Tag: M.W=150-200

Shi, Yang; Pan, Bo-Wen; Li, Wen-Chao; Wang, Qing; Wu, Qiong; Pan, Meng; Fu, Hong-Zheng published the artcile< Synthesis and biological evaluation of Isosteviol derivatives as FXa inhibitors>, HPLC of Formula: 19241-24-8, the main research area is isosteviol derivative preparation FXa inhibitor anticoagulant; FXa inhibitors; Isosteviol; Structural modification.

Firstly, a series of Isosteviol derivatives were synthesized and evaluated for FXa inhibitory activity. Among these compounds, the inhibitory activity of three compounds on FXa was better than that of Isosteviol. Secondly, surface plasmon resonance (SPR) assays were performed for selected compounds The three compounds have similar kinetic signatures, and affinity values were at μM level. Thirdly, two compounds displayed moderate-to-high anticoagulation activity and showed similar sensitivity to PT and aPTT. These findings will provide new insight into the exploration of FXa inhibition.

Bioorganic & Medicinal Chemistry Letters published new progress about Anticoagulants. 19241-24-8 belongs to class esters-buliding-blocks, and the molecular formula is C11H13NS, HPLC of Formula: 19241-24-8.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Yuan, Feipeng; Hou, Zhen-Lin; Pramanick, Pranab K.; Yao, Bo published the artcile< Site-selective modification of α-amino acids and oligopeptides via native amine-directed γ-C(sp3)-H arylation>, Application of C8H18ClNO2, the main research area is amino acid functionalization arylation aryl iodide amine directed acylation; peptide coupling functionalization arylation aryl iodide amine solvent effect.

Site-selective modification of chem. and biol. valuable α-amino acids and peptides is of great importance for biochem. study and pharmaceutical development. Few methods based on remote C(sp3)-H functionalization of aliphatic side-chains of peptides has been disclosed in recent years. In this report, we developed a novel approach for γ-C(sp3)-H and γ-/δ-C(sp2)-H arylation of α-amino acids with α-hydrogen by native amine-directed C-H functionalization and further realized the γ-C(sp3)-H arylation of N-terminally unprotected peptides.

Organic Letters published new progress about Acylation. 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Application of C8H18ClNO2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Hughes, Chambers C.; Kauffman, Christopher A.; Jensen, Paul R.; Fenical, William published the artcile< Structures, Reactivities, and Antibiotic Properties of the Marinopyrroles A-F>, Related Products of 252932-48-2, the main research area is antimicrobial antitumor marinopyrrole isolation preparation structure activity.

Cultivation of actinomycete strain CNQ-418, retrieved from a deep ocean sediment sample off the coast of La Jolla, CA, has provided marinopyrroles A-F. Sharing just 98% 16S rRNA gene sequence identity with S. sannurensis, the strain likely represents a new Streptomyces species. The metabolites contain an unusual 1,3′-bipyrrole core decorated with several chlorine and bromine substituents and possess marked antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). The congested N,C-biaryl bond establishes an axis of chirality that, for marinopyrroles A-E, is configurationally stable at room temperature Moreover, the natural products are fashioned strictly in the M-configuration. The Paal-Knorr condensation was adapted for the synthesis of the 1,3′-bipyrrole core. Halogenation of this material with N-bromosuccinimide cleanly furnished the 4,4′,5,5′-tetrahalogenated core that characterizes this class of marine-derived metabolites.

Journal of Organic Chemistry published new progress about Actinobacteria. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Related Products of 252932-48-2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Suzuki, Hitomi; Takeuchi, Toyomi; Mori, Tadashi published the artcile< Ozone-Mediated Nitration of Phenylalkyl Ethers, Phenylacetic Esters, and Related Compounds with Nitrogen Dioxide. The Highest Ortho Substitution Observed in the Electrophilic Nitration of Arenes>, Quality Control of 30095-98-8, the main research area is ozone nitration phenylalkyl ether phenylacetate; aryl ether nitration Kyodai regiochem; regioselective substitution Kyodi nitration phenyl ether; Kyodai nitration phenylalkyl ether benzeneacetate; electrophilic nitration nitrogen dioxide.

By the combined action of ozonized oxygen and nitrogen dioxide (the Kyodai nitration), the title compounds were smoothly nitrated in dichloromethane at subzero degrees with high ortho positional selectivity. Although the conventional nitration of phenylacetic acid and esters mainly produces m- and p-nitro derivatives, the present nitration offers a simple high-yield synthesis of o-nitro derivatives which are important as precursor in organic synthesis. The proportions of the ortho isomer in the nitration products from Me 2-phenylethyl ether and Me phenylacetate were 71 and 88%, resp., the latter value being the highest ortho isomer proportion so far observed in the electrophilic aromatic nitration. The observed high ortho selectivity has been rationalized in terms of radical cation intermediate and six-membered cyclic transition state.

Journal of Organic Chemistry published new progress about Alkyl aryl ethers Role: RCT (Reactant), RACT (Reactant or Reagent). 30095-98-8 belongs to class esters-buliding-blocks, and the molecular formula is C9H9NO4, Quality Control of 30095-98-8.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zhang, Hua; Wang, Zheyuan; Wang, Zirui; Chu, Yunpeng; Wang, Shuncheng; Hui, Xin-Ping published the artcile< Visible-Light-Mediated Formal Carbene Insertion Reaction: Enantioselective Synthesis of 1,4-Dicarbonyl Compounds Containing All-Carbon Quaternary Stereocenter>, HPLC of Formula: 94-02-0, the main research area is dicarbonyl compound preparation enantioselective; diketone diazoester carbene insertion visible light.

Authors developed an efficient visible-light-mediated formal carbene insertion reaction of 1,3-diketones with diazoesters for the construction of enantioenriched 1,4-dicarbonyl compounds with a quaternary carbon center. Combining visible light and a Bronsted acid catalyst, chiral 1,4-dicarbonyl compounds were achieved in good yields with high enantioselectivities by a photochem. carbene transfer protocol.

ACS Catalysis published new progress about Diazo compounds, aryl Role: RCT (Reactant), RACT (Reactant or Reagent). 94-02-0 belongs to class esters-buliding-blocks, and the molecular formula is C11H12O3, HPLC of Formula: 94-02-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Thi Ngo, Men; Han, Jae Woo; Van Nguyen, Minh; Le Dang, Quang; Kim, Hun; Choi, Gyung Ja published the artcile< Antifungal properties of natural products from Pterocarya tonkinensis against phytopathogenic fungi>, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate, the main research area is Pterocarya antifungal phytopathogenic fungus.

The objectives of this article were (i) to isolate and identify the antifungal substances from the Pterocarya tonkinensis extract based on a bioassay-guided fractionation and (ii) to investigate their potential as a biocontrol agent with their antifungal activities in vitro and in vivo. Eighteen compounds were identified from methanol extract of Pterocarya tonkinensis, including two new natural products 1 and 2: 1, pterocaryalactone; 2, pterocaryafuranone; 3, (1S, 6R)-9-hydroxymegastigm-7-en-3-one; 4, (S)-di-Me malate; 5, α-linolenic acid; 6-8, α-tetralones; 9, (R)-methyl-2-hydroxyl-3-phenyl-propanoate; 10, (E)-4-hydroxycinnamic acid Me ester; 11-14, diarylheptanoids, and 15-18, pentacyclic triterpenoids. Based on results of in vitro antifungal assay, Magnaporthe oryzae and Phytophthora infestans were most sensitive to isolated compounds among tested phytopathogenic fungi. When ten active compounds were applied onto plants at concentration of 100 or 500 μg mL-1, compounds 1 and 8 effectively suppressed rice blast disease, and compounds 15 and 16 not only strongly reduced development of blast on rice but also effectively controlled the development of late blight on tomatoes. This is first report to evaluate the in vitro and in vivo antifungal activities of the isolated compounds from a methanol extract of Pterocarya tonkinensis against phytopathogenic fungi, and our results suggest that Pterocarya tonkinensis and its substances can be used as source to develop natural fungicides.

Pest Management Science published new progress about Alternaria brassicicola. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zampella, Angela; Bassarello, Carla; Bifulco, Giuseppe; Gomez-Paloma, Luigi; D’Auria, Maria Valeria published the artcile< Stereochemistry of sphinxolides and reidispongiolides. Asymmetric synthesis of the C17-C22 fragment of reidispongiolide A>, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate, the main research area is reidispongiolide absolute stereochem fragment preparation ozonolysis; asym synthesis hexanetetraol derivative.

Five fragments, [I (R = α, β-OH), II, III (R = α, β-OH)] embedding all the stereogenic centers of reidispongiolide A (IV), have been prepared by a controlled ozonolysis of the IV. The absolute stereochem. of the asym. centers of II, corresponding to the C17-C22 portion of IV, was determined by enantioselective synthesis and application of the advanced Mosher method.

European Journal of Organic Chemistry published new progress about Absolute configuration. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Recommanded Product: (S)-Dimethyl 2-hydroxysuccinate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Musso, Loana; Cincinelli, Raffaella; Zuco, Valentina; De Cesare, Michelandrea; Zunino, Franco; Fallacara, Anna Lucia; Botta, Maurizio; Dallavalle, Sabrina published the artcile< 3-Arylidene-N-hydroxyoxindoles: A New Class of Compounds Endowed with Antitumor Activity>, Recommanded Product: Methyl 2-(2-nitrophenyl)acetate, the main research area is arylidene hydroxyoxindole synthesis antitumor p53 apoptosis; N-hydroxyoxindole; antiproliferative activity; antitumor agents; apoptosis; p53.

A series of compounds containing the N-hydroxyoxindole scaffold were synthesized and evaluated for antitumor activity. The compounds showed potent antiproliferative activity against the wild-type p53 IGROV-1 ovarian carcinoma cell line and considerably lower efficacy against the mutant IGROV-1/Pt1 subline that lacks p53 function. The differential response of ovarian carcinoma cells depending on p53 status was also reflected in the varied susceptibility to apoptosis of the treated cell lines. These results support a role for the p53 transcription factor as a determinant of cytotoxicity. The therapeutic potential of the most promising compound of the series was evaluated in the treatment of an IGROV-1 xenograft growing as ascitic tumor in mice. Using i.p. administration, daily treatment with the compound for four weeks produced a significant delay in the onset of ascites.

ChemMedChem published new progress about Antitumor agents. 30095-98-8 belongs to class esters-buliding-blocks, and the molecular formula is C9H9NO4, Recommanded Product: Methyl 2-(2-nitrophenyl)acetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Frelek, Jadwiga; Geiger, Marcela; Voelter, Wolfgang published the artcile< Absolute configurational assignment of α-hydroxy acids and α-hydroxy esters from their Cupra A circular dichroism spectra>, Formula: C6H10O5, the main research area is chiral alpha hydroxy acid absolute configuration Cotton effect; CD spectra Cupra A hydroxy acid chiral complex.

The in situ formed complexes of cuprammonium solution (Cupra A) with optically active α-hydroxy acids and α-hydroxy esters show CD spectra suitable for determination of the absolute configuration of both groups of compounds In the long wavelength spectral region, compounds of R configuration at the α carbon atom display a pos. Cotton effect of around 600 nm and a neg. one at ca. 720 nm, whereas (S)-α-hydroxy acids and esters exhibit neg. and pos. Cotton effects, resp., in the same spectral range.

Tetrahedron: Asymmetry published new progress about Absolute configuration. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Formula: C6H10O5.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Deb, Barnali; Chakraborty, Ankita; Hossain, Jewel; Majumdar, Swapan published the artcile< A Task-Specific Ionic-Liquid-Mediated Solvent-Free Protocol for Direct Access to Dimethyl Acetal Protected Benzimidazole 2-Carboxaldehydes>, Product Details of C7H12O5, the main research area is dimethyl acetal benzimidazole carboxaldehyde preparation; amino aniline methyl dimethoxyoxobutanoate cyclization imidazolium ionic liquid catalyst.

A robust and straightforward protocol has been developed for the synthesis of a diverse array of di-Me acetal protected benzimidazole-2-carboxaldehydes I (R = H, 6-Me, 5,6-di-Me, 6-Cl, carboxyl; R1 = H, Bn, prop-2-en-1-yl, etc.) by reacting various 2-amino aniline derivatives II with Me 4,4-dimethoxy-3-oxobutanoate using the task-specific imidazolium ionic liquid (HBIm·TFA) as a promoter for N-C/C-N annulation processes. The present protocol offers several advantages over existing protocols, such as single-step process, short reaction times, very mild reaction conditions, high yields, ease of purification, recovery and reusability of the catalyst, and scale-up of the reaction.

SynOpen published new progress about Acetals Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 60705-25-1 belongs to class esters-buliding-blocks, and the molecular formula is C7H12O5, Product Details of C7H12O5.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics