Month: November 2022

Tharp, Jeffery M. published the artcileInitiation of protein synthesis with non-canonical amino acids in vivo, Product Details of C11H22N2O4, the publication is Angewandte Chemie, International Edition (2020), 59(8), 3122-3126, database is CAplus and MEDLINE.

By transplanting identity elements into E. coli tRNA^fMet, we have engineered an orthogonal initiator tRNA (itRNA^Ty2) that is a substrate for Methanocaldococcus jannaschii TyrRS. We demonstrate that itRNA^Ty2 can initiate translation in vivo with aromatic non-canonical amino acids (ncAAs) bearing diverse sidechains. Although the initial system suffered from low yields, deleting redundant copies of tRNA^fMet from the genome afforded an E. coli strain in which the efficiency of non-canonical initiation equals elongation. With this improved system we produced a protein containing two distinct ncAAs at the first and second positions, an initial step towards producing completely unnatural polypeptides in vivo. This work provides a valuable tool to synthetic biol. and demonstrates remarkable versatility of the E. coli translational machinery for initiation with ncAAs in vivo.

Angewandte Chemie, International Edition published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C2H8Cl2N4S2, Product Details of C11H22N2O4.

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

Audoux, Jerome published the artcileSynthesis of new flat polyheterocyclic systems, potential DNA intercalating agents. Diazines Part 47, HPLC of Formula: 146140-95-6, the publication is Journal of Heterocyclic Chemistry (2006), 43(6), 1497-1503, database is CAplus.

Using a regioselective metalation in connection with Stille cross-coupling reaction, various flat tetra- or pentaheterocyclic compounds were obtained which could be potential intercalating DNA agents.

Journal of Heterocyclic Chemistry published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, HPLC of Formula: 146140-95-6.

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

Bettadahalli, Sadashivaiah published the artcileEvidence on n-3 Fatty Acids and Oleic Acid Role in Retinal Inflammation and Microvascular Integrity: Insight from a Hyperlipidemic Rat Model, Quality Control of 321673-30-7, the publication is Inflammation (2020), 43(3), 868-877, database is CAplus and MEDLINE.

Loss of retinal function due to manifestation of chronic inflammation and oxidative stress in hyperglycemia is well addressed. However, the effect of hyperlipidemia on retinal inflammation and microvascular integrity, and the modulatory effects of oxidation-stable oleic acid and long-chain n-3 fatty acids have never been addressed. The objective of this investigation was to assess the retinoprotective effect of oxidation stable oleic acid and oxidation-susceptible EPA + DHA on retinal inflammation and microvascular integrity, under hyperlipidemic conditions. Male Wistar rats were fed with control (7.0% lard), high-fat (35.0% lard), high-fat with fish oil (17.5% fish oil + 17.5% lard), high-fat with olive oil (17.5% olive oil + 17.5% lard), and high-fat with fish oil and olive oil (11.66% fish oil + 11.66% of olive oil + 11.66% of lard) diet for 90 days. Systemic and retinal inflammation, as measured by eicosanoids and cytokines, retinal expression of NF-kB, capillary degeneration, and pericyte loss, were assessed. Besides, the retinal NF-kB-p65 expression, capillary degeneration, and pericyte loss were significantly (p < 0.05) increased under hyperlipidemic conditions. Dietary incorporation of oleic acid and EPA + DHA significantly (p < 0.05) suppressed hyperlipidemia-induced effects in the retina. In conclusion, hyperlipidemia causes retinal aberrations by compromising the balance in the inflammatory response and microvascular integrity.

Inflammation published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Quality Control of 321673-30-7.

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

Avitabile, Concetta published the artcileIncorporation of Naked Peptide Nucleic Acids into Liposomes Leads to Fast and Efficient Delivery, HPLC of Formula: 186046-83-3, the publication is Bioconjugate Chemistry (2015), 26(8), 1533-1541, database is CAplus and MEDLINE.

The delivery of peptide nucleic acids (PNAs) to cells is a very challenging task. We report here that a liposomal formulation composed of egg PC/cholesterol/DSPE-PEG2000 can be loaded, according to different encapsulation techniques, with PNA or fluorescent PNA oligomers. PNA loaded liposomes efficiently and quickly promote the uptake of a PNA targeting the microRNA miR-210 in human erythroleukemic K562 cells. By using this innovative delivery system for PNA, down-regulation of miR-210 is achieved at a low PNA concentration

Bioconjugate 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, HPLC of Formula: 186046-83-3.

