Shao, Changdong et al. published their research in Organic Letters in 2015 | CAS: 1016-47-3

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Formula: C12H14N2O

Palladium-Catalyzed C-H Ethoxycarbonyldifluoromethylation of Electron-Rich Heteroarenes was written by Shao, Changdong;Shi, Guangfa;Zhang, Yanghui;Pan, Shulei;Guan, Xiaohong. And the article was included in Organic Letters in 2015.Formula: C12H14N2O This article mentions the following:

The first Pd-catalyzed C-H ethoxycarbonyldifluoromethylation with BrCF2CO2Et has been developed. The use of a bidentate phosphine ligand (Xantphos) is critical for the reaction to occur. A variety of electron-rich heteroarenes, including indoles, furans, thiophenes, and pyrroles, can be ethoxycarbonyldifluoromethylated in moderate to excellent yields. The reactions take place at the C-H bonds adjacent to the heteroatoms with high regioselectivity. This method provides a new protocol for the introduction of difuoroalkyl groups into electron-rich heteroarenes. In the experiment, the researchers used many compounds, for example, N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3Formula: C12H14N2O).

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Formula: C12H14N2O

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Zi, You et al. published their research in RSC Advances in 2014 | CAS: 1016-47-3

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Safety of N-(2-(1H-Indol-3-yl)ethyl)acetamide

In(OTf)3-catalyzed chemoselective alkylation of tryptamines with 2-oxo-1-pyrrolidine derivatives was written by Zi, You;Chu, Xue-Qiang;Lu, Xin-Mou;Wang, Shun-Yi;Ji, Shun-Jun. And the article was included in RSC Advances in 2014.Safety of N-(2-(1H-Indol-3-yl)ethyl)acetamide This article mentions the following:

The chemoselective alkylation of tryptamine derivatives with 2-oxo-1-pyrrolidine compounds, catalyzed by In(OTf)3, was investigated. A series of 2-alkyl and N-alkyl tryptamine derivatives were synthesized under mild conditions with good total yields (up to 99%) and chemoselectivity (up to 95 : 5). In the experiment, the researchers used many compounds, for example, N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3Safety of N-(2-(1H-Indol-3-yl)ethyl)acetamide).

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Safety of N-(2-(1H-Indol-3-yl)ethyl)acetamide

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Backlund, Peter S. et al. published their research in Journal of Biological Rhythms in 2017 | CAS: 1016-47-3

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide

Daily Rhythm in Plasma N-acetyltryptamine was written by Backlund, Peter S.;Urbanski, Henryk F.;Doll, Mark A.;Hein, David W.;Bozinoski, Marjan;Mason, Christopher E.;Coon, Steven L.;Klein, David C.. And the article was included in Journal of Biological Rhythms in 2017.Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide This article mentions the following:

Normal physiol. undergoes 24-h changes in function that include daily rhythms in circulating hormones, most notably melatonin and cortical steroids. This study focused on N-acetyltryptamine, a little-studied melatonin receptor mixed agonist-antagonist and the likely evolutionary precursor of melatonin. The central issue addressed was whether N-acetyltryptamine is physiol. present in the circulation. N-acetyltryptamine was detected by LC-MS/MS in daytime plasma of 3 different mammals in subnanomolar levels (mean 卤 SEM: rat, 0.29 卤 0.05 nM, n = 5; rhesus macaque, 0.54 卤 0.24 nM, n = 4; human, 0.03 卤 0.01 nM, n = 32). Anal. of 24-h blood collections from rhesus macaques revealed a nocturnal increase in plasma N-acetyltryptamine (p < 0.001), which varied from 2- to 15-fold over daytime levels among the 4 animals studied. Related RNA sequencing studies indicated that the transcript encoding the tryptamine acetylating enzyme arylalkylamine N-acetyltransferase (AANAT) is expressed at similar levels in the rhesus pineal gland and retina, thereby indicating that either tissue could contribute to circulating N-acetyltryptamine. The evidence that N-acetyltryptamine is a physiol. component of mammalian blood and exhibits a daily rhythm, together with known effects as a melatonin receptor mixed agonist-antagonist, shifts the status of N-acetyltryptamine from pharmacol. tool to candidate for a physiol. role. This provides a new opportunity to extend our understanding of 24-h biol. In the experiment, the researchers used many compounds, for example, N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide).

