Simple exploration of 5-Methoxy-3,4-dihydro-2H-pyrrole

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Chemical Compounds

Provided are a series of novel pyridine or pyrimidine derivatives which inhibit CDK9 and may be useful for the treatment of hyperproliferative diseases. In particular the compounds are of use in the treatment of proliferative disease such as cancer including hematological malignancies such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, diffuse large B cell lymphoma, Burkitt’s lymphoma, follicular lymphoma and solid tumors such as breast cancer, lung cancer, neuroblastoma and colon cancer.

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Pyrroline – Wikipedia,
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ALKALOIDS FROM PLATYCAPNOS SPICATA

Two new phenanthrene alkaloids, N-methylsecoglaucine and thalicthuberine N-oxide, were isolated from aerial parts of Platycapnos spicata along with the known alkaloids: dehydronantenine, dehydroglaucine, (+)-glaucine, (+)-nantenine, (+)-domesticine, (+)-thalicmidine, (+)-isodomesticine, (+)-N-methyllaurotetanine, (+)-predicetrine, O-methylateroline, oxonantenine, corunine, pontevedrine, thalicthuberine and protopine.The structures of all the isolated alkaloids were established by spectroscopic methods and, in the case of the new alkaloids, corroborated by syntheses. Key Word Index – Platycapnos spicata; Fumariaceae; isoquinoline alkaloids; phenanthrene alkaloids; N-methylsecoglaucine; thalicthuberine N-oxide.

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Simple exploration of 4-[2-[(3-Ethyl-4-methyl-2-oxo-3-pyrrolin-1-yl)carboxamido]ethyl]benzenesulfonamide

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Method for the Manufacture of Compounds Related to the Class of Substituted Sulphonyl Urea Anti-Diabetics

A process for the formation of high purity sulphonyl urea compounds in high throughput conditions. The sulphonyl urea compounds are preferably the pharmaceutically useful anti-diabetic drugs such as Glimepiride, Gliclazide, Glipizide, Glibenclamide, Glibornuride, Glisoxepide etc, where the purity & economy of the compound are of utmost importance.

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Pyrroline – Wikipedia,
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Final Thoughts on Chemistry for 1-(4-Methoxyphenyl)-1H-pyrrole-2,5-dione

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In vitro antiplasmodial, antiamoebic, and cytotoxic activities of some monomeric isoquinoline alkaloids

Twenty-one alkaloids have been assessed for activities against Plasmodium falciparum (multidrug-resistant strain K1) in vitro; 18 of these are reported for the first time. Two protoberberine alkaloids, dehydrodiscretine and berberine, were found to have antiplasmodial IC50 values less than 1 muM, while seven alkaloids – allocrytopine, columbamine, dehydroocoteine, jatrorrhizine, norcorydine, thalifendine, and ushinsunine – had values between 1 and 10 muM. These results are discussed in the context of structure-activity relationships. Compounds were also assessed for antiamoebic and cytotoxic activities, but none was significantly active except for berberine, which was moderately cytotoxic.

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Pyrroline – Wikipedia,
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The Absolute Best Science Experiment for 4-(2,5-Dioxo-2,5-dihydro-pyrrol-1-yl)-benzoicacid

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Ex vivo anticholinesterase activity of benzoic acid derivatives.

p-Aminobenzoic acid (p-ABA) derivatives were evaluated as acetylcholinesterase inhibitors (AChEIs). Finding a correlation between AChE activity with the partition coefficient (log P) and the highest occupied molecular orbital (HOMO) energy of the compounds.

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Pyrroline – Wikipedia,
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Electrophysiological effects of protopine in cardiac myocytes: Inhibition of multiple cation channel currents

1. Protopine (Pro) from Corydalis tubers has been shown to have multiple actions on cardiovascular system, including anti-arrhythmic, anti-hypertensive and negative inotropic effects. Although it was thought that Pro exerts its actions through blocking Ca2+ currents, the electrophysiological profile of Pro is unclear. The aim of this study is to elucidate the ionic mechanisms of Pro effects in the heart. 2. In single isolated ventricular myocytes from guinea-pig, extracellular application of Pro markedly and reversibly abbreviates action potential duration, and decreases the rate of upstroke (dV/dt)(max), amplitude and overshoot of action potential in a dose-dependent manner. Additionally, it produces a slight, but significant hyperpolarization of the resting membrane potential. 3. Pro at 25, 50 and 100 muM reduces L-type Ca2+ current (I(Ca,L)) amplitude to 89.1, 61.9 and 45.8% of control, respectively, and significantly slows the decay kinetics of I(Ca,L) at higher concentration. The steady state inactivation of I(Ca,L) is shifted negatively by 5.9-7.0 mV (at 50-100 muM Pro), whereas the voltage-dependent activation of I(Ca,L) remains unchanged. In contrast, Pro at 100 muM has no evident effects on T-type Ca2+ current (I(Ca,T)). 4. In the presence of Pro, both the inward rectifier (I(K1)) and delayed rectifier (I(K)) potassium currents are variably inhibited, depending on Pro concentrations. 5. Sodium current (I(Na)), recorded in low [Na+](o) (40 mM) solution, is more potently suppressed by Pro. At 25 muM, Pro significantly attenuated I(Na) at most of the test voltages (-60 ~ + 40 mV, with a 53% reduction at -30 mV. 6. Thus, Pro is not a selective Ca2+ channel antagonist. Rather, it acts as a promiscuous inhibitor of cation channel currents including I(Ca,L), I(K), I(K1) as well as I(Na). These findings may provide some mechanistic explanations for the therapeutic actions of Pro in the heart.

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Pyrroline – Wikipedia,
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Simple exploration of N-Boc-2-pyrroline

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Synthesis of indoles via 6pi-electrocyclic ring closures of trienecarbamates

A new method for the preparation of indoles from readily available alpha-haloenones and alpha-(trialkylstannyl)enecarbamates is described. Following a Stille coupling, trienecarbamate 2 is electronically activated to undergo a facile 6pi-electrocyclic ring closure and subsequent oxidation to afford protected aniline 4. Upon deprotection and reductive amination, acid 5 underwent clean cyclization to N-acetylindole 6 (Ac2O, NEt3, 130 C). This method has been used to construct a variety of substituted indoles that are not easily prepared by conventional indole annelation methods. Copyright

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An aza-enolate alkylation strategy for the synthesis of alpha-alkyl-delta-amino esters and alpha-alkyl valerolactams

Alkylation of the aza-enolate of valerolactim methyl ether with electrophiles affords alpha-alkyl lactims that may be hydrolysed under mild acidic conditions to afford their corresponding alpha-alkyl-delta-amino esters as their hydrochloride salts. Neutralisation of these salts with base results in smooth intramolecular cyclisation to afford their corresponding alpha-alkyl lactams in excellent yield. Georg Thieme Verlag Stuttgart.

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Dual C-H functionalization of N-aryl amines: Synthesis of polycyclic amines via an oxidative povarov approach

Iminium ions generated in situ via copper(I) bromide catalyzed oxidation of N-aryl amines readily undergo [4 + 2] cycloadditions with a range of dienophiles. This method involves the functionalization of both a C(sp 3)-H and a C(sp2)-H bond and enables the rapid construction of polycyclic amines under relatively mild conditions.

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Synthesis and antibacterial activity of new 2,5-diaryl-3-styryl-4H,2,3,3a, 5,6,6a-hexahydropyrrolo[3,4-d]isoxazole-4,6-diones

The synthesis of some biologically interesting pyrrolo-isoxazolidine derivatives has been accomplished by the 1,3-dipolar cycloaddition reaction of substituted open chain conjugated azomethine N-oxides 1 with substituted N-aryl maleimides 2 leading to the formation of new stereoisomeric 2,5-diaryl-3-styryl- 4H,2,3,3a,5,6,6a-hexahydropyrrolo[3,4-d]isoxazole-4,6-dione derivatives 3 in excellent yields. These stereoisomers have been characterized as cis-3A and trans-3B on the basis of their 1H-NMR spectral measurements. The synthesized compounds have been screened for their antibacterial activities and have been found to be active against the bacteria Escherichia coli and Pseudomonas aeruginosa up to a significant extent.

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Pyrroline – Wikipedia,
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