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Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds

Several thiazolyl thiourea derivatives were designed and synthesized as non-nucleoside inhibitors (NNRTI) of HIV-1 reverse transcriptase. Six lead compounds were identified that showed subnanomolar IC50 values for the inhibition of HIV replication, were minimally toxic to human peripheral blood mononuclear cells (PBMC) with CC50 values ranging from 28 to >100 muM, and showed remarkably high selectivity indices ranging from 28,000 to >100,000. The most promising compound was N-[1-(1-furoylmethyl)]-N?-[2-(thiazolyl)]thiourea (compound 6), which showed potency against two NNRTI-resistant HIV-1 isolates (A17 and A17 variant) at nanomolar to low micromolar concentrations, exhibited much greater potency against both wild-type as well as NNRTI-resistant HIV-1 than nevirapine, delavirdine, HI-443, and HI-244, was minimally toxic to PBMC, and had a selectivity index of >100,000. The potency and minimal cytotoxicity of these aromatic/heterocyclic thiourea compounds suggest that they may be potentially useful as anti-AIDS drugs.

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Piperidine – Wikipedia,
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Simple exploration of 4,4′-Bipiperidine dihydrochloride

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Bicyclic fibrinogen antagonists

This invention relates to compounds of the formulae: whereinA1 is O, S, N?R1 or CHR1;A4 is N?R4 or CHR4;R2 is a sidechain containing an acid or ester group;R1, R4 and R5 are substituents such as H, alkyl and aryl alkyl, andR6 is a sidechain containing a nitrogen group; andpharmaceutically acceptable salts thereof,which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.

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Extracurricular laboratory:new discovery of 177-11-7

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SULFONAMIDES AS INHIBITORS OF BCL-2 FAMILY PROTEINS FOR THE TREATMENT OF CANCER

The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of Formula (I) or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyper proliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula (I) and pharmaceutically acceptable salts thereof

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Piperidine – Wikipedia,
Piperidine | C5H7360N – PubChem

 

The Absolute Best Science Experiment for 392331-66-7

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 392331-66-7 is helpful to your research. Electric Literature of 392331-66-7

Electric Literature of 392331-66-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.392331-66-7, Name is 1-Boc-4-(Aminomethyl)-4-hydroxypiperidine, molecular formula is C11H22N2O3. In a Patent£¬once mentioned of 392331-66-7

5-AMINO-QUINOLINE-8-CARBOXAMIDE DERIVATIVES AS 5-HT4 RECEPTOR AGONISTS

The present invention relates to novel quinoline compounds of formula (I), and their pharmaceutically acceptable salts and process for their preparation. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptor agonists.

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New explortion of 4-Piperidinone

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INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

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More research is needed about tert-Butyl 4-(4-amino-1H-pyrazol-1-yl)piperidine-1-carboxylate

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PYRIMIDO-DIAZEPINONE COMPOUNDS AND METHODS OF TREATING DISORDERS

The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1,2,3, or 4, Ackl, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rskl, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

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Piperidine – Wikipedia,
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The important role of 6574-15-8

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Electric Literature of 6574-15-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.6574-15-8, Name is 1-(4-Nitrophenyl)piperidine, molecular formula is C11H14N2O2. In a article£¬once mentioned of 6574-15-8

Aromatic Nucleophilic Substitution of Halobenzenes with Amines under High Pressure

The nucleophilic substitution reactions of aromatic halides having electron-attracting groups on ortho or para position with various primary and secondary amines were accelerated by high pressure to give the corresponding N-substituted anilines in high yields.The bulkiness of amines affects its reactivity to lower the yields of the products.Although the secondary amines are usually less reactive than primary amines, cyclic secondary amines such as morpholine, piperidine, and pyrrolidine were found very reactive. 1,4-Diazabicyclo<2.2.2>octane and quinuclidine gave N-quarternary ammonium halides in high yields in contrast to the low reactivity of acyclic tertiary amines.Dichloro- and trichloro-nitrobenzenes also react with diethylamine, pyrrolidine, and morpholine to give mono-, di-, and trisubstitution products depending upon the amount of amine and the position of nitro group in these chlorides.

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Piperidine – Wikipedia,
Piperidine | C5H15289N – PubChem

 

Brief introduction of 106-52-5

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Electric Literature of 106-52-5, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 106-52-5, Name is 1-Methylpiperidin-4-ol, molecular formula is C6H13NO. In a Article£¬once mentioned of 106-52-5

Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies

Through virtual screening, we identified the lead compound MCL1020, which exhibited modest CHK1 inhibitory activity. Then a series of 5-(pyrimidin-2-ylamino)picolinonitrile derivatives as CHK1 inhibitors were discovered by further rational optimization. One promising molecule, (R)-17, whose potency was one of the best, had an IC50 of 0.4 nM with remarkable selectivity (>4300-fold CHK1 vs. CHK2). Compound (R)-17 effectively inhibited the growth of malignant hematopathy cell lines especially Z-138 (IC50: 0.013 muM) and displayed low affinity for hERG (IC50 > 40 muM). Moreover, (R)-17 significantly suppressed the tumor growth in Z-138 cell inoculated xenograft model (20 mg/kg I.V., TGI = 90.29%) as a single agent with body weight unaffected. Taken together, our data demonstrated compound (R)-17 could be a promising drug candidate for the treatment of hematologic malignancies.

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Brief introduction of 39546-32-2

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Related Products of 39546-32-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.39546-32-2, Name is Piperidine-4-carboxamide, molecular formula is C6H12N2O. In a Patent£¬once mentioned of 39546-32-2

AMINOTHIAZOLE DERIVATIVES AS AGONISTS OF THE THROMBOPOIETIN RECEPTOR

A compound of the formula (I) wherein R1, R2, R3, X, and d are defined as above. The presently disclosed compounds are TPO agonists useful as promoters of thrombopoiesis and megakaryocytopoiesis.

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Top Picks: new discover of 2213-43-6

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NOVEL IMIDAZO[1,2-a]PYRIDINE CANNABINOID RECEPTOR LIGANDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

The present invention relates to novel imidazo[1,2-a]pyridine cannabinoid receptor ligands, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor ligands, and uses thereof for treating diseases, conditions and/or disorders modulate by a cannabinoid receptors (such as pain, neurodegenerative disorders, eating disorders, weight loss or control, obesity and diabetes).

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