Month: November 2022

Wang, Daoxin published the artcileAlternating Current Electrolysis Enabled Formal C-O/O-H Cross-Metathesis of 4-Alkoxy Anilines with Alcohols, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Angewandte Chemie, International Edition (2022), 61(18), e202201543, database is CAplus and MEDLINE.

A new protocol to achieve the formal C-O/O-H cross-metathesis via a.c. electrolysis was reported. Featuring mild reaction conditions, the protocol allowed readily available 4-alkoxy anilines and alcs. to be converted into a wide range of valuable complex 4-alkoxy anilines I [R = n-Bu, (CH₂)₂OH, (CH₂)₄OH, etc.; R¹ = t-BuC(O), Ts, 4-MeOC₆H₄C(O), etc.; R² = H, 2-Me, 3-Cl, etc.] in highly regioselective and chemoselective manner. Moreover, the present strategy could be used in the late-stage modification of pharmaceuticals as well as biol. active compounds, which demonstrated the potential application.

Angewandte Chemie, International Edition published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C8H5F3O3, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wang, Shengju published the artcileA comparative study on the traditional versus modern yellow rice wine processing methods using Taohong Siwu Decoction for pharmaceutical production, HPLC of Formula: 169590-42-5, the publication is Journal of Ethnopharmacology (2022), 115114, database is CAplus and MEDLINE.

Taohong Siwu Decoction (THSWD) is based on the “First Recipe of Gynecol”. It is widely used in various blood stasis and deficiency syndromes, mainly in gynecol. blood stasis, irregular menstruation, and dysmenorrhea. THSWD has great demand in traditional Chinese medicine (TCM), gynecol., orthopedics, and internal medicine. According to classical records, three medicinal materials, namely Rehmanniae radix, Angelica sinensis, and Carthamus tinctorius, used in THSWD need to be “washed with yellow rice wine”. In the study of TCM prescriptions, the processing methods of medicinal materials not only needed to follow traditional records but also should consider modern tech. conditions. Many medicinal materials in the repertoire of classical prescriptions involve yellow rice wine processing. Determining the processing method for medicinal materials is a key and difficult problem in the research and development of classical prescriptions. With THSWD as the representative, this study analyzed differences between no processing method, the modern processing method of “stir-frying the materials with yellow rice wine,” and the traditional processing method of “washing with yellow rice wine”. We focused on three aspects: composition, efficacy, and endogenous metabolism This study aimed to provide a reference for research on the processing methods of medicinal materials used in classical prescriptions. UPLC-Q-Orbitrap HRMS was used to quickly identify and classify the main chem. compounds of THSWD. A model of primary dysmenorrhea (PD) was established using estradiol benzoate combined with oxytocin. The latent period and writhing time; the levels of serum PGF2α, PGE2, ET-1, and β-EP; and the pathol. sections of the uterus were observed to determine their pharmacodynamic differences. GC-TOF/MS was used to analyze the differences in serum metabolites in rats. A total of 54 active compounds were identified, and the results showed that catalpol and rehmapicroside disappeared following yellow rice wine processing. Compared with materials processed by the traditional method, the relative contents of 15 components, such as 5-hydroxymethylfurfural and digitalis C, increased in materials processed by the modern method. However, the relative contents of 16 components, such as hydroxysafflor yellow A, verbascoside, and ferulic acid, decreased in the modern processing method. The modern and classic processing methods acted on PD through different metabolic pathways. THSWD obtained by classical processing methods mainly treated PD through anti-inflammatory and estrogen metabolism pathways, whereas THSWD obtained by modern processing methods mainly treated PD through anti-inflammatory metabolic pathways. The study revealed the differences in different yellow rice wine processing methods in terms of chem. composition of the THSWD obtained, as well as the mechanisms of action for the treatment of PD. This study provides a reference for the clin. application of THSWD and development of classical prescription preparations

Journal of Ethnopharmacology published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C6H10O3, HPLC of Formula: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Chen, Wei published the artcileSyntheses of 3,4-dihydro-4-oxopyrimido[4,5-b]quinolines, Quality Control of 15029-36-4, the publication is Gaodeng Xuexiao Huaxue Xuebao (1990), 11(5), 532-3, database is CAplus.

Pyrimidoquinolines I (R = H, alkyl, PHCH₂, Ph; R¹, R² = H, H; R¹R² = methylenedioxy) were prepared in 81-94% yield by heating aminoquinolinecarboxamides II with HCONH₂ at 160-170°.

Gaodeng Xuexiao Huaxue Xuebao published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, Quality Control of 15029-36-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kim, Yong-Chul published the artcileAnilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A_2B adenosine receptors, Category: amides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2000), 43(6), 1165-1172, database is CAplus and MEDLINE.

