Day: March 30, 2022

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Sulfide analogues of flupirtine and retigabine with nanomolar KV7.2/KV7.3 channel opening activity, published in 2019, which mentions a compound: 4360-63-8, Name is 2-Bromomethyl-1,3-dioxolane, Molecular C4H7BrO2, Synthetic Route of C4H7BrO2.

The potassium channel openers flupirtine and retigabine have proven to be valuable analgesics or antiepileptics. Their recent withdrawal due to occasional hepatotoxicity and tissue discoloration, resp., leaves a therapeutic niche unfilled. Metabolic oxidation of both drugs gives rise to the formation of electrophilic quinones. These elusive, highly reactive metabolites may induce liver injury in the case of flupirtine and blue tissue discoloration after prolonged intake of retigabine. We examined which structural features can be altered to avoid the detrimental oxidation of the aromatic ring and shift oxidation toward the formation of more benign metabolites. Structure-activity relationship studies were performed to evaluate the KV7.2/3 channel opening activity of 45 derivatives Sulfide analogs were identified that are devoid of the risk of quinone formation, but possess potent KV7.2/3 opening activity. For example, flupirtine analog 3-(3,5-difluorophenyl)-N-(6-(isobutylthio)-2-(pyrrolidin-1-yl)pyridin-3-yl)propanamide (48) has 100-fold enhanced activity (EC50=1.4 nM), a vastly improved toxicity/activity ratio, and the same efficacy as retigabine in vitro.

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Arbuzov, B. A.; Zhitinkina, A. K.; Vizel, A. O.; Ivanova, E. F.; Ivanovskaya, K. M.; Giniyatullin, R. S. published the article 《Conversion of diphenylmethane diisocyanate to poly(carbodiimide) during catalysis by phospholene derivatives》. Keywords: polymerization catalyst phospholene derivative; catalyst polymerization phenylmethane isocyanate.They researched the compound: 4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide( cas:707-61-9 ).Recommanded Product: 707-61-9. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:707-61-9) here.

Activity of phospholene derivatives as catalysts for polymerization of diphenylmethane diisocyanate (I) [26447-40-5] increased with increasing electron-donor activity of the substituent on the P atom of the catalyst. Kinetics data showed a dependence of the catalytic activity of phospholene derivatives on their structure, and the highest activity showed oxides of tertiary phosphines, whereas introduction of O and Cl in the ester radical decreased the polymerization rate. A nucleophilic character of the catalyst in the formation of carbodiimide-containing polymers was suggested. The highest polymerization rate of I was observed in the presence of 1-oxo-1-ethyl-3-methyl-2-phospholene (II) [56255-62-0], 1-oxo-1,3-dimethyl-3-phospholene [15450-79-0] and 1-oxo-3-methyl-1-phenyl-2-phospholene [707-61-9] as catalysts. A combined addition of I and 1-oxo-1-ethoxy-3-methyl-3-phospholene [697-31-4] had an additive catalytic effect on polymerization rate of I.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Probing the B- & C-rings of the antimalarial tetrahydro-β-carboline MMV008138 for steric and conformational constraints, published in 2020-11-15, which mentions a compound: 7524-52-9, Name is H-Trp-OMe.HCl, Molecular C12H15ClN2O2, Related Products of 7524-52-9.

The antimalarial candidate MMV008138 (1a, I, (1R,3S) active isomer shown) is of particular interest because its target enzyme (IspD) is absent in human. To achieve higher potency, and to probe for steric demand, a series of analogs of 1a were prepared that featured methyl-substitution of the B- and C-rings, as well as ring-chain transformations. X-ray crystallog., NMR spectroscopy and calculation were used to study the effects of these modifications on the conformation of the C-ring and orientation of the D-ring. Unfortunately, all the B- and C-ring analogs explored lost in vitro antimalarial activity. The possible role of steric effects and conformational changes on target engagement are discussed.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: H-Trp-OMe.HCl( cas:7524-52-9 ) is researched.Computed Properties of C12H15ClN2O2.Brandhofer, Tobias; Stinglhamer, Martin; Derdau, Volker; Mendez, Maria; Poverlein, Christoph; Garcia Mancheno, Olga published the article 《Easy access to drug building-blocks through benzylic C-H functionalization of phenolic ethers by photoredox catalysis》 about this compound( cas:7524-52-9 ) in Chemical Communications (Cambridge, United Kingdom). Keywords: tyrosine methyl ester functionalization alkylation methyl acrylate photoredox catalysis; peptide synthesis alkylation photoredox catalysis reaction mechanism cyclic voltammetry. Let’s learn more about this compound (cas:7524-52-9).

