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A short, efficient, and highly stereoselective synthesis of a series of (3R,6R,7R)-2,5-diketopiperazine oxytocin antagonists and their pharmacokinetics in rat and dog is described. Prediction of the estimated human oral absorption (EHOA) using measured lipophilicity (CHI log D) and calculated size (cMR) has allowed us to rank various 2,5-diketopiperazine templates and enabled us to focus effort on those templates with the greatest chance of high bioavailability in humans. This rapidly led to the 2?,4?-difluorophenyl- dimethylamide 25 and the benzofuran 4 with high levels of potency (pK i) and good bioavailability in the rat and dog. Dimethylamide 25 is more potent (>20-fold) than 4 in vivo and has a high degree of selectivity toward the vasopressyi receptors, > 10000 for hV1a/hV1b and ?500 for hV2. It has a good Cyp450 profile with no time dependent inhibition and was negative in the genotoxicity screens with a satisfactory oral safety profile in rats.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4699N – PubChem

 

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Disclosed is a hair revitalizing tonic composition containing a dimethylpropanediol derivative of the formula: wherein R1 and R2 are each independently a C1-30 hydrocarbon group which may be substituted, or a five- or six-membered heterocyclic group which contains 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen atoms and which may be substituted, R3 is hydrogen atom, an alkyl group which may be substituted, an acyl group, an alkoxycarbonyl group, a phenoxycarbonyl group, or a carbamoyl group which may be substituted, and a and b are each 0 or 1, as well as a method for effecting hair growth promotion, hair growth stimulation, or hair loss prevention in mammals by using such a hair revitalizing tonic composition. Also disclosed is the use of a compound of formula (I) in the preparation of a hair revitalizing tonic composition. Thus, this invention can provide an excellent means of hair revitalization or hair loss prevention in mammals.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4577N – PubChem

 

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Related Products of 27578-60-5, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 27578-60-5, Name is N-(2-Aminoethyl)piperidine, molecular formula is C7H16N2. In a Article,once mentioned of 27578-60-5

A number of new xanthenone and benzo[b]xanthenone amino derivatives and their pyrazole-fused counterparts have been designed and synthesized possessing structural analogy to the potent anticancer agent 9-methoxypyrazoloacridine. The synthesis of the compounds proceeds through nucleophilic substitution of 1-chloro-4-nitroxanthenone or the corresponding benzo[b]xanthenone by the appropriately substituted amine or hydrazine, reduction of the nitro group, and conversion into the suitable dialkylaminoacetamides. This method cannot be applied for synthesis of the pyrazole-fused benzo[b]xanthenones, consequently a different, simple, and high-yielding synthetic procedure was developed for the preparation of the target molecules. In vitro cytotoxic potencies of the new derivatives toward the murine leukemia L1210 cell line, human colorectal adenocarcinoma (HT-29), and human uterine sarcoma (MES-SA and its 100-fold resistant to doxorubicin variant MES-SA/D x 5) cell lines are described and compared to those of reference drugs. The compounds exhibited significant cytotoxic activity against the tested cell lines and in addition they retain activity against the multidrug resistant MES-SA/D x 5 subline, showing resistant factors close to 1. A number of derivatives were found to posses DNA binding capacity, according to a standard ethidium bromide displacement assay. The majority of the studied compounds induce a G2/M arrest, although among them some G1 or S blockers have also been identified.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4791N – PubChem

 

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Formula: C7H16N2, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 27578-60-5, Name is N-(2-Aminoethyl)piperidine, molecular formula is C7H16N2. In a Patent, authors is ,once mentioned of 27578-60-5

The present invention relates to novel terephthalamide derivatives and in particular to novel terephthalamide derivatives of the following formula 1, its pharmaceutically acceptable salts as antiviral agents having remarkable inhibitory actions against the proliferation of various viruses including HIV and HBV, and preparing method thereof STR1 wherein R1, R2 and R3 are the same as defined in the detailed description of the present invention.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4185N – PubChem

 

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Chemistry is traditionally divided into organic and inorganic chemistry. Quality Control of: N-(2-Aminoethyl)piperidine. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 27578-60-5

The synthesis of a series of novel 1-unsubstituted and 1-alkyl-1,2,3,4-tetrahydro<1>benzothieno<2,3-b>pyrazine-2,3-diones 4a-d and their corresponding dialkylaminoalkylamino derivatives 6a-d starting from 2-nitro-3-bromobenzothiophene is described.The title ring system has not been reported previously.