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

Li, Linfeng published the artcileAn improved high yield total synthesis and cytotoxicity study of the marine alkaloid neoamphimedine: an ATP-competitive inhibitor of topoisomerase IIα and potent anticancer agent, Formula: C11H16BNO3, the publication is Marine Drugs (2014), 12(9), 4833-4850, database is CAplus and MEDLINE.

Recently, we characterized neoamphimedine (neo) as an ATP-competitive inhibitor of the ATPase domain of human Topoisomerase IIα. Thus far, neo is the only pyridoacridine with this mechanism of action. One limiting factor in the development of neo as a therapeutic agent has been access to sufficient amounts of material for biol. testing. Although there are two reported syntheses of neo, both require 12 steps with low overall yields (≤6%). In this article, we report an improved total synthesis of neo achieved in 10 steps with a 25% overall yield. In addition, we report an expanded cytotoxicity study using a panel of human cancer cell lines, including: breast, colorectal, lung, and leukemia. Neo displays potent cytotoxicity (nM IC₅₀ values) in all, with significant potency against colorectal cancer (lowest IC₅₀ = 6 nM). We show that neo is cytotoxic not cytostatic, and that neo exerts cytotoxicity by inducing G2-M cell cycle arrest and apoptosis.

Marine Drugs published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Formula: C11H16BNO3.

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

Ibrahim, Eman Ibrahim published the artcileA single oral dose of celecoxib-loaded solid lipid nanoparticles for treatment of different developmental stages of experimental schistosomiasis mansoni, Formula: C17H14F3N3O2S, the publication is Acta Tropica (2022), 106342, database is CAplus and MEDLINE.

Schistosomiasis, a neglected tropical parasitic disease, is associated with severe pathol., mortality and economic loss. The treatment and control of schistosomiasis depends mainly on a single dose of praziquantel (PZQ). Drug repurposing and nanomedicine attract great attention to improve anti-schistosomal therapy. Previously, we reported that celecoxib (CELE), the non-steroidal anti-inflammatory drug, showed potent anti-schistosomal efficacy in an oral dose of 20 mg/kg/day for five days against different developmental stages of Schistosoma mansoni (S. mansoni) infection in mice. The aim of the current study was to shorten the duration of CELE treatment to reach an effective single oral dose against different developmental stages of S. mansoni infection using solid lipid nanoparticles (SLNs) as nano-carriers. The latter enhance the solubility, bioavailability and drug delivery and hence can decrease the frequency of administration which is of great clin. value. CELE-loaded SLNs showed good colloidal properties, high entrapment efficiency and drug loading, sustained biphasic release pattern with excellent storage stability. The used regimen was efficient against different developmental stages of S. mansoni infection with the most pronounced effect against the juvenile stage where the worm load, the hepatic egg count and the intestinal egg count were reduced by 86.39%, 91.45% and 90.11%, resp. Meanwhile, when targeting the invasive and the adult stages, it induced reduction in the worm load by 73.55% and 78.22%, the hepatic egg count by 69.99% and 75.39% and the intestinal egg count by 77.57% and 79.89%, resp. Addnl., CELE-loaded SLNs caused extensive tegumental damage of adult worms and marked improvement in the liver pathol.

Acta Tropica 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 C17H14F3N3O2S, Formula: C17H14F3N3O2S.

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

El-Kafrawy, Dina S. published the artcileComparative study of two versatile multi-analyte chromatographic methods for determination of diacerein together with four non-steroidal anti-inflammatory drugs: Greenness appraisal using Analytical Eco-Scale and AGREE metrics, HPLC of Formula: 169590-42-5, the publication is Sustainable Chemistry and Pharmacy (2022), 100709, database is CAplus.

According to green anal. chem. (GAC) principles, multi-analyte methods are usually more preferred than methods determining one analyte at a time (principle 8) as they allow saving resources (time, reagents and money) (principle 9) and permit the reduction of generated waste (principle 7) as well as reduction of needed samples (principle 2). The present work herein, describes for the first time the development, validation and comparison of novel green versatile multi-analyte HPLC-DAD and HPTLC methods for the quant. estimation of five drugs (diacerein, aceclofenac, diclofenac sodium, celecoxib and meloxicam) within a single run in a short anal. time. For HPLC-DAD, separation was performed through using Zorbax SB C18 (4.6 x 250 mm, 5μm particle size) with the mobile phase composed of 0.05 M phosphate buffer pH 3.0 and acetonitrile (42:58, volume/volume) at a flow rate of 1 mL/min. The chromatograms were extracted at 258, 276 and 355 nm. In HPTLC procedure, precoated TLC silica gel aluminum plates 60 F254 were used with a mobile phase consisting of mixture of (chloroform: methanol: acetic acid, 92:8:0.25, volume/volume/v). The developed plates were scanned densitometrically at 258, 280 and 360 nm. Validation of the proposed methods was performed following the ICH guidelines for linearity, ranges, precision, accuracy, robustness, detection and quantification limits. Good linearities were confirmed by the high values of correlation coefficients (r > 0.9992). Appraisal of the greenness of the developed methods and comparison with different reported chromatog. methods was performed using the anal. Eco-scale (AES) approach and the novel Anal. GREEnness (AGREE) metric.