A visible light-mediated photocatalyzed C-C-bond forming method for the benzylic C-H functionalization of phenolether containing synthetic building blocks based on a radical-cation/deprotonation strategy is reported. This method allows the mild, selective generation of benzyl radicals in phenolic complex mols. and drug-like compounds, providing new entries in synthetic and medicinal chem.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Conversion of diphenylmethane diisocyanate to poly(carbodiimide) during catalysis by phospholene derivatives, published in 1975, which mentions a compound: 707-61-9, Name is 4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide, Molecular C11H13OP, SDS of cas: 707-61-9.

Activity of phospholene derivatives as catalysts for polymerization of diphenylmethane diisocyanate (I) [26447-40-5] increased with increasing electron-donor activity of the substituent on the P atom of the catalyst. Kinetics data showed a dependence of the catalytic activity of phospholene derivatives on their structure, and the highest activity showed oxides of tertiary phosphines, whereas introduction of O and Cl in the ester radical decreased the polymerization rate. A nucleophilic character of the catalyst in the formation of carbodiimide-containing polymers was suggested. The highest polymerization rate of I was observed in the presence of 1-oxo-1-ethyl-3-methyl-2-phospholene (II) [56255-62-0], 1-oxo-1,3-dimethyl-3-phospholene [15450-79-0] and 1-oxo-3-methyl-1-phenyl-2-phospholene [707-61-9] as catalysts. A combined addition of I and 1-oxo-1-ethoxy-3-methyl-3-phospholene [697-31-4] had an additive catalytic effect on polymerization rate of I.

If you want to learn more about this compound(4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide)SDS of cas: 707-61-9, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(707-61-9).

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Synthetic Route of C12H15ClN2O2. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Synthesis, characterization and antioxidant activity of chitosan Schiff base derivatives bearing (-)-gossypol. Author is Beyazit, Neslihan; Cakran, Halide Sinem; Cabir, Ali; Akiscan, Yasar; Demetgul, Cahit.

In this work, two new chitosan-Schiff base derivatives (HCS-GSP and LCS-GSP) were synthesized by the condensation reaction of high mol. weight chitosan (HCS) and low mol. weight chitosan (LCS) with (-)-gossypol (GSP), resp. For this purpose, racemic gossypol was isolated from cotton seeds and it was further enantiomerically purified by diastereomeric resolution technique using L-tryptophan Me ester hydrochloride. Then, chitosan polymers were derivatized with (-)-gossypol by the condensation reaction. The isolated and synthesized compounds were characterized by phys. measurements and spectroscopic methods (elemental anal. C,H,N, Uv-vis, FT-IR, 1H&13C NMR and TG/DTG/DTA). The antioxidant activity of high mol. weight chitosan (HCS), low mol. weight chitosan (LCS) and their gossypol derivatives was evaluated as radical scavengers against 1,1-diphenyl-2-picrylhydrazyl radicals (DPPH). The results showed that both of the chitosan-gossypol derivatives (HCS-GSP and LCS-GSP) had a better ability to scavenging DPPH radical (IC50, 12 μg/mL and 16 μg/mL, resp.) than its unmodified chitosan.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Design, synthesis and bio-evaluation of C-1 alkylated tetrahydro-β-carboline derivatives as novel antifungal lead compounds, the main research direction is alkylated tetrahydrocarboline design synthesis Candida antifungal; Antifungals; Apoptosis; Candida glabrata; Pictet-Spengler; SAR; Synergistic effect; β-Carboline.Reference of H-Trp-OMe.HCl.

The field of antifungal agent has become static and development of resistance by the pathogen as well as limited clin. efficacy of marketed drugs demand the constant development of new antifungals. The presence of hydrocarbon chain of specific length linked with various different heterocycles was found to be an important structural feature in various antifungal lead compounds Based on the prominent antimicrobial activity of β-carboline derivatives, a set of C1 alkylated tetrahydro-β-carboline derivatives were proposed to be active against fungi. To validate and confirm the role of suitable alkyl chains linked to a β-carboline scaffold, few related analogs having C1 aryl substituents were also synthesized in one step via classic Pictet-Spengler reaction. The synthesized library was evaluated for its antifungal activity against C. albicans, C. krusei, C. parapsilosis, C. kefyr, C. glabrata, C. tropicalis and C. neoformans. One of the library members I, with n-alkyl chain of eight carbons exhibited potent antifungal activity against C. glabrata and C. kefyr. The lead compound, being selectively toxic also demonstrated prominent synergy enhancing the potency of antifungal drugs up to 10-fold. The time kill kinetic studies confirmed the efficacy of compound I, where the results obtained were comparable to that of Amp B. FE-SEM anal. revealed the increased asymmetry, disintegration and roughness of cell surface which could be because of the possible interaction of compound I at membrane level or interference in cell wall structure. Apoptosis/necrosis detection assay confirmed the significant apoptotic activity in C. glabrata cells after I treatment which was responsible for the rapid killing of C. glabrata cells.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Application In Synthesis of H-Trp-OMe.HCl. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Examination of sulfonamide-based inhibitors of MMP3 using the conditioned media of invasive glioma cells. Author is Poole, Alisha T.; Sitko, Christopher A.; Le, Caitlin; Naus, Christian C.; Hill, Bryan M.; Bushnell, Eric A. C.; Chen, Vincent C..

Glioblastoma multiforme (GBM) is the deadliest and the most common primary malignant brain tumor. The median survival for patients with GBM is around one year due to the nature of glioma cells to diffusely invade that make the complete surgical resection of tumors difficult. Based upon the connexin43 (Cx43) model of glioma migration we have developed a computational framework to evaluate MMP inhibition in materials relevant to GBM. Using the ilomastat Leu-Trp backbone, we have synthesized novel sulfonamides and monitored the performance of these compounds in conditioned media expressing MMP3. From the results discussed herein we demonstrate the performance of sulfonamide based MMPIs included AP-3, AP-6, and AP-7.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called The synthesis, structure-toxicity relationship of cisplatin derivatives for the mechanism research of cisplatin-induced nephrotoxicity, published in 2017-08-01, which mentions a compound: 22353-34-0, Name is 5-Chloropyridin-3-amine, Molecular C5H5ClN2, Formula: C5H5ClN2.

Cisplatin is a widely used antineoplastic drug, while its nephrotoxicity limits the clin. application. Although several mechanisms contributing to nephrotoxicity are reported, the direct protein targets are unclear. Herein the authors reported the synthesis of 29 cisplatin derivatives and the structure-toxicity relation (STR) of these compounds with MTT assay in human renal proximal tubule cells (HK-2) and pig kidney epithelial cells (LLC-PK1). To the best of the authors’ knowledge, this study represented the 1st report regarding the structure-toxicity relation (STR) of cisplatin derivatives The potency of biotin-pyridine conjugated derivative 3 met the requirement for target identification, and the preliminary chem. proteomics results suggested that it is a promising tool for further target identification of cisplatin-induced nephrotoxicity.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Computed Properties of C12H15ClN2O2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Synthesis, characterization and antioxidant activity of chitosan Schiff base derivatives bearing (-)-gossypol.

In this work, two new chitosan-Schiff base derivatives (HCS-GSP and LCS-GSP) were synthesized by the condensation reaction of high mol. weight chitosan (HCS) and low mol. weight chitosan (LCS) with (-)-gossypol (GSP), resp. For this purpose, racemic gossypol was isolated from cotton seeds and it was further enantiomerically purified by diastereomeric resolution technique using L-tryptophan Me ester hydrochloride. Then, chitosan polymers were derivatized with (-)-gossypol by the condensation reaction. The isolated and synthesized compounds were characterized by phys. measurements and spectroscopic methods (elemental anal. C,H,N, Uv-vis, FT-IR, 1H&13C NMR and TG/DTG/DTA). The antioxidant activity of high mol. weight chitosan (HCS), low mol. weight chitosan (LCS) and their gossypol derivatives was evaluated as radical scavengers against 1,1-diphenyl-2-picrylhydrazyl radicals (DPPH). The results showed that both of the chitosan-gossypol derivatives (HCS-GSP and LCS-GSP) had a better ability to scavenging DPPH radical (IC50, 12 μg/mL and 16 μg/mL, resp.) than its unmodified chitosan.

Here is a brief introduction to this compound(7524-52-9)Computed Properties of C12H15ClN2O2, if you want to know about other compounds related to this compound(7524-52-9), you can read my other articles.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem