Month: November 2022

On August 2, 2018, Qian, Yimin; Crew, Andrew P.; Crews, Craig M.; Dong, Hanqing; Hornberger, Keith R.; Wang, Jing published a patent.Related Products of 882518-89-0 The title of the patent was Preparation of substituted benzothiophenes as modulators of estrogen receptor proteolysis and associated methods of use. And the patent contained the following:

The disclosure relates to bifunctional compounds of formulas I and II, which find utility as modulators of estrogen receptor (target protein). In particular, the disclosure is directed to bifunctional compounds of formulas I and II, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the resp. E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Compounds of formulas I and II wherein ULM is a small mol. E3 ubiquitin ligase binding moiety that binds or targets and E3 ubiquitin ligase; L is a chem. linker; X is O and CO; X1 and X2 are independently N and HC; R1 is OH, alkanoyloxy, aroyloxy and lower alkoxy; R2 and R4 are independently H, OH, halo, CN, CF3, etc.; R3 and R5 are independently H and halo; with provisions; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. The disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the disclosure. Example compound III was prepared by a general procedure (procedure given). The invention compounds were evaluated for their estrogen receptor proteolysis modulatory activity. From the assay, it was determined that compound III exhibited IC50 value of 12.7 nM. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Related Products of 882518-89-0

The Article related to benzothiophene preparation estrogen receptor proteolysis modulator, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Related Products of 882518-89-0

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

Shakam, Huda M.; Mohamed, Abeer A.; Salem, Mohamed Z. M. published an article in 2022, the title of the article was Down-regulatory effect of essential oils on fungal growth and Tri4 gene expression for some Fusarium oxysporum strains: GC-MS analysis of essential oils.SDS of cas: 85-91-6 And the article contains the following content:

The objectives of this work were to evaluate the efficacy of Eucalyptus camaldulensis green branches (GB) and Origanum majorana whole plant (WP) essential oils (EOs) on Tri4 gene expression and Fusarium oxysporum strains growth In vitro. Five strains of Fusarium oxysporum were identified molecularly through polymerase chain reaction (PCR) amplification of the internal transcript spacer (ITS) region. The efficacy of the EOs from Eucalyptus camaldulensis GB and Origanum majorana WP on Tri4 gene expression and F. oxysporum strains growth were evaluated In vitro. GC-MS anal. of the EOs referred that 1,8-cineole, and spathulenol were presented in E. camaldulensis GB, while in O. majorana WP were tricyclene, and p-cymene as abundant compounds E. camaldulensis and O. majorana EOs showed MIC of 32-64 mug/mL and 32 mug/mL, resp. E. camaldulensis EO was more suppressive against all the F. oxysporum strains. Both EOs reduced Tri4 gene expression significantly compared with control. qRT-PCR results revealed a down-regulation in Tri4 gene expression of all of F. oxysporum strains exposed to both EOs at the MIC values. The results suggest that both EOs can be used as safe and green bio-pesticide. The experimental process involved the reaction of Methyl N-Methylanthranilate(cas: 85-91-6).SDS of cas: 85-91-6

The Article related to fusarium oxysporum tri4 gene expression fungal growth essential oil, Plant Biochemistry: Photosynthesis (Algae, Bacteria, and Green Plants) and other aspects.SDS of cas: 85-91-6

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

On October 9, 2008, Kaila, Neelu; Janz, Kristin Marie; Huang, Adrian; Moretto, Allessandro Fabio; Bedard, Patricia Ward published a patent.COA of Formula: C12H14F3NO2 The title of the patent was Preparation of quinoline compounds as selectin inhibitors for disease treatment. And the patent contained the following:

