamoylphenylketone derivatives – were designed, synthesized, and evaluated for activity. Structure-activity relationship studies revealed the importance of a carboxylic acid at substituent R2 and a tert-butoxycarbonyl group at R1 in structure A. Compound 7a (S-0509) showed remarkable affinity for the CCK-B/gastrin receptor and a subtype selectivity profile in vitro. Administration (id) of 7a led to excellent inhibition of gastric acid secretion induced by pentagastrin in anesthetized rats with an ED50 value of 0.014 mg/kg. Furthermore, 7a proved to have poor blood-brain permeability by its small effect on enhancement of morphine analgesia. Thus, S-0509 has an increase in selectivity for the peripheral effects of gastrin antagonism from the central effects of CCK-B antagonism.

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Pyridazine | C4H4N2637 – PubChem

 

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Application of 20375-65-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.20375-65-9, Name is 3-Phenyl-6-chloropyridazine, molecular formula is C10H7ClN2. In a Article£¬once mentioned of 20375-65-9

Amino Acid-Derived Chiral Acyl Nitroso Compounds: Diastereoselectivity in Intermolecular Hetero Diels-Alder Reactions

The diastereoselectivities of chiral acyl nitroso dienophiles derived from optically pure N-protected alpha-amino hydroxamic acids have been determined in intermolecular hetero Diels-Alder reactions.The cycloaddition reactions afforded synthetically useful quantities of functionally rich, optically pure cycloadducts, useful for the preparation of a variety of compounds of potential biological interest.Molybdenum hexacarbonyl reduction of the cycloadducts gave optically pure allylic alcohols.Osmium teraoxide-catalyzed dihydroxylation of several bis-allylically substituted intermediates gave only the diastereomerically pure diols corresponding to naturally occurring 2′,3′-dihydroxynucleoside analogs.

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Pyridazine | C4H4N2729 – PubChem

 

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 20375-65-9, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 20375-65-9, name is 3-Phenyl-6-chloropyridazine. In an article£¬Which mentioned a new discovery about 20375-65-9

Tetrabutylammonium hydroxide/p-toluenesulphonyl chloride , a novel peptide coupling agent

A new peptide coupling reagent TBA+OH-/TsCl, is reported.This peptide coupling is free of any racemization when carbobenzoxy protected aminoacids are used.

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Pyridazine | C4H4N2698 – PubChem