Sustainable Chemistry and Pharmacy 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 C17H14F3N3O2S, HPLC of Formula: 169590-42-5.

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

Ibara, Miho published the artcileChemo- and site-selective replacement of N-terminal carbamates in peptides, Name: H-Lys(Boc)-OH, the publication is Organic Letters (2022), 24(11), 2131-2136, database is CAplus and MEDLINE.

In peptide synthesis, it is important to distinguish the terminal amino group and carry out the selective transformation of only the N-terminal protecting group. We describe herein a reaction for the chemo- and site-selective replacement of carbamates with various other carbamates only at the N-terminus of peptides. We demonstrate the scope of carbamates and peptides and the introduction of fluorine into a peptide. This strategy is applicable to the late stage of peptide synthesis.

Organic Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Name: H-Lys(Boc)-OH.

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

Zaki, Remon M. published the artcileA convenient synthesis, reactions and biological evaluation of novel pyrazolo[3,4-b]selenolo[3,2-e]pyrazine heterocycles as potential anticancer and antimicrobial agents, Application In Synthesis of 79-07-2, the publication is Medicinal Chemistry Research (2020), 29(12), 2130-2145, database is CAplus.

A novel series of 5-amino-6-substituted-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]selenolo[3,2-e]pyrazines was synthesized by the reaction of the chloro pyrazolo[3,4-b]pyrazine carbonitrile with selenium element in the presence of sodium borohydride and ethanol, followed by the reaction with α-halo alkylating agents to produce the selanyl-alkylated derivatives The latter compounds underwent Thorpe-Ziegler cyclization upon heating with ethanolic sodium ethoxide solution to afford the target selenolopyrazolopyrazine compounds The 5-amino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]selenolo[3,2-e]pyrazine-6-carboxamide was used as a versatile precursor for synthesis of new heterocyclic fused to the pyrazoloselenolopyrazine moiety namely: pyrimidine and imidazopyrimidine. Assignment of the chem. structures for the newly synthesized compounds was confirmed on the bases of elemental and spectral techniques including FT-IR, ¹H NMR, ¹³C NMR, and mass spectra. Furthermore, certain compounds were screened for their antimicrobial activity which revealed remarkable activities against various pathogenic strains of bacteria and fungi. Alternatively, some of these compounds exhibited promising anticancer action against some colon and breast cancer cells.

Medicinal Chemistry Research published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C25H23NO4, Application In Synthesis of 79-07-2.

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

El-Awady, Mohamed I. published the artcileDecision-making tree for improving selectivity and sensitivity of sweeping-MEKC determination of hydrophobic analytes: Application to five cardiovascular drugs with greenness assessment, Category: amides-buliding-blocks, the publication is Microchemical Journal (2022), 107792, database is CAplus.

Efficient separation of five cardiovascular drugs has been achieved by a new micellar electrokinetic chromatog. method based on using a general strategy that can be applied for the separation of different hydrophobic analytes, while keeping the highest possible sweeping efficiency and hence the highest possible sensitivity. The studied drugs include valsartan, atorvastatin, ezetimibe, amlodipine, and simvastatin. The separation is accomplished in less than 12 min by applying a basic background electrolyte composed of 10 mM disodium tetraborate buffer of pH 10.5 containing 25 mM SDS and 11% n-propanol at 30 kv. Cromolyn sodium is used as an internal standard Variables that may influence the electrophoretic mobility of the five compounds are investigated. The calibration plots are linear within ranges of 0.5-20.0 μg/mL, 0.5-10.0 μg/mL and 10.0-100.0 μg/mL for valsartan, ezetimibe and simvastatin (at 200 nm) and 1.0-30.0 μg/mL for amlodipine, atorvastatin and simvastatin (at 240 nm). Correlation coefficients are ≥ 0.9997 and detection limits are ranged between 0.12 and 2.05 μg/mL. The developed procedure is successfully utilized to estimate the studied compounds in different pharmaceutical preparations The obtained data are statistically analyzed and evaluated. The greenness profile of the investigated approach has been assessed by a recent assessment tool to ensure the principles of green chem.

Microchemical Journal 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, Category: amides-buliding-blocks.

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