The present teachings relate to novel compounds of formula I wherein R1 is -OR9, -C(O)R10, etc.; R2 is -C(O)OR9, etc.; R3 and R3′ independently are H, -CN, -NO2, halo, etc.; R4-R7 independently are H, C1-10alkyl, etc.; or R3 and R3′ together, R4 and R5 together, and R6 and R7 together form part of a ring; R8 is (un)substituted C6-14 aryl or 5-14 membered heteroaryl; R9 is H, -C(O)R10, etc.; R10 is H, OH, SH, etc. Compounds of the present teachings can act as antagonists of the mammalian adhesion proteins known as selectins. Methods for treating or preventing selectin-mediated disorders are provided, which include administration of these compounds in a therapeutically effective amount Synthetic procedures for preparing I are exemplified. Example compound II, prepared by reacting the appropriate indoline-2,3-dione with the appropriate 2-oxopropyl acetate, caused 37% inhibition in a Biacore P-selectin/PSGL-1 inhibition assay at 250μM. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).COA of Formula: C12H14F3NO2

The Article related to quinoline compound preparation selectin inhibitor disease treatment, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.COA of Formula: C12H14F3NO2

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

On September 29, 2011, Brooks, Carl A.; Cheung, Mui; Eidam, Hilary S.; Fox, Ryan M.; Hilfker, Mark A.; Manas, Eric S.; Ye, Guosen published a patent.Recommanded Product: 141940-37-6 The title of the patent was 4-Quinolinecarboxamide derivatives as TRPV4 antagonists and their preparation and use for the treatment of diseases. And the patent contained the following:

The invention relates to 4-quinolinecarboxamide derivatives of formula I, which are TRPV4 antagonists and which are useful in the treatment of diseases. Compounds of formula I wherein R1 is C1-6 alkyl and C3-6 cycloalkyl; each R2 is independently OH, C1-4 alkoxy, C1-4 alkyl, etc.; R3 is (un)substituted morpholinyl, (un)substituted piperidinyl, (un)substituted pyrrolidinyl, etc.; each R4 is independently CF3, halo, C1-3 alkyl and C1-3 alkoxy; each R5 is independently (un)substituted 2-oxopyrrolidin-1-yl, halo, CN, etc.; two adjacent R5 taken together to form OCH2O and O(CH2)2O; each R6 is independently halo, Me and methoxy; X is N and CH; each n is independently 0 to 2; each p is independently 0 to 2; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their TRPV4 antagonistic activity. From the assay, it was determined that all compounds exhibited IC50 values in the range from 1 nM to 10 μM. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Recommanded Product: 141940-37-6

The Article related to quinolinecarboxamide preparation trpv4 antagonist treatment disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Recommanded Product: 141940-37-6

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

On October 26, 2021, Duan, Wenhu; Shen, Xu; Wang, Wei; Wang, Jiaying; Cao, Sufen; Lv, Jianlu; Xu, Xu published a patent.Application In Synthesis of Methyl 2-(3-formylphenyl)acetate The title of the patent was Preparation of compounds with AMPK agonistic activity and prodrugs thereof and their application in medicine. And the patent contained the following:

The invention discloses the preparation method of the compounds with AMPK agonistic activity with general formula I, [wherein X = H or halogen; M = N or CH, R1 = substituted or unsubstituted 6-10 membered aryl, substituted or unsubstituted 3-10 membered heteroaryl containing 1-3 heteroatoms selected from N, O and S; R2 = hydroxyl, carboxyl, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted 6-10 membered aryl and substituted or unsubstituted 3-10 membered heteroaryl containing 1-3 heteroatoms selected from N, O and S], which has the advantages of preparing and treating diseases related to abnormal energy metabolism, neurodegenerative diseases and inflammation related diseases; cardiovascular and cerebrovascular diseases, tumor drug. For example, 2-(3-(7-chloro-6-(4-(1- hydroxycyclobutyl) phenyl)-2-oxo-1,2- dihydroquinoline-3-yl) phenyl) acetic acid was prepared via Suzuki-coupling with 1-(4- bromophenyl) cyclobutanol and bis(pinacolato)diboron, hydrolysis of di-Et isophthalate, followed by acylation with 2-amino-5-bromo-4-chlorobenzaldehyde, followed by Knoevenagel reaction, followed by Suzuki coupling with 1-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl] cyclobutanol, and followed by hydrolysis. The compounds with AMPK agonistic activity can be used as therapeutic agents for diseases related to abnormal energy metabolism, neurodegenerative diseases, neurol. and mitochondrial dysfunction and disorder diseases, inflammation related diseases, cardiovascular and cerebrovascular diseases and tumors. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Application In Synthesis of Methyl 2-(3-formylphenyl)acetate