No highly selective antagonists of the A_2B adenosine receptor (AR) have been reported; however such antagonists have therapeutic potential as antiasthmatic agents. Here the synthesis of potent and selective A_2B receptor Antagonists is reported. The structure-activity relationships (SAR) of 8-phenyl-1,3-di-(n-propyl)xanthine derivatives in binding to recombinant human A_2B ARs in HEK-293 cells (HEK-A_2B) and at other AR subtypes were explored. Various amide derivatives of 8-[4-[[carboxymethyl]oxy]phenyl]-1,3-di(n-propyl)xanthine, I (R₁ = n-Pr, X = OCH₂, R₂ = OH) (II), were synthesized. A comparison of aryl, alkyl, and aralkyl amides demonstrated that simple anilides, particularly those substituted in the para-position with electron-withdrawing groups, such as nitro, cyano, and acetyl, bind selectively to human A_2B receptors in the range of 1-3 nM. The unsubstituted anilide I (R₁ = n-Pr, X = OCH₂, R₂ = NHPh) had a K_i value at A_2B receptors of 1.48 nM but was only moderately selective vs. human A₁/A_2A receptors and nonselective vs. rat A₁ receptors. Highly potent and selective A_2B antagonists were a p-aminoacetophenone derivative I (R₁ = n-Pr, X = OCH₂, R₂ = 4-MeOC₆H₄NH) (K_i value 1.39 nM) and a p-cyanoanilide I (R₁ = n-Pr, X = OCH₂, R₂ = NHC₆H₄CN-4) (III) (K_i value 1.97 nM). Compound III was 400-, 245-, and 123-fold selective for human A_2B receptors vs. human A₁/A_2A/A₃ receptors, resp., and 8.5- and 310-fold selective vs. rat A₁/A_2A receptors, resp. Substitution of the 1,3-di-Pr groups with 1,3-di-Et offered no disadvantage for selectivity, and high affinities at A_2B receptors were maintained. Substitution of the p-carboxymethyloxy group of II and its amides with acrylic acid decreased affinity at A_2B receptors while increasing affinity at A₁ receptors. 1,3-Di(cyclohexylmethyl) groups greatly reduced affinity at ARs, although the p-carboxymethyloxy derivative I (R₁ = cyclohexylmethyl, X = CH:CH, R₂ = OH) was moderately selective for A_2B receptors. Several selective A_2B antagonists inhibited NECA-stimulated calcium mobilization in HEK-A_2B cells.

Journal of Medicinal Chemistry published new progress about 264622-53-9. 264622-53-9 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Adenosine Receptor, name is N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide, and the molecular formula is C27H29N5O5, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Joshi, Rajendra published the artcileFacile synthesis of peptide nucleic acids and peptide nucleic acid-peptide conjugates on an automated peptide synthesizer, SDS of cas: 186046-83-3, the publication is Journal of Peptide Science (2011), 17(1), 8-13, database is CAplus and MEDLINE.

Peptide nucleic acids (PNAs) are DNA mimics with a neutral peptide backbone instead of the neg. charged sugar phosphates. PNAs exhibit several attractive features such as high chem. and thermal stability, resistance to enzymic degradation, and stable binding to their RNA or DNA targets in a sequence-specific manner. Therefore, they are widely used in mol. diagnosis of antisense-targeted therapeutic drugs or probes and in pharmaceutical applications. However, the main hindrance to the effective use of PNAs is their poor uptake by cells as well as the difficult and laborious chem. synthesis. In order to achieve an efficient delivery of PNAs into cells, there are already many published reports of peptides being used for transport across the cell membrane. In this protocol, the authors describe the automated as well as cost-effective semi-automated synthesis of PNAs and PNA-peptide constructs on an automated peptide synthesizer. The facile synthesis of PNAs will be helpful in generating PNA libraries usable, e.g. for high-throughput screening in biomol. studies. Efficient synthetic schemes, the automated procedure, the reduced consumption of costly reagents, and the high purity of the products are attractive features of the reported procedure. Copyright © 2010 European Peptide Society and John Wiley & Sons, Ltd.

Journal of Peptide Science published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, SDS of cas: 186046-83-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kashani, Saeed K. published the artcileExploring Homogeneous Conditions for Mild Buchwald-Hartwig Amination in Batch and Flow, Quality Control of 1453-82-3, the publication is Organic Process Research & Development (2020), 24(10), 1948-1954, database is CAplus.

The use of high throughput experimentation to identify a number of conditions that enable Buchwald-Hartwig reactions to be carried out using readily available ligands (e.g. XantPhos) with DBU as a soluble, functional group tolerant, homogeneous base was described. Application of this system to diverse aminations in batch and flow were demonstrated, as was the translation of this technique to performing continuous Mizoroki-Heck and Sonogashira coupling reactions.

Organic Process Research & Development published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Quality Control of 1453-82-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Bethge, Lucas published the artcileNew cyanine dyes as base surrogates in PNA: Forced intercalation probes (FIT-probes) for homogeneous SNP detection, Recommanded Product: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, the publication is Bioorganic & Medicinal Chemistry (2008), 16(1), 114-125, database is CAplus and MEDLINE.