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Piperidine – Wikipedia,
Piperidine | C5H4140N – 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, 27578-60-5, name is N-(2-Aminoethyl)piperidine, introducing its new discovery. Application In Synthesis of N-(2-Aminoethyl)piperidine

The mechanisms by which odors induce instinctive behaviors are largely unknown. Odor detection in the mouse nose is mediated by >1, 000 different odorant receptors (ORs) and trace amine-associated receptors (TAARs). Odor perceptions are encoded combinatorially by ORs and can be altered by slight changes in the combination of activated receptors. However, the stereotyped nature of instinctive odor responses suggests the involvement of specific receptors and genetically programmed neural circuits relatively immune to extraneous odor stimuli and receptor inputs. Here, we report that, contrary to expectation, innate odor-induced behaviors can be context-dependent. First, different ligands for a given TAAR can vary in behavioral effect. Second, when combined, some attractive and aversive odorants neutralize one another’s behavioral effects. Both a TAAR ligand and a common odorant block aversion to a predator odor, indicating that this ability is not unique to TAARs and can extend to an aversive response of potential importance to survival. In vitro testing of single receptors with binary odorant mixtures indicates that behavioral blocking can occur without receptor antagonism in the nose. Moreover, genetic ablation of a single receptor prevents its cognate ligand from blocking predator odor aversion, indicating that the blocking requires sensory input from the receptor. Together, these findings indicate that innate odor-induced behaviors can depend on context, that signals from a single receptor can block innate odor aversion, and that instinctive behavioral responses to odors can be modulated by interactions in the brain among signals derived from different receptors.

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Piperidine – Wikipedia,
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A series of new 1,4-naphtho-and benzoquinone derivatives possessing N-, S-, O-substituted groups which has not been reported yet has been synthesized from 2,3-dichloro-1,4-naphthoquinone 1 and 2,3,5,6-tetrachlorocyclohexa-2,5-diene-1,4-dione 15 involving a Michael addition. In the synthesized compounds, antimicrobial activity at low concentrations against Escherichia coli B-906, Staphylococcus aureus 209-P, and Mycobacterium luteum B-917 bacteria and Candida tenuis VKM Y-70 and Aspergillus niger F-1119 fungi in comparison with controls was identified. 2-Chloro-3-((2-(piperidin-1-yl)ethyl)amino)naphthalene-1,4-dione 3g and 2,5-dichloro-3-ethoxy-6-((2,4,6-trifluorophenyl)amino)cyclohexa-2,5-diene-1,4-dione 17 were the most potent, with a minimum inhibitory concentration value of 15.6 mug/mL against test-culture M. luteum and S. aureus, respectively. Furthermore, in this work, a catalase activity of benzo-and naphthoquinone derivatives was examined for the first time. The catalase activity of benzo-and naphthoquinone derivatives was determined, showing that compound 3g had significant inhibition activity for catalase enzyme.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H4745N – PubChem

 

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N-(substituted-aminoalkyl)-2-oxo-1-pyrrolidineacetamides which are useful as pharmacological agents, especially cognition activators, are disclosed. They can be produced by reacting a 2-oxo-1-pyrrolidineacetate ester with an appropriate amine.

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Piperidine – Wikipedia,
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Substituted 7H-pyrido[4,3-c]carbazoles with potent anti-HIV activity

Several substituted 7H-pyrido[4,3-c]carbazoles were synthesized from the natural product mukonal and tested for inhibition of HIV replication in H9 lymphocytes. 5-Methoxy-7-methyl-7H-pyrido[4,3-c]carbazole (7) had an EC50 value of 0.0054 mug/mL and the highest therapeutic index (TI = 503) in the series.

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Piperidine – Wikipedia,
Piperidine | C5H4381N – PubChem

 

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HClO4-SiO2 as a new, highly efficient, inexpensive and reusable catalyst for N-tert-butoxycarbonylation of amines

Perchloric acid adsorbed on silica-gel (HClO4-SiO2) was found to be a new, highly efficient, inexpensive and reusable catalyst for chemoselective N-tert-butoxycarbonylation of amines at room temperature and under solvent-free conditions. The Royal Society of Chemistry 2006.

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Reference£º
Piperidine – Wikipedia,
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