The Article related to ampk agonist quinoline condensation suzuki coupling hydrolysis human, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application In Synthesis of Methyl 2-(3-formylphenyl)acetate

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

On May 3, 2007, Hurt, Clarence Ray; Pennell, Andrewm. K.; Wright, John Jessen; Wang, Qiang; Leleti, Manmohan Reddy; Thomas, William D.; Li, Yandong; Dragoli, Dean R. published a patent.Formula: C10H10O3 The title of the patent was Substituted dihydropyridines as C5a receptor modulators and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I are provided that are modulators of the C5a receptor. Compounds of formula I wherein A is N or C; B is halo, CN, NO2, CO2H and derivatives, CONH2 and derivatives, NH and derivatives, etc.; R1 is H, amino, (un)substituted C1-8 (di)alkylamino, (un)substituted C1-8 alkoxy, (un)substituted C1-8 (halo)alkyl, etc.; C1 and C2 are independently (un)substituted (hetero)aryl, (un)substituted (hetero)aryl-C1-4 alkyl, (un)substituted (hetero)cycloalkyl, and (un)substituted (hetero)cycloalkyl-C1-4 alkyl; L1 is bond, (un)substituted C1-8 (hetero)alkylene, (un)substituted C1-8 alkenylene, (un)substituted C2-8 alkynylene, S, SO, SO2, O, NH and derivatives; R2 is OH and derivatives, NH2 and derivatives, C1-8 (halo)alkyl, C3-6 cycloalkyl, C2-8 alkenyl, (hetero)aryl, etc.; R3 is H, C1-6 (halo)alkyl, C1-6 acyl, C3-8 cycloalkyl, (hetero)aryl, etc.; D is O, S, and NOH and derivatives; and their pharmaceutically acceptable salts thereof, are claimed. The compounds are substituted dihydropyridines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathol. activation of C5a receptors. Example compound II was prepared by condensation of 4-methylbenzaldehyde with acetone; the resulting (E)-4-(4-methylphenyl)-3-buten-2-one underwent cyclization with di-Et malonate followed by decarboxylation to give 4-(4-methylphenyl)cyclohexane-1,3-dione, which underwent cyclization with 3-hydroxybenzaldehyde, cyclopentyl acetoacetate and ammonium acetate to give compound II. All the invention compounds were evaluated for their C5a receptor modulatory activity. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Formula: C10H10O3

The Article related to dihydropyridine preparation c5a receptor modulator treatment disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Formula: C10H10O3

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

On January 31, 2019, Zhang, Ruijie K.; Chen, Kai; Huang, Xiongyi; Wohlschlager, Lena; Renata, Hans; Arnold, Frances H. published an article.Quality Control of 3-Acetyldihydrofuran-2(3H)-one The title of the article was Enzymatic assembly of carbon-carbon bonds via iron-catalysed sp3 C-H functionalization. And the article contained the following:

Although abundant in organic mols., carbon-hydrogen (C-H) bonds are typically considered unreactive and unavailable for chem. manipulation. Recent advances in C-H functionalization technol. have begun to transform this logic, while emphasizing the importance of and challenges associated with selective alkylation at a sp3 carbon. Here we describe iron-based catalysts for the enantio-, regio- and chemoselective intermol. alkylation of sp3 C-H bonds through carbene C-H insertion. The catalysts, derived from a cytochrome P 450 enzyme in which the native cysteine axial ligand has been substituted for serine (cytochrome P411), are fully genetically encoded and produced in bacteria, where they can be tuned by directed evolution for activity and selectivity. That these proteins activate iron, the most abundant transition metal, to perform this chem. provides a desirable alternative to noble-metal catalysts, which have dominated the field of C-H functionalization. The laboratory-evolved enzymes functionalize diverse substrates containing benzylic, allylic or α-amino C-H bonds with high turnover and excellent selectivity. Furthermore, they have enabled the development of concise routes to several natural products. The use of the native iron-haem cofactor of these enzymes to mediate sp3 C-H alkylation suggests that diverse haem proteins could serve as potential catalysts for this abiol. transformation, and will facilitate the development of new enzymic C-H functionalization reactions for applications in chem. and synthetic biol. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Quality Control of 3-Acetyldihydrofuran-2(3H)-one

The Article related to engineering cytochrome p411 heme iron substrate alkylation carbene insertion, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Quality Control of 3-Acetyldihydrofuran-2(3H)-one

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

On September 30, 2022, La-ongthong, Kannika; Sawekteeratana, Natthapat; Klaysuk, Jasarin; Soorukram, Darunee; Leowanawat, Pawaret; Reutrakul, Vichai; Krobthong, Sucheewin; Wongtrakoongate, Patompon; Kuhakarn, Chutima published an article.Name: 3-Acetyldihydrofuran-2(3H)-one The title of the article was Cyclization of o-Alkynylisocyanobenzenes with 1,3-Dicarbonyl Compounds. And the article contained the following:

A facile and convenient reaction of o-alkynylisocyanobenzenes with various active-methylene compounds, including 1,3-diesters, 1,3-diketones,β-keto esters, and β-keto amides, under Bronsted basic conditions, had been developed. Di-Et malonate reacted smoothly with a collection of o-alkynylisocyanobenzenes to provide the corresponding 2-quinolin-2-yl malonates in excellent yields. Acetylacetone gave a mixture of quinolin-4-yl and quinolin-2-yl derivatives Acetoacetate esters and acetoacetyl amide derivative initially gave 2-quinolin-2-yl adducts that underwent partial deacetylation under the reaction conditions. The experimental process involved the reaction of 3-Acetyldihydrofuran-2(3H)-one(cas: 517-23-7).Name: 3-Acetyldihydrofuran-2(3H)-one

The Article related to quinoline preparation, alkynylisocyanobenzene dicarbonyl compound cyclization, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Name: 3-Acetyldihydrofuran-2(3H)-one

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

Dippe, M.; Brandt, W.; Rost, H.; Porzel, A.; Schmidt, J.; Wessjohann, L. A. published an article in 2015, the title of the article was Rationally engineered variants of S-adenosylmethionine (SAM) synthase: reduced product inhibition and synthesis of artificial cofactor homologues.Name: 3-Aminodihydrothiophen-2(3H)-one hydrochloride And the article contains the following content:

S-Adenosylmethionine (SAM) synthase was engineered for biocatalytic production of SAM and long-chain analogs by rational re-design. Substitution of two conserved isoleucine residues extended the substrate spectrum of the enzyme to artificial S-alkylhomocysteines. The variants proved to be beneficial in preparative synthesis of SAM (and analogs) due to a much reduced product inhibition. The experimental process involved the reaction of 3-Aminodihydrothiophen-2(3H)-one hydrochloride(cas: 6038-19-3).Name: 3-Aminodihydrothiophen-2(3H)-one hydrochloride

The Article related to adenosylmethionine synthase bacillus protein engineering sam analog methylation, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Name: 3-Aminodihydrothiophen-2(3H)-one hydrochloride

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

On January 31, 2014, Majee, A.; Kundu, S. K.; Santra, S.; Hajra, A. published an article.Category: esters-buliding-blocks The title of the article was An improved procedure of Miyashita protocol for the preparation of ureidomethylene derivatives of 1,3-dicarbonyl compounds. And the article contained the following:

The synthesis of ureidomethylene derivatives I [R1 = CH3, OCH2CH3; R2 = CH3, OCH2CH3, OCH3, OC(CH3), etc.], through a three-component condensation of 1,3-dicarbonyl compounds, urea and trimethylorthoformate in presence of zinc triflate under solvent-free conditions, has been developed. Me substituted ureas also give the condensation product under similar reaction conditions. The experimental process involved the reaction of (Trimethoxymethyl)benzene(cas: 707-07-3).Category: esters-buliding-blocks

The Article related to ureidomethylene preparation, urea trimethyl orthoformate dicarbonyl condensation, Aliphatic Compounds: Ketones and Derivatives, Including Sulfur Analogs and other aspects.Category: esters-buliding-blocks

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