Forced intercalation probes (FIT-probes) are nucleic acid probes, in which an intercalator cyanine dye such as thiazole orange (TO) serves as a replacement of a canonical nucleobase. These probes signal hybridization by showing strong increases of fluorescence. TO in FIT-probes responds to adjacent base mismatches by attenuation of fluorescence intensities at conditions where both matched and mismatched target DNA are bound. The interesting features of TO labeled FIT-probes posed the question whether the forced intercalation concept can be extended to other cyanine dyes of the thiazole orange family. Herein, we present the synthesis of three asym. cyanine dyes and their incorporation into PNA-conjugates by means of both divergent and linear solid-phase synthesis. Melting anal. revealed that the DNA affinity of PNA probes remained high irresp. of the replacement of a nucleobase by the cyanines YO (oxazole yellow), MO or JO. Of the three new tested dye-PNA-conjugates, the YO-containing PNA has properties useful for homogeneous SNP detection. YO-PNA is demonstrated to signal the presence of fully complementary DNA by up to 20-fold enhancement of fluorescence. In addition, YO emission discriminates against single base mismatches by attenuation of fluorescence. Oxazole yellow (YO) as a base surrogate in PNA may prove useful in the multiplex detection of single base mutations at non-stringent conditions.

Bioorganic & Medicinal Chemistry published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Recommanded Product: 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kim, Moo Jun published the artcileAcute Tubular Necrosis Associated with Angiotensin Receptor-neprilysin Inhibitor., Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, the publication is Internal medicine (Tokyo, Japan) (2022), 61(10), 1573-1576, database is MEDLINE.

Sacubitril/valsartan, an angiotensin receptor-neprilysin inhibitor (ARNI), significantly reduces mortality and morbidity in patients with chronic heart failure with a reduced ejection fraction (HFrEF). However, a considerable number of patients treated with sacubitril/valsartan experience hypotension, oliguria, progressive azotemia, and renal failure as adverse events. These issues have been linked to significant gaps in the usage and dosing of guideline-directed medical therapy with ARNI in patients with HFrEF. We herein report a relevant case of pathologically proven acute tubular necrosis after the first dose of sacubitril/valsartan, highlighting the importance of optimizing the medical therapy in an outpatient with HFrEF.

Internal medicine (Tokyo, Japan) published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Recommanded Product: (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kim, Joong-Gon published the artcileA convenient one-pot method for the synthesis of N-methoxy-N-methyl amides from carboxylic acids, Synthetic Route of 100377-32-0, the publication is Bulletin of the Korean Chemical Society (2010), 31(1), 171-173, database is CAplus.

A mild and convenient 1-pot synthesis of Weinreb amides from carboxylates using Cl₃CCN and PPh₃ was developed. The process is general for the preparation of Weinreb amides from a variety of carboxylates. The reaction was also applicable to the preparation of α-amino Weinreb amides and proceeded without deprotection of the N-Fmoc protecting group or racemization.

Bulletin of the Korean Chemical Society published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Synthetic Route of 100377-32-0.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Viswanatha, Gollapalle L. published the artcileSynthesis and anti-hyperlipidemic activity of 3H-benzo[4,5]thieno[2,3-d][1,2,3]triazin-4-ones: possible mechanism of altered lipid metabolism, Related Products of amides-buliding-blocks, the publication is Oman Medical Journal (2012), 27(5), 388-395, database is CAplus and MEDLINE.

Objectives: The present study aimed to evaluate the anti-hyperlipidemic activity of newly synthesized tricyclic benzothieno[1,2,3]triazine derivatives I (R = Me, Et, 2-chlorophenyl), namely CP-1 (3-methyl-5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d][1,2,3]triazin-4-one), CP-2 (3-ethyl-5,6,7,8-tetrahydro-3H-benzo[4,5] thieno[2,3-d][1,2,3]triazin-4-one) and CP-6 [3-(2-chlorophenyl)-5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d][1,2,3]triazin-4-one] against dexamethasone and Triton WR-1339-induced hyperlipidemia in rats. Methods: Anti-hyperlipidemic activities of the test compounds were evaluated against dexamethasone (10 mg/kg, s.c. [s.c.]) and Triton WR-1339 (200 mg/kg, i.p. [i.p]) induced hyperlipidemia in rats. Results: Administration of a single dose of Triton WR-1339 (200 mg/kg i.p) and dexamethasone (10 mg/kg s.c.) for 8 consecutive days to adult wistar rats caused severe hyperlipidemia characterized by a marked increase in serum cholesterol, LDL-C, VLDL-C and triglyceride levels along with an increase in atherogenic index. Serum HDL-C levels were decreased significantly compared to a normal control. Pretreatment with Atorvastatin (10 mg/kg p.o.), CP-1 (25 and 50 mg/kg), CP-2 (25 and 50 mg/kg) and CP-6 (25 and 50 mg/kg) showed significant and dose-dependent protection against dexamethasone and Triton WR-1339-induced hyperlipidemia in rats by maintaining serum total cholesterol, LDL-C, VLDL-C and HDL-C levels within the normal range. Also, a significant decrease in the atherogenic index was observed The anti-hyperlipidemic effect of CP-6 was comparable with reference standard Atorvastatin. Furthermore, CP-6 was found to be more potent than CP-1 and CP-2. Conclusion: These findings suggest that CP-1, CP-2 and CP-6 possess significant anti-hyperlipidemic activity against exptl. animal models of hyperlipidemia.

Oman Medical Journal published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C6H5BN2O3, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics