Tag: 100-200

Cinnamoyl amide type chiral P,olefin ligands for Pd-catalyzed reactions was written by Mino, Takashi;Fujisawa, Yohei;Yoshida, Shizuki;Hirama, Mitsuru;Akiyama, Takumu;Saito, Ryo;Yoshida, Yasushi;Kasashima, Yoshio;Sakamoto, Masami. And the article was included in Organic & Biomolecular Chemistry in 2021.Electric Literature of C8H6N2O2 This article mentions the following:

Cinnamoyl amide type chiral P,olefin ligands are synthesized. Authors successfully obtained separable diastereomers of I with axial chirality and demonstrated Pd-catalyzed asym. allylic substitution reactions of indoles using compound I as a chiral ligand with high enantioselectivities (up to 98% ee). In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Electric Literature of C8H6N2O2).

6-Nitro-1H-indole (cas: 4769-96-4) 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. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Electric Literature of C8H6N2O2

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

Induction of Apoptosis in SKOV3 and DNA Binding by Cobalt(III) Polypyridyl Complexes was written by Ravi, Ch.;Vuradi, Ravi Kumar;Avudoddi, Srishailam;Ramchander, M.;Satyanarayana, S.. And the article was included in Russian Journal of Bioorganic Chemistry in 2019.Product Details of 827-01-0 This article mentions the following:

Abstract: Three new Co(III) polypyridyl complexes [Co(phen)₂CIIP]³⁺ {CIIP = 2-(5-chloro-3a,H-isoindol-3-yl)-1H-imidazo[4,5-f][1,10]phenantholine} (phen = 1,10 phenanthroline), [Co(bpy)₂CIIP]³⁺ (bpy = 2,2′-bipyridine), and [Co(dmb)₂CIIP]³⁺ (dmb = 4,4′-dimethyl-2,2′-bipyridine) were synthesized and characterized by different spectral methods. The complexes interact with DNA in an intercalation mode as confirmed by spectroscopic titration and viscosity measurements. All three complexes cleaved the pBR322 DNA in photoactivated cleavage studies and exhibited good antimicrobial activity. Anticancer activity of these Co(III) complexes was evaluated on the SKOV3 cell line. Cytotoxicity by MTT assay showed growth inhibition in dose dependent manner. Cell cycle anal. by flow cytometry data showed increase in Sub G1 population. Annexin V FITC/PI staining confirmed that these complexes caused cell death by the induction of apoptosis. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Product Details of 827-01-0).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Product Details of 827-01-0

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

Design of Helicobacter pylori glutamate racemase inhibitors as selective antibacterial agents: A novel pro-drug approach to increase exposure was written by Basarab, Gregory S.;Hill, Pamela J.;Rastagar, Abdullah;Webborn, Peter J. H.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.Quality Control of 5-Chloroindole-3-carboxaldehyde This article mentions the following:

High-throughput screening uncovered a pyrazolopyrimidinedione hit as a selective, low micromolar inhibitor of Helicobacter pylori glutamate racemase (MurI). Variation of the substituents around the scaffold led to low nanomolar inhibitors and improved antibacterial activity. The challenge in this program was to translate excellent enzyme inhibition into potent antibacterial activity and pharmacokinetics suitable for oral therapy. Compounds were profiled for MurI inhibition, activity against H. pylori, microsomal stability, and pharmacokinetics in mice. Iterative cycles of analog synthesis and biol. testing led to compounds with substituents optimized for both low MICs (鈮? 渭g/mL) and good microsomal stability. In order to achieve high bioavailability, a novel pro-drug approach was implemented wherein a solubilizing sulfoxide moiety is oxidized in vivo to a sulfone. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Quality Control of 5-Chloroindole-3-carboxaldehyde).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Quality Control of 5-Chloroindole-3-carboxaldehyde

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

Platinum(II)-catalyzed dehydrative C3-benzylation of electron-deficient indoles with benzyl alcohols was written by Hikawa, Hidemasa;Matsuura, Yuuki;Kikkawa, Shoko;Azumaya, Isao. And the article was included in Organic Chemistry Frontiers in 2019.Related Products of 4769-96-4 This article mentions the following:

A synthetic strategy for the water-promoted direct dehydrative coupling of indoles I (R = H, Me; R¹ = 6-NO₂, 7-COOH, 5-CN, etc.; R² = H, COOH, phenyl) with benzyl alcs. ArC(OH)(R³)(R⁴) (Ar = C₆H₅, 4-MeOC₆H₄, 3-F₃CC₆H₄, CH=CHC₆H₅, etc.; R³ = Ph, 4-chlorophenyl, Me, etc.; R⁴ = H, Ph) catalyzed by PtCl₂(PhCN)₂ in 1,2-dichloroethane has been developed. Water mols. significantly accelerate C-C bond formation to construct 3-benzylindoles II, whereas the reaction proceeds slowly under anhydrous conditions. Comparative rate plots for reactions in the presence of H₂O and D₂O show a kinetic solvent isotope effect (KSIE) of 1.5. A Hammett study of the dehydrative reaction of para-substituted benzhydrols shows neg. 蟻 values, indicating a build-up of cationic charge during the rate-determining sp³ C-O bond cleavage step. This catalytic system can be used on the gram scale with simplified product isolation and catalysis is performed using 1 mol% of a Pt(II) catalyst with an addnl. mol. of water. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Related Products of 4769-96-4).

6-Nitro-1H-indole (cas: 4769-96-4) 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. 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.Related Products of 4769-96-4

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

Synthesis, molecular docking and enzyme inhibitory approaches of some new chalcone-engrafted pyrazoles as potential antialzheimer, antidiabetic and antioxidant agents was written by Islam, Mohammad Shahidul;Al-Majid, Abdullah Mohammed;Sholkamy, Essam Nageh;Yousuf, Sammer;Ayaz, Muhammad;Nawaz, Asif;Wadood, Abdul;Rehman, Ashfaq Ur;Verma, Ved Prakash;Bari, Ahmed;Haukka, Matti;Soliman, Saied M.;Barakat, Assem. And the article was included in Journal of Molecular Structure in 2022.SDS of cas: 827-01-0 This article mentions the following:

A series of pyrazole-based chalcones I (R = Ph, 3-MeC₆H₄, 2-benzothienyl, 3-indolyl, 5-chloro-3-methyl-1-phenylpyrazol-4-yl, etc.) was designed and constructed in two steps from readily available acetylacetone, phenylhydrazine and DMF-DMA as starting materials. The synthesized chalcone analogs were screened for in vitro anti-acetylcholinesterase potential, antidiabetic potential against 伪-glucosidase and 伪-amylase, and antioxidant potentials against DPPH free radicals. The compounds I (R = ferrocenyl, Ph, 1-naphthyl, 3-BrC₆H₄, 3-O₂NC₆H₄) showed strongest acetylcholine esterase inhibition (AChEI) with IC₅₀ values of 5 卤 1.16渭g/mL, 8 卤 0.14渭g/mL, 8 卤 0.57渭g/mL, 10 卤 1.73渭g/mL and 10 卤 0.60渭g/mL, resp. The highest inhibition against 伪-glucosidase was demonstrated by compounds I (R = 4-ClC₆H₄, 3-O₂NC₆H₄, 3-FC₆H₄, 4-MeOC₆H₄, 3-MeC₆H₄, Ph) with IC₅₀ values of 4 卤 0.14, 6 卤 0.43, 8 卤 0.43, 10 卤 0.11, 11 卤 0.28 and 12 卤 0.57渭g/mL, resp., whereas, the compounds I (R = 5-bromo-3-indolyl, benzothiophen-2-yl, 1-methyl-3-indolyl, 5-chloro-3-indolyl, 5-chloro-3-methyl-1-phenylpyrazol-4-yl) showed prominent 伪-amylase inhibition with IC₅₀ values of 20 卤 1.15渭g/mL, 30 卤 0.60渭g/mL, 40 卤 0.72渭g/mL, 40 卤 0.50渭g/mL, and 60 卤 2.19渭g/mL, resp.. The highest anti-oxidant potential against DPPH free radicals was demonstrated by compounds I (R = 1-methyl-3-indolyl, 3-indolyl, 5-chloro-3-indolyl) with IC₅₀ values of 160 卤 5.77, 260 卤 4.63, and 360 卤 4.04渭g/mL, resp. Mol. docking was used to study their interaction with the active site of enzymes. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0SDS of cas: 827-01-0).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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 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). SDS of cas: 827-01-0

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

Synthesis of Pyranocyclopentaindolines Representing the Western Sections of Janthitrem B, JBIR-137, and Shearinine G was written by Fresia, Marvin;Lindel, Thomas. And the article was included in European Journal of Organic Chemistry in 2022.Name: 6-Nitro-1H-indole This article mentions the following:

The synthesis of the ABCD tetracyclic partial structures of the fungal indole diterpenes janthitrem B, JBIR-137, and shearinine G is reported. The route starts from 5-formylated indoline that is coupled to a dihydropyran moiety, followed by Prins cyclization. A diene was obtained that was oxygenated in a divergent manner. The hydroxylated tetracyclic western half of janthitrem B was obtained in eight steps and 10% overall yield. We also share our experience with alternative approaches passing via alkynylated precursors. This includes the gold-catalyzed cycloisomerization of a 6-ethynyl-5-prenylindoline. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Name: 6-Nitro-1H-indole).

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Name: 6-Nitro-1H-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

Flexible Versus Rigid G-Quadruplex DNA Ligands: Synthesis of Two Series of Bis-indole Derivatives and Comparison of Their Interactions with G-Quadruplex DNA was written by Prasad, Bagineni;Jamroskovic, Jan;Bhowmik, Sudipta;Kumar, Rajendra;Romell, Tajanena;Sabouri, Nasim;Chorell, Erik. And the article was included in Chemistry – A European Journal in 2018.Computed Properties of C8H6N2O2 This article mentions the following:

This work centered around how different design features of small mols. were affected the interactions with G4 DNA structures, exemplified by the development of synthetic methods to bis-indole scaffolds. The synthesized series of bis-indole scaffolds were structurally very similar but differ greatly in the flexibility of their core structures. The flexibility of the mols. proved to be an advantage compared to locking the compounds in the presumed bioactive G4 conformation. The flexible derivatives demonstrated similar or even improved G4 binding and stabilization in several orthogonal assays even though their entropic penalty of binding was higher. In addition, mol. dynamics simulations with the c-MYC G4 structure showed that the flexible compounds adapted better to the surrounding. This was reflected by an increased number of both stacking and polar interactions with both the residues in the G4 DNA structure and the DNA residues just upstream of the G4 structure. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Computed Properties of C8H6N2O2).

6-Nitro-1H-indole (cas: 4769-96-4) 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Computed Properties of C8H6N2O2

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

Synthesis and SARs of indole-based 伪-amino acids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors was written by Han, Xin;Wu, Haoming;Wang, Wei;Dong, Chune;Tien, Po;Wu, Shuwen;Zhou, Hai-Bing. And the article was included in Organic & Biomolecular Chemistry in 2014.Application of 4769-96-4 This article mentions the following:

A series of non-nucleoside reverse transcriptase inhibitors derived from indole-based 伪-amino acids were designed and synthesized. Their inhibitory activities were detected by a TZM-bl cell assay on HIV virus type HIV-1_IIIB. The comprehensive understanding of the SAR was obtained by utilizing the variation of the substituents of the indole-based 伪-amino acids. From the screened compounds, the novel inhibitors (I) (R¹ = 5-Cl and 6-Br) were identified to be highly potent candidates with EC₅₀ values of 0.060 渭M and 0.045 渭M resp. (CC₅₀ values of 109.545 渭M and 49.295 渭M and SI values of 1825.8 and 1095.4). In most cases, the variation of substituents at different positions had a significant effect on the potency of activities. The results also indicate that the indole-based 伪-amino acids as efficient NNRTIs displayed comparable anti-HIV-1 activities to the reference drug NVP. We hope the identification of these indole-based amino acids as efficient NNRTIs of RT could stimulate researchers to develop more diversified anti-HIV drugs. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Application of 4769-96-4).

6-Nitro-1H-indole (cas: 4769-96-4) 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Application of 4769-96-4

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

Synthesis of Pyrido[2,3-b]indole Derivatives via Rhodium-Catalyzed Cyclization of Indoles and 1-Sulfonyl-1,2,3-triazoles was written by Duan, Shengguo;An, Yuehui;Xue, Bing;Chen, Yidian;Zhang, Wan;Xu, Ze-Feng;Li, Chuan-Ying. And the article was included in Advanced Synthesis & Catalysis in 2020.Formula: C9H6ClNO This article mentions the following:

Acyloxy-substituted 伪,尾-unsaturated imines generated in-situ from triazoles acts as aza-[4C] synthons and be trapped by indoles in a stepwise [4 + 2] cycloaddition reaction, thus providing rapid access to valuable pyrido[2,3-b]indoles in high yields. Attractive features of this reaction system included operational simplicity, readily available substrates, construction of sterically demanding quaternary centers and convenient derivatization using triflate. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Formula: C9H6ClNO).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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.Formula: C9H6ClNO

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