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Jiang, Xi-Ling et al. published their research in Drug Metabolism and Disposition in 2009 | CAS: 20315-68-8

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Category: indole-building-block

Pinoline may be used as a probe for CYP2D6 activity was written by Jiang, Xi-Ling;Shen, Hong-Wu;Yu, Ai-Ming. And the article was included in Drug Metabolism and Disposition in 2009.Category: indole-building-block This article mentions the following:

Pinoline, 6-methoxy-1,2,3,4-tetrahydro-尾-carboline, is a serotonin analog that selectively inhibits the activity of monoamine oxidase-A and shows antidepressant activity. Our previous study using a panel of recombinant cytochrome P 450 (P 450) enzymes suggests that pinoline O-demethylation may be selectively catalyzed by polymorphic CYP2D6. The current study, therefore, aimed to delineate the impact of CYP2D6 status on pinoline metabolism Enzyme kinetic studies using recombinant CYP2D6 allelic isoenzymes revealed that CYP2D6.2 exhibited 5-fold lower enzyme efficiency (Vmax/Km) toward pinoline compared with CYP2D6.1, and CYP2D6.10 did not show any catalytic activity. Inhibition study showed that quinidine (1 渭M) completely blocked pinoline O-demethylase activity in human liver microsomes, whereas other P 450 isoform-selective inhibitors had no or minimal effects. Pinoline O-demethylase activities in 10 human liver microsomes showed significantly strong correlation with bufuralol 1′-hydroxylase activities (R2 = 0.93; p < 0.0001) and CYP2D6 contents (R2 = 0.82; p = 0.005), whereas no appreciable correlations with enzymic activities of other P 450 enzymes were found. Furthermore, we compared pinoline urinary metabolic ratio (pinoline/6-hydroxy-1,2,3,4-tetrahydro-尾-carboline) between CYP2D6-humanized and wild-type control mice after i.p. injection of pinoline (30 mg/kg). Results indicated that the two genotyped mice were clearly distinguished by pinoline metabolic ratio (mean 卤 S.D.), which was much higher in wild-type mice (0.29 卤 0.19, n = 4) than in CYP2D6-humanized transgenic mice (0.0070 卤 0.0048, n = 4). Our findings suggest that pinoline O-demethylation is governed by CYP2D6 status, and pinoline, at a proper concentration or dose, may be a good probe to evaluate CYP2D6 activity. In the experiment, the researchers used many compounds, for example, 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8Category: indole-building-block).

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Category: indole-building-block

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Pedras, M. Soledade C. et al. published their research in Journal of Agricultural and Food Chemistry in 2012 | CAS: 1016-47-3

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Application In Synthesis of N-(2-(1H-Indol-3-yl)ethyl)acetamide

Metabolism and Metabolites of Dithiocarbamates in the Plant Pathogenic Fungus Leptosphaeria maculans was written by Pedras, M. Soledade C.;Sarma-Mamillapalle, Vijay K.. And the article was included in Journal of Agricultural and Food Chemistry in 2012.Application In Synthesis of N-(2-(1H-Indol-3-yl)ethyl)acetamide This article mentions the following:

