Archives for Chemistry Experiments of 20375-65-9

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Structures of cytotoxic bicyclic hexapeptides, RA-XIX, -XX, -XXI, and -XXII, from Rubia cordifolia L.

Novel bicyclic hexapeptides, RA-XIX, -XX, -XXI, and -XXII, were isolated from the roots of Rubia cordifolia L. The structures of RA-XIX and RA-XX were established by semisynthesis from a cycloisodityrosine, derived from previously reported RA-VII, and those of RA-XXI and RA-XXII by chemical correlation with RA-XX and previously reported RA-VIII, respectively. The IC50 values of these new peptides against P-388 leukemia cells were 0.013-0.63 mug/mL.

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Pyridazine | C4H4N2684 – PubChem

 

Discovery of 5-Iodo-2,3-dihydropyridazin-3-one

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Application of 825633-94-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.825633-94-1, Name is 5-Iodo-2,3-dihydropyridazin-3-one, molecular formula is C4H3IN2O. In a Patent£¬once mentioned of 825633-94-1

AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS

MCHR1 antagonists are provided having the following Formula (I): A 1 and A 2 are independently C or N, E is C or N, Q 1 , Q 2 , and Q 3 are independently C or N provided that at least one of Q 1 , Q 2 , and Q 3 is N but not more than one of Q 1 , Q 2 , and Q 3 is N, D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10′ -, -C-C-, or 1,2-cyclopropyl; X is O, S or NR 11, R 1 , R 2 , and R 3 are ,independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -OCF 3 , -OR 12 and -SR 12, G is O, S or -NR 15, D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkylcycloalkoxy or when G is NR 15 , G and D 2 together may optionally form an azetidine, pyrrolidine or piperidine ring; Z 1 and Z 2 are independently hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14′ , -CN, -CONR 14 R 14′ , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14′ , -NR 14 CO 2 R 14′ , -CO 2 R 12 , NR 14 SO 2 R 12 or COR 12 ; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -CN, -CONR 14 R 14′ , SOR 12 , SO 2 R 12 , NR 14 COR 14′ , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10′ , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; R 14 and R 14′ are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14′ together with the N to which they are attached form a ring having 4 to 7 atoms; and R 15 is independently selected from the group consisting of hydrogen and lower alkyl. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety

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Simple exploration of 20744-39-2

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Synthetic Route of 20744-39-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.20744-39-2, Name is Pyridazin-4-amine, molecular formula is C4H5N3. In a Article£¬once mentioned of 20744-39-2

Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation

Human African trypanosomiasis (HAT) is a deadly disease in need of new chemotherapeutics that can cross into the central nervous system. We previously reported the discovery of 2 (NEU-617), a small molecule with activity against T. brucei bloodstream proliferation. Further optimization of 2 to improve the physicochemical properties (LogP, LLE, [1], and MPO score) [2] have led us to twelve sub-micromolar compounds, most importantly the headgroup variants 9i and 9j, and the linker variant 18. Although these 3 compounds had reduced potency compared to 2, they all had improved LogP, LLE and MPO scores. Cross-screening these analogs against other protozoan parasites uncovered 9o with potent activity towards T. brucei, T. cruzi and L. major, while four others compounds (17, 18, 21, 26) showed activity towards P. falciparum D6. This reinforces the effectiveness of lead repurposing for the discovery of new protozoan disease therapeutics.

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Brief introduction of 3-Bromopyridazine

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88491-61-6, Name is 3-Bromopyridazine, belongs to pyridazine compound, is a common compound. SDS of cas: 88491-61-6In an article, once mentioned the new application about 88491-61-6.

BENZOCARBONYL COMPOUNDS

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

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Extended knowledge of 35857-89-7

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35857-89-7, Name is 6-Chloropyridazine-3-carbonitrile, belongs to pyridazine compound, is a common compound. Safety of 6-Chloropyridazine-3-carbonitrileIn an article, once mentioned the new application about 35857-89-7.

Synthesis and biological evaluation of potential acetylcholinesterase inhibitors based on a benzoxazine core

With the purpose of expanding the structural variety of chemical compounds available as pharmacological tools for the treatment of Alzheimer’s disease, we synthesized and evaluated a novel series of indole-benzoxazinones (Family I) and benzoxazine-arylpiperazine derivatives (Family II) for potential human acetylcholinesterase (hAChE) inhibitory properties. The most active compounds 7a and 7d demonstrated effective inhibitory profiles with Ki values of 20.3 ¡À 0.9 muM and 20.2 ¡À 0.9 muM, respectively. Kinetic inhibition assays showed non-competitive inhibition of AChE by the tested compounds. According to our docking studies, the most active compounds from both series (Families I and II) showed a binding mode similar to donepezil and interact with the same residues.

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Can You Really Do Chemisty Experiments About 4,5-Dichloro-3(2H)-pyridazinone

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SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists

In this Letter we report on the advances in our NPBWR1 antagonist program aimed at optimizing the 5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy) pyridazin-3(2H)-one lead molecule previously obtained from a high-throughput screening (HTS)-derived hit. Synthesis and structure-activity relationships (SAR) studies around the 3,5-dimethylphenyl and 4-methoxyphenyl regions resulted in the identification of a novel series of non-peptidic submicromolar NPBWR1 antagonists based on a 5-chloro-4-(4-alkoxyphenoxy)-2-(benzyl)pyridazin-3(2H)- one chemotype. Amongst them, 5-chloro-2-(9H-fluoren-9-yl)-4-(4-methoxyphenoxy) pyridazin-3(2H)-one 9h (CYM50769) inhibited NPW activation of NPBWR1 with a submicromolar IC50, and displayed high selectivity against a broad array of off-targets with pharmaceutical relevance. Our medicinal chemistry study provides innovative non-peptidic selective NPBWR1 antagonists that may enable to clarify the biological role and therapeutic utility of the target receptor in the regulation of feeding behavior, pain, stress, and neuroendocrine function.

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The important role of 3-Methoxypyridazine

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Electric Literature of 19064-65-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19064-65-4, Name is 3-Methoxypyridazine, molecular formula is C5H6N2O. In a Article£¬once mentioned of 19064-65-4

Fossil redox-conditions influence organic matter composition in loess paleosols

The soil memory recorded in paleosols of loess-paleosol sequences is an important contributor to our understanding of past climatic conditions. Molecular proxies based on the organic matter preserved in paleosols form an essential part of this record, but the long-term preservation of SOM is poorly understood, especially for sediment traps and slope profiles. This paper addresses the composition of organic material from the Early Weichselian A-horizons of the Rocourt paleosol, a major paleostratigraphic marker for the Eemian and Early Weichselian in Western Europe. NaOH-extractable organic matter from an exceptionally thick Rocourt profile in the Kesselt Quarry (Belgian Loess Belt) was analyzed by pyrolysis-Gas Chromatography/Mass Spectrometry (pyrolysis-GC/MS) and the results evaluated against paleopedological data. The molecular composition of the organic matter at Kesselt was compared with reference samples from two nearby quarries (including the type locality at Veldwezelt-Hezerwater), and to a sample from the contemporary Nussloch sequence in Germany. The SOM composition found at the four sites indicated a large content of microbial matter and was dominated by?carbohydrates and N compounds, many of which were not reported before from SOM pyrolysates. Differences in the molecular composition between samples, both within profiles and between sites, coincided with differences in landscape position (slope-shoulder-plateau) and fossil redox conditions (surface gleys). Samples form drier and more upland situations contained more burnt material, while samples from slope profiles and surface gleys contained even more microbial material, in particular chitin. Results therefore suggest that the admixture of microbial SOM is considerable in loess-paleosols and that differences in edaphic conditions (in particular slope position and soil moisture) and occurrence of wildfires are important for the long-term preservation of SOM. These should therefore be considered when interpreting biogeochemical proxies.

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Awesome Chemistry Experiments For 6-Chloropyridazine-3-carbonitrile

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, category: pyridazine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 35857-89-7, Name is 6-Chloropyridazine-3-carbonitrile, molecular formula is C5H2ClN3

A concise and efficient synthesis of substituted morpholines

A simple and efficient method has been developed for the synthesis of substituted morpholines by a sequence of coupling, cyclization, and reduction reactions of easily available amino alcohols and alpha-halo acid chlorides. Various mono-, di-, and trisubstituted morpholines, spiro morpholines, and ring-fused morpholines, as well as morpholine homologues, were synthesized in good to excellent yields by a single methodology under similar reaction conditions. The method was also used in a multigram synthesis of (3S)-3-methylmorpholine.

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Extended knowledge of 4-Bromo-1,2-dihydropyridazine-3,6-dione

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 15456-86-7, help many people in the next few years.Computed Properties of C4H3BrN2O2

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Computed Properties of C4H3BrN2O2, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 15456-86-7, name is 4-Bromo-1,2-dihydropyridazine-3,6-dione. In an article£¬Which mentioned a new discovery about 15456-86-7

SUBSTITUTED 1-METHYL-1H-QUINOLIN-2-ONES AND 1-METHYL-1H-1,5-NAPHTHYRIDIN-2-ONES AS ANTIBACTERIALS

Bicyclic nitrogen containing compounds of formula (I) and their use as antibacterials.

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Brief introduction of 1178884-53-1

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INHIBITORS OF BRUTON’S TYROSINE KINASE

This application discloses the Btk inhibitor compounds 6-tert-Butyl-8-fluoro-2-{3- hydroxymethyl-4-[1-methyl-5-(1′-methyl-1′,2′,3′,4′,5′,6′-hexahydro-[3,4′]bipyridinyl-6-ylamino)- 6-oxo-1,6-dihydro-pyridazin-3-yl]-pyridin-2-yl}-2H-phthalazin-1-one, 2-(2-{3-[5-(5-Azetidin-1- ylmethyl-1-methyl-1H-pyrazol-3-ylamino)-1-methyl-6-oxo-1,6-dihydro-pyridazin-3-yl]-2- hydroxymethyl-phenyl}-8-fluoro-1-oxo-1,2-dihydro-isoquinolin-6-yl)-2-methyl-propionitrile, and 6-tert-Butyl-2-[2-hydroxymethyl-3-(5-{5-[(2-methoxy-ethylamino)-methyl]-pyridin-2- ylamino}-6-oxo-1,6-dihydro-pyridin-3-yl)-phenyl]-3,4-dihydro-2H-isoquinolin-1-one, formulations thereof, and methods of treatment of asthma, as described herein.

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