Category: 1716-12-7

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Quality Control of Sodium 4-phenylbutanoate, 1716-12-7, Name is Sodium 4-phenylbutanoate, SMILES is O=C([O-])CCCC1=CC=CC=C1.[Na+], in an article , author is Alsayed, Shahinda S. R., once mentioned of 1716-12-7.

The treacherous nature of tuberculosis (TB) combined with the ubiquitous presence of the drug-resistant (DR) forms pose this disease as a growing public health menace. Therefore, it is imperative to develop new chemotherapeutic agents with a novel mechanism of action to circumvent the cross-resistance problems. The unique architecture of the Mycobacterium tuberculosis (M. tb) outer envelope plays a predominant role in its pathogenesis, contributing to its intrinsic resistance against available therapeutic agents. The mycobacterial membrane protein large 3 (MmpL3), which is a key player in forging the M. tb rigid cell wall, represents an emerging target for TB drug development. Several indole-2-carboxamides were previously identified in our group as potent anti-TB agents that act as inhibitor of MmpL3 transporter protein. Despite their highly potent in vitro activities, the lingering Achilles heel of these indoleamides can be ascribed to their high lipophilicity as well as low water solubility. In this study, we report our attempt to improve the aqueous solubility of these indole-2-carboxamides while maintaining an adequate lipophilicity to allow effective M. tb cell wall penetration. A more polar adamantanol moiety was incorporated into the framework of several indole-2-carboxamides, whereupon the corresponding analogues were tested for their anti-TB activity against drug-sensitive (DS) M. tb H37Rv strain. Three adamantanol derivatives 8i, 8j and 8l showed nearly 2- and 4-fold higher activity (MIC = 1.32 – 2.89 mu M) than ethambutol (MIC = 4.89 mu M). Remarkably, the most potent adamantanol analogue 8j demonstrated high selectivity towards DS and DR M. tb strains over mammalian cells [IC50 (Vero cells) >= 169 mu M], On evincing its lack of cytotoxicity. The top eight active compounds 8b, 8d, 8f, 8i, 8j, 8k, 8l and 10a retained their in vitro potency against DR M. tb strains and were docked into the MmpL3 active site. The most potent adamantanol/adamantane-based indoleamides 8j/8k displayed a two-fold surge in potency against extensively DR (XDR) M. tb strains with MIC values of 0.66 and 0.012 mu M, respectively. The adamantanol-containing indole-2-carboxamides exhibited improved water solubility both in silico and experimentally, relative to the adamantane counterparts. Overall, the observed antimycobacterial and physicochemical profiles support the notion that adamantanol moiety is a suitable replacement to the adamantane scaffold within the series of indole-2-carboxamide-based MmpL3 inhibitors.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 1716-12-7, you can contact me at any time and look forward to more communication. Quality Control of Sodium 4-phenylbutanoate.

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

In an article, author is Qiu, Zhongxuan, once mentioned the application of 1716-12-7, Recommanded Product: Sodium 4-phenylbutanoate, Name is Sodium 4-phenylbutanoate, molecular formula is C10H11NaO2, molecular weight is 186.18, MDL number is MFCD00800247, category is indole-building-block. Now introduce a scientific discovery about this category.

A series of indane-based phosphine-oxazoline ligands with a spirocarbon stereogenic center were examined for palladium-catalyzed asymmetric allylic alkylation of indoles. Under optimized conditions, high yields (up to 98%) and enantioselectivities (up to 98% ee) were obtained with a broad scope of indole derivatives. The ligand was determined to be the most efficient P,N-ligand for this reaction. Moreover, the ligand was also efficient for Pd-catalyzed asymmetric allylic etherification with hard aliphatic alcohols as nucleophiles.

If you are interested in 1716-12-7, you can contact me at any time and look forward to more communication. Recommanded Product: Sodium 4-phenylbutanoate.

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

Reference of 1716-12-7, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 1716-12-7, Name is Sodium 4-phenylbutanoate, SMILES is O=C([O-])CCCC1=CC=CC=C1.[Na+], belongs to indole-building-block compound. In a article, author is Kothandapani, Jagatheeswaran, introduce new discover of the category.

TBHP Mediated Substrate Controlled Oxidative Dearomatization of Indoles to C2/C3-Quaternary Indolinones

Oxidative dearomatization of indoles with 70% aqueous tert-butylhydroperoxide (TBHP) in the absence of any metal salts/organic solvents gave the corresponding C2/C3-quaternary indolinones under open-air reaction conditions. The nature of substituent on the indole nitrogen dictates the type of product formed in these reactions. Free (NH)-indoles gave C2-quaternary indolinone derivatives whilst (NR)-indoles yielded C3-quaternary indolinones as the major product. Moreover, the addition of an excess amount of TBHP also facilitated the one-pot transformation of (NR)-indoles to the corresponding isatin derivatives.

Reference of 1716-12-7, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 1716-12-7.

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

Application of 1716-12-7, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 1716-12-7, Name is Sodium 4-phenylbutanoate, SMILES is O=C([O-])CCCC1=CC=CC=C1.[Na+], belongs to indole-building-block compound. In a article, author is Zhou, Feilong, introduce new discover of the category.

Synthesis of 3,4-diarylsubstituted hexahydro-1H-indoles

Efficient syntheses of 3,4-diarylsubstituted hexahydro-1H-indoles in good yields with excellent diastere-oselectivities were achieved with a two-step protocol comprising an allylic cation mediated nucleophilic addition and an intramolecular cyclization reaction. The N-aryl sulfonyl protecting groups of cyclization products were readily removed to furnish free amines with retention of halogen substitutions and C-C double bonds. (C) 2018 Elsevier Ltd. All rights reserved.

Application of 1716-12-7, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 1716-12-7 is helpful to your research.

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