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The cyclopenta[b]indole motif is present in several natural and synthetic biologically active compounds, being directly responsible for the biological effects some of them present. We described herein a three step sequence for the synthesis of cyclopenta[b]indoles with a great structural diversity. The method is based on an oxidative Michael addition of suitable indoles on the double bond of Morita-Baylis-Hillman adducts mediated by a hypervalent iodine reagent (IBX) to form beta-ketoesters, which were chemoselectively reduced with NaBH4 in THF to give the corresponding beta-hydroxy-esters. The diastereoisomeric mixture was then treated with a catalytic amount of triflic acid (20 mol %) to give cyclopenta[b]indoles with overall yields ranging from 8 to 73% (for 2 steps). The acid-catalyzed cyclization step gave the required heterocycles, via an intramolecular Friedel-Crafts reaction, with high diastereoselectivity, where only the trans product was observed. A mechanistic study monitored by ESI-(+)-MS was also conducted to collect evidence about the mechanism of this reaction. The new molecules herein synthesized were also evaluated against a panel of human cancer cells demonstrating a promising antitumoral profile.

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Reference:
Thiazole | C3H4236NS – PubChem,
Thiazole | chemical compound | Britannica

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Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.

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Thiazole | C3H4377NS – PubChem,
Thiazole | chemical compound | Britannica

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.10200-59-6, Name is 2-Thiazolecarboxaldehyde, molecular formula is C4H3NOS. In a Article,once mentioned of 10200-59-6, Formula: C4H3NOS

The dimeric motif is the smallest unit for two interacting spin centers allowing for systematic investigations of cooperative interactions. As spin transition compounds, dinuclear complexes are of particular interest, since they potentially reveal a two-step spin crossover (SCO), switching between the high spin-high spin [HS-HS], the high spin-low spin [HS-LS], and the low spin-low spin [LS-LS] states. Herein, we report the synthesis and characterization of six dinuclear iron(II) complexes [FeII2(mu2-L1)2](BF4)4 (C1), [FeII2(mu2-L1)2](ClO4)4 (C2), [FeII2(mu2-L1)2](F3CSO3)4 (C3), [FeII2(mu2-L2)2](BF4)4 (C4), [FeII2(mu2-L2)2](BF4)4 (C5), and [FeII2(mu2-L2)2](BF4)4 (C6), based on the 1,3,4-thiadiazole bridging motif. The two novel bis-tridentate ligands (L1 = 2,5-bis{[(1H-imidazol-2-ylmethyl)-amino]-methyl}-1,3,4-thiadiazole and L2 = 2,5-bis{[(thiazol-2-ylmethyl)-amino]-methyl}-1,3,4-thiadiazole) were employed in the presence of iron(II) salts with the different counterions. Upon varying ligands and counterions, we were able to change the magnetic properties of the complexes from a temperature-independent [HS-HS] spin state over a one-step spin transition toward a two-step SCO. When cooled slowly from room temperature, the two-step SCO goes along with two distinct phase transitions, and in the intermediate mixed [HS-LS] state distinct HS/LS pairs can be identified unambiguously. In contrast, rapid cooling precludes a crystallographically observable phase transition. For the mixed [HS-LS] state Moessbauer spectroscopy confirms a statistical (random) orientation of adjacent [HS-LS]·[HS-LS]·[HS-LS] chains.

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Reference:
Thiazole | C3H4231NS – PubChem,
Thiazole | chemical compound | Britannica

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(Figure Presented) The amyloid precursor protein (APP) plays a central role in Alzheimer’s disease (AD). Preventing deregulated APP processing by inhibiting amyloidogenic processing of carboxy-terminal fragments (APP-CTFs), and reducing the toxic effect of amyloid beta (Abeta) peptides remain an effective therapeutic strategy. We report the design of piperazine-containing compounds derived from chloroquine structure and evaluation of their effects on APP metabolism and ability to modulate the processing of APP-CTF and the production of Abeta peptide. Compounds which retained alkaline properties and high affinity for acidic cell compartments were the most effective. The present study demonstrates that (1) the amino side chain of chloroquine can be efficiently substituted by a bis(alkylamino)piperazine chain, (2) the quinoline nucleus can be replaced by a benzyl or a benzimidazole moiety, and (3) pharmacomodulation of the chemical structure allows the redirection of APP metabolism toward a decrease of Abeta peptide release, and increased stability of APP-CTFs and amyloid intracellular fragment. Moreover, the benzimidazole compound 29 increases APP-CTFs in vivo and shows promising activity by the oral route. Together, this family of compounds retains a lysosomotropic activity which inhibits lysosome-related Abeta production, and is likely to be beneficial for therapeutic applications in AD.

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Reference:
Thiazole | C3H4504NS – PubChem,
Thiazole | chemical compound | Britannica

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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. 10200-59-6, Name is 2-Thiazolecarboxaldehyde, molecular formula is C4H3NOS. In a Article,once mentioned of 10200-59-6, Recommanded Product: 2-Thiazolecarboxaldehyde

Optimization of a series of R132H IDH1 inhibitors from a high throughput screen led to the first potent molecules that show robust tumor 2-HG inhibition in a xenograft model. Compound 35 shows good potency in the U87 R132H cell based assay and ?90% tumor 2-HG inhibition in the corresponding mouse xenograft model following BID dosing. The magnitude and duration of tumor 2-HG inhibition correlates with free plasma concentration.

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Reference:
Thiazole | C3H4291NS – PubChem,
Thiazole | chemical compound | Britannica

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“Ion fishing”: Protonated intermediates in the catalytic cycle of the Baylis-Hillman reaction between an activated alkene and an electrophile have been intercepted and characterized by electrospray ionization tandem mass spectrometry. This approach provides direct evidence for the currently accepted mechanism (see scheme).

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Reference:
Thiazole | C3H4512NS – PubChem,
Thiazole | chemical compound | Britannica

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Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 10200-59-6, C4H3NOS. A document type is Patent, introducing its new discovery., Recommanded Product: 2-Thiazolecarboxaldehyde

It is intended to provide a novel compound having an excellent agonism to PPARs a/? and desirable properties as a drug. An agonist to peroxisome proliferator-activated receptors a/? which is represented by the general formula (I) (wherein Q represents an optionally substituted benzene ring or pyridine ring; R1 and R2 represent each an optionally substituted phenyl group or a 5- to 6-membered aromatic heterocycle group; X, Y and Z independently represent each C, O, S or N; R3 to R9 represent each a hydrogen atom, a lower alkyl group, etc.; and n is an integer of from 0 to 3.Lambdaa presente invention porte sur un nouveau compose presentant d”excellentes proprietes agonistes des PPAR a/? et des proprietes interessantes en tant que medicament. Un agoniste des recepteurs actives par les proliferateurs des peroxysomes a/? de formule generale (I) (ou Q represente un cycle benzenique ou pyridinique eventuellement substitue ; R1 et R2 representent chacun un groupement phenyle eventuellement substitue ou un groupement heterocyclique aromatique a 5 ou 6 chainons ; X, Y et Z representent chacun independamment C, O, S ou N ; R3 a R9 representent chacun un atome d”hydrogene, un groupement alkyle court, etc. ; et n represente un entier compris entre 0 et 3 inclus.

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Reference:
Thiazole | C3H4325NS – PubChem,
Thiazole | chemical compound | Britannica

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Due largely to the emergence of multi-drug-resistant HIV strains, the development of new HIV protease inhibitors remains a high priority for the pharmaceutical industry. Toward this end, we previously identified a 4-hydroxy-5,6-dihydropyrone lead compound (CI-1029, 1) which possesses excellent activity against the protease enzyme, good antiviral efficacy in cellular assays, and promising bioavailability in several animal species. The search for a suitable back-up candidate centered on the replacement of the aniline moiety at C-6 with an appropriately substituted heterocyle. In general, this series of heterocyclic inhibitors displayed good activity (in both enzymatic and cellular tests) and low cellular toxicity; furthermore, several analogues exhibited improved pharmacokinetic parameters in animal models. The compound with the best combination of high potency, low toxicity, and favorable bioavailabilty was (S)-3-(2-tertbutyl-4-hydroxymethyl-5-methyl-phenylsulfanyl)-4-hydroxy-6- isopropyl-6-(2-thiophen-3-yl-ethyl)-5,6-dihydro-pyran-2-one (13-(S)). This thiophene derivative also exhibited excellent antiviral efficacy against mutant HIV protease and resistant HIV strains. For these reasons, compound 13-(S) was chosen for further preclinical evaluation.

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Thiazole | C3H4361NS – PubChem,
Thiazole | chemical compound | Britannica

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A series of 7-chloro-2,3-dihydro-2-[1-(pyridinyi)alkyl]-pyridazino[4,5-b] quinoline-1,4,10(5H)-triones were synthesized and found to have potent activity at the glycine site of the NMDA receptor. In some cases, these compounds possessed poor aqueous solubility that may have contributed to poor rat oral bioavailability. Subsequently, compounds have been identified with improved aqueous solubility and oral bioavailability. Several of these compounds were examined in a rat chronic constrictive injury (CCI) model of neuropathic pain and found to have potent activity when dosed orally.

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Thiazole | C3H4446NS – PubChem,
Thiazole | chemical compound | Britannica

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A systematically generated series of hydrazones were analyzed as potential inhibitors of anthrax lethal factor. The hydrazones were screened using one UV-based and two fluorescence-based in vitro assays. The study identified several inhibitors with IC50 values in the micromolar range, and importantly, significant differences in the types of inhibition were observed with the different assays.

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Reference:
Thiazole | C3H4432NS – PubChem,
Thiazole | chemical compound | Britannica