Synthetic compounds containing a dithiocarbamate group are known to have a variety of biol. effects and applications including antifungal, herbicidal, and insecticidal application. Leptosphaeria maculans is a fungal pathogen of crucifers able to detoxify efficiently the only plant natural product containing a dithiocarbamate group, the phytoalexin brassinin. To evaluate the effects of dithiocarbamates on L. maculans, a number of structurally diverse S-Me dithiocarbamates containing indolyl, biphenyl, and benzimidazolyl moieties were synthesized, and their antifungal activities and metabolism by L. maculans were investigated. All dithiocarbamates were transformed by L. maculans through hydrolysis to the corresponding amines, which were less antifungal than the parent compounds Two dithiocarbonates were shown to be much less antifungal than the corresponding dithiocarbamates. Results of this investigation indicate that S-Me dithiocarbamates are not useful inhibitors of L. maculans and that their rates of transformation by L. maculans did not correlate with the antifungal activity of the particular compound In the experiment, the researchers used many compounds, for example, N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3Application In Synthesis of N-(2-(1H-Indol-3-yl)ethyl)acetamide).

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Application In Synthesis of N-(2-(1H-Indol-3-yl)ethyl)acetamide

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Leino, Markku et al. published their research in Acta Ophthalmologica in 1984 | CAS: 20315-68-8

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application of 20315-68-8

Light microscopic autoradiography of rat retinae after intravitreal injection of [3H]6-methoxy-tetrahydro]尾-carboline was written by Leino, Markku;Markkanen, Seppo;Airaksinen, Mauno M.;Gynther, Jukka;Kari, Ilkka. And the article was included in Acta Ophthalmologica in 1984.Application of 20315-68-8 This article mentions the following:

The autoradiog. retinal distribution of intravitreally injected [3H]6-methoxy-tetrahydro-尾-carboline (6-MeO-THBC) in rats was studied. The synaptic and ganglion cell layers accumulate pronounced radioactivity, as do some intra- and extracellular locations in the inner nuclear layer and the outer segments of the photoreceptors. The pigment epithelium gradually accumulates a very dense band of radioactivity. The relation between 6-MeO-THBC, melatonin and other 5-methoxy-indoles is discussed. In the experiment, the researchers used many compounds, for example, 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8Application of 20315-68-8).

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application of 20315-68-8

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Lee, Jong Seok et al. published their research in Bulletin of the Korean Chemical Society in 2013 | CAS: 1016-47-3

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide

A concise and rapid approach to the marine natural product streptochlorin and its analogs was written by Lee, Jong Seok;Shin, Junho;Lee, Hyi-Seung;Shin, Hee Jae;Lee, Yeon-Ju. And the article was included in Bulletin of the Korean Chemical Society in 2013.Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide This article mentions the following:

The synthesis of the target compounds was achieved by a strategy involving a a van Leusen oxazole synthesis and a Gabriel-Robinson reaction (cyclodehydration). The title compounds thus formed included a streptochlorin analog (I) and related substances [3-(4-chloro-5-oxazolyl)-1H-indole, streptochlorin derivatives and analogs]. The synthesis of the target compounds was achieved using 3-formyl-1H-indole-1-carboxylic acid 1,1-dimethylethyl ester derivatives and 1-[(isocyanomethyl)sulfonyl]-4-methylbenzene (TosMIC) as starting materials. In the experiment, the researchers used many compounds, for example, N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide).

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Quality Control of N-(2-(1H-Indol-3-yl)ethyl)acetamide

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Taylor, Dorothy L. et al. published their research in Journal of Pharmacy and Pharmacology in 1984 | CAS: 20315-68-8

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.HPLC of Formula: 20315-68-8

Effects of 6-methoxytetrahydro-尾-carboline on 5-hydroxytryptamine binding in rat brain was written by Taylor, Dorothy L.;Silverman, Peter B.;Ho, Beng T.. And the article was included in Journal of Pharmacy and Pharmacology in 1984.HPLC of Formula: 20315-68-8 This article mentions the following:

6-Methoxytetraydro--carboline (I) [20315-68-8] competes for 5-HT聽聽[50-67-9] binding sites in rat brain in vitro and in vivo. The 尾-carboline is more active at the type 1, 5-HT, than the type 2, spiperone, receptors in vitro. Following injection into rats, I decreases 5-HT but not spiperone binding to the brain cortex. The ineffectiveness of I on spiperone binding in vivo corresponds with the results obtained in vitro. Thus, the effect of I on central 5-HT binding may be a significant aspect of its 5-hydroxytryptaminergic activity. In the experiment, the researchers used many compounds, for example, 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8HPLC of Formula: 20315-68-8).

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.HPLC of Formula: 20315-68-8

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wang, Wei et al. published their research in Anhui Nongye Kexue in 2012 | CAS: 1016-47-3

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Synthetic Route of C12H14N2O

Study on secondary metabolite of Trachelospermum jasminoides endophyte Myrothecium roridum (IFB-E009) was written by Wang, Wei;Jiang, Rong. And the article was included in Anhui Nongye Kexue in 2012.Synthetic Route of C12H14N2O This article mentions the following:

Eight compounds were isolated and identified from liquid fermentation products of Myrothecium roridum (IFB-E009) in Trachelospermum jasminoides, 1-4 were trichothecenes compounds, 5-6 were amides compounds, 7 was cyclic peptide, and 8 was uracil. As indicated by activity test, compound 1,4 showed activities to the human colon cancer cells SW1116. IC50 were 25.68 and 38.93 渭mol/L, while the IC50 of adriamycin was 5.31 渭mol. The study would provide theory and practice basis for the development and utilization of endophytes in pharmaceutical plants. In the experiment, the researchers used many compounds, for example, N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3Synthetic Route of C12H14N2O).

N-(2-(1H-Indol-3-yl)ethyl)acetamide (cas: 1016-47-3) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Synthetic Route of C12H14N2O

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Darwish, Khaled M. et al. published their research in Journal of Molecular Structure in 2022 | CAS: 20315-68-8

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Application In Synthesis of 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole

Discovery of tetrahydro-尾-carboline- and indole-based derivatives as promising phosphodiesterase-4 inhibitors: Synthesis, biological evaluation, and molecular modeling studies was written by Darwish, Khaled M.;Abdelwaly, Ahmad;Atta, Asmaa M.;Helal, Mohamed A.. And the article was included in Journal of Molecular Structure in 2022.Application In Synthesis of 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole This article mentions the following:

Phosphodiesterase-4 (PDE4) is responsible for the selective degradation of the 3′-cyclic phosphate bonds of cAMP. A collection of twenty-three diverse 1,2,3,4-tertahydro-尾-carboline- and indole-based analogs were synthesized and assessed for their inhibitory activity against human PDE4. The compounds were prepared using straightforward procedures and characterized using 1H- and 13C NMR, IR, and mass spectroscopy as well as elemental anal. Fifteen of the prepared compounds exhibited significant inhibitory activity with IC50 values in the lower micromolar to upper nanomolar ranges. The most active compounds also showed good selectivity for PDE4 over the related enzyme family member, PDE5, with either insignificant or null% inhibition of the latter enzyme. The indole-based compounds, 21b (I) and 21c (II), showed the most pronounced PDE4 inhibition with IC50 values of 754 and 664 nM, resp. The PDE4B active site comprises both hydrophobic and solvent-filled pockets. The hydrophobic pocket (Q) includes the invariant purine-selective Gln443 which is critical for cAMP. Below this Gln443 lies Phe446 which acts as a hydrophobic P-clamp stabilizing the ligand aromatic ring system. Mol. docking investigation showed preferential anchoring of the active compounds within the PDE4 active site through interactions between the indole nitrogens and the dimethoxy Ph groups with key residues. Overall, the prepared compounds are novel and simple mols. with good potential for future optimization. Showing satisfactory predicted ADME/safety and drug-likeness properties, compound 21c is considered a promising lead for further optimization towards clin. investigation against inflammatory, auto-immune diseases, or certain types of cancer. In the experiment, the researchers used many compounds, for example, 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8Application In Synthesis of 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole).

6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole (cas: 20315-68-8) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Application In Synthesis of 6-Methoxy-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles