Archives for Chemistry Experiments of 56346-57-7

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Substrate-based cyclic peptidomimetics of Phe-Ile-Val that inhibit HIV-1 protease using a novel enzyme-binding mode

Results are presented for inhibitors of HIV-1 protease that demonstrate a new strategy for developing peptidomimetics, involving the replacement of flexible segments of peptide substrates with conformationally constrained hydrolytically-stable macrocyclic structural mimics. A 15-membered macrocycle that imitates the tripeptide Phe-Ile-Val was designed and incorporated into the C-terminus of Ac-Leu-Val-Phe-CHOHCH2-{Phe-Ile-Val}-NH2, an inhibitor of HIV-1 protease derived from a substrate sequence. Advantages of the macrocycle over the acyclic peptide include constraining its components into their bioactive conformation and protecting the amide bonds from enzymatic degradation, the cycle being stable to acid, gastric proteases, and plasma. Molecular modeling and X-ray structural studies reveal that the cyclic inhibitors have a unique enzyme-binding mode, the sterically unencumbered hydroxyethylamine isostere binds via both its hydroxyl and protonated nitrogen to the anionic Asp25 catalytic residues. The novel macrocycle superimposes well on the linear peptidic inhibitor for which it was designed as a structural mimic. Structural mimicry led to functional mimicry as shown by comparable inhibition of the protease by cyclic and acyclic molecules. Further modification of the acyclic N-terminus (Leu-Val-Phe) gave stable, water-soluble, potent inhibitors of HIV-1 protease. This approach may have general application to the development of mimetics of other bioactive peptides, including inhibitors of other enzymes.

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Piperidine – Wikipedia,
Piperidine | C5H15456N – PubChem

 

Final Thoughts on Chemistry for 2-(1-Carbamoylpiperidin-4-yl)acetic acid

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Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a potent and selective inhibitor of big MAP kinase 1

Kinome-wide selectivity profiling of a collection of 2-amino-pyrido[2,3-d] pyrimidines followed by cellular structure-activity relationship-guided optimization resulted in the identification of moderately potent and selective inhibitors of BMK1/ERK5 exemplified by 11, 18, and 21. For example, 11 possesses a dissociation constant (Kd) for BMK1 of 19 nM, a cellular IC 50 for inhibiting epidermal growth factor induced BMK1 autophosphorylation of 0.19 ¡À 0.04 muM, and an Ambit KINOMEscan selectivity score (S5) of 0.035. Inhibitors 18 and 21 are also potent BMK1 inhibitors and possess favorable pharmacokinetic properties which enable their use as pharmacological probes of BMK1-dependent phenomena as well as starting points for further optimization efforts.

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Piperidine | C5H11540N – PubChem

 

Discovery of Benzyl 4-formylpiperidine-1-carboxylate

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Reference of 138163-08-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.138163-08-3, Name is Benzyl 4-formylpiperidine-1-carboxylate, molecular formula is C14H17NO3. In a Patent£¬once mentioned of 138163-08-3

HYDROXY SUBSTITUTED ISOQUINOLINONE DERIVATIVES

The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof

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The important role of 203661-69-2

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Related Products of 203661-69-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.203661-69-2, Name is tert-Butyl 2-oxo-7-azaspiro[3.5]nonane-7-carboxylate, molecular formula is C13H21NO3. In a Patent£¬once mentioned of 203661-69-2

NEW DIAZASPIROCYCLOALKANE AND AZASPIROCYCLOALKANE

The invention provides novel compounds having the general formula (I), wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds

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Archives for Chemistry Experiments of 1903-69-1

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BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

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Extended knowledge of 1-Aminopiperidine

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Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids

The synthesis and evaluation of 3-enaminetetramic acids as antibacterial agents is reported; contrary to the analogous 3-acyltetramic acids, the enaminetetramic acid class of compound exhibits modest antibacterial activity against a limited spectrum of organisms, and even that activity is strongly dependent on the identity of the tetramate ring substituents. Moreover, these compounds appear to have a different mode of action to the analogous 3-acyltetramic acids, and appear to offer more limited opportunity for further elaboration in drug discovery.

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The important role of tert-Butyl 4-iodopiperidine-1-carboxylate

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Related Products of 301673-14-3, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 301673-14-3, name is tert-Butyl 4-iodopiperidine-1-carboxylate. In an article£¬Which mentioned a new discovery about 301673-14-3

Visible-Light-Initiated Manganese Catalysis for C?H Alkylation of Heteroarenes: Applications and Mechanistic Studies

A visible-light-driven Minisci protocol that employs an inexpensive earth-abundant metal catalyst, decacarbonyldimanganese Mn2(CO)10, to generate alkyl radicals from alkyl iodides has been developed. This Minisci protocol is compatible with a wide array of sensitive functional groups, including oxetanes, sugar moieties, azetidines, tert-butyl carbamates (Boc-group), cyclobutanes, and spirocycles. The robustness of this protocol is demonstrated on the late-stage functionalization of complex nitrogen-containing drugs. Photophysical and DFT studies indicate a light-initiated chain reaction mechanism propagated by .Mn(CO)5. The rate-limiting step is the iodine abstraction from an alkyl iodide by .Mn(CO)5.

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Awesome and Easy Science Experiments about (S)-1-Benzylpiperidin-3-amine

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NOVEL COMPOUNDS AS ANTI-TUBERCULAR AGENTS

The present invention relates to novel compounds of formula (1): The present invention also discloses compounds of formula (1) along with other pharmaceutical acceptable excipients and use of the compounds as anti-tubercular agents.

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Piperidine | C5H12577N – PubChem

 

Properties and Exciting Facts About 27578-60-5

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Optically active 1,3,4,4-tetrasubstituted beta-lactams: Synthesis and evaluation as tumor cell growth inhibitors

The in vitro cytotoxicity assays of several enantiopure (3S,4S)- and (3R,4R)-1,3,4,4-tetrasubstituted beta-lactams derived from amino acids have shown that the (3S,4S)-4-benzyl-1-p-methoxybenzyl-3-methyl-4-methoxycarbonyl derivative 2a, obtained from Phe, displays significant activity, which is comparable to that of the anticancer drug Doxorubicin against HT29 cell lines. Modifications at positions 1 and 4 of the beta-lactam ring led to identify the Tyr(2,6-ClBz) analogu 26d with similar activity data to those of 2a. The synthesis and SAR of all these tetrasubstituted beta-lactams are reported here.

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Piperidine | C5H4314N – PubChem

 

Final Thoughts on Chemistry for tert-Butyl 3-bromo-4-oxopiperidine-1-carboxylate

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Structure-Function Relationship of Acyl Amino Acid Surfactants: Surface Activity and Antimicrobial Properties

Amino acid surfactants (AAS), having the general structure alpha-amino-(N-acyl)-beta-alkoxypropionate, were synthesized chemically.Surface activity and antimicrobial properties of the AAS were evaluated.Increases in acyl chain length (i.e., C10-C14) resulted in a linear reduction in surface tension (i.e., 43-36 mN*m-1), as well as dramatic decreases in critical micelle concentrations (cmc) (i.e., 17.9-0.43 mM).Strong correlations existed between the cmc of AAS and their minimal inhibitory concentrations (mic) against Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger, and Saccharomyces cerevisiae.Sensitivity of the microorganisms to the various AAS followed the order Staphylococcus aureus > A. niger= S. cerevisiae> E. coli> P. aeruginosa.In comparison with methyl p-hydroxybenzoate, AAS (MN14) showed 2-8, 64, and 4-8 times the activity against Gram-negative bacteria, Gram-positive bacteria, and fungi, respectively.Surface adsorption and/or bifunctional binding to the cell membrane may account for AAS action on microorganisms.

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Piperidine – Wikipedia,
Piperidine | C5H22449N – PubChem