Month: November 2022

Matsunuma, Satoru published the artcileHigh concentration of oxaliplatin may be a risk factor for vascular pain, SDS of cas: 169590-42-5, the publication is Journal of Clinical Pharmacy and Therapeutics (2022), 47(4), 462-468, database is CAplus and MEDLINE.

Oxaliplatin (L-OHP) is an antineoplastic agent that frequently causes vascular pain. However, the risk factors for vascular pain are unclear, and prevention methods have not been established. We retrospectively investigated patients who were treated with L-OHP to examine the influence of patient characteristics and concomitant analgesic use on the incidence of vascular pain. We collected information about the presence or absence of vascular pain, age, sex, treatment dose and analgesic use of patients who received L-OHP at Tokyo Medical University Hachioji Medical Center. We analyzed the relevance of each factor between the vascular pain onset and non-onset groups. Thirty-two patients (average age: 68.6 years; 69.8% and 30.2% men and women, resp.) were classified into the vascular pain onset (n = 64) and non-onset groups (n = 68). The multivariate logistic regression anal. revealed that L-OHP concentration (>358.5 mg/L) was an independent determinant of vascular pain development (odds ratio: 2.422, 95% CI: 1.117-5.252). Intergroup differences in age, sex, body mass index, non-steroidal anti-inflammatory drug use, and underlying pain from cancer and other comorbidities were not significant. High L-OHP concentration was identified as a significant risk factor for L-OHP-induced vascular pain. Our results indicate that the dilution of L-OHP may reduce the incidence of vascular pain.

Journal of Clinical Pharmacy and Therapeutics 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, SDS of cas: 169590-42-5.

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

Li, Bin published the artcileSubstance P-regulated leukotriene B4 production promotes acute pancreatitis-associated lung injury through neutrophil reverse migration, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is International Immunopharmacology (2018), 147-156, database is CAplus and MEDLINE.

Leukotriene B4 (LTB4) is a potent chemoattractant and inflammatory mediator involved in multiple inflammatory diseases. Substance P (SP) has been reported to promote production of LTB4 in itch-associated response in vivo and in some immune cells in vitro. Here, we investigated the role of LTB4 in acute pancreatitis (AP), AP-associated acute lung injury (ALI) and the related mechanisms of LTB4 production in AP. In vivo, murine AP model was induced by caerulein and lipopolysaccharide or L-arginine. The levels of LTB4 and its specific receptor BLT1 were markedly upregulated in both AP models. Blockade of BLT1 by LY293111 attenuated the severity of AP, decreased neutrophil reverse transendothelial cell migration (rTEM) into the circulation and alleviated the severity of ALI. In vitro, treatment of pancreatic acinar cells with SP increased LTB4 production Furthermore, SP treatment increased phosphorylation of protein kinase C (PKC) α and mitogen activated protein kinases (MAPKs), including extracellular signal-regulated kinase (ERK), p-38 MAPK and c-Jun NH2-terminal kinase (JNK). Finally, blockade of neurokinin-1 receptor by CP96345 significantly attenuated the severity of AP and decreased the level of LTB4 when compared to AP group. In summary, these results show that SP regulates the production of LTB4 via PKC α/MAPK pathway, which further promotes AP-associated ALI through neutrophil rTEM.

International Immunopharmacology 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, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Lin, Songwen published the artcileIdentification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors, Synthetic Route of 100377-32-0, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(3), 790-793, database is CAplus and MEDLINE.

Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors. Design, synthesis and structure activity relationship are reported.

Bioorganic & Medicinal Chemistry Letters 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

Wang, Changliu published the artcileYnamide-Mediated Thioamide and Primary Thioamide Syntheses, Safety of 3-Methoxybenzothioamide, the publication is Journal of Organic Chemistry (2022), 87(9), 5617-5629, database is CAplus and MEDLINE.

Environmentally friendly ynamide-mediated thioamidation of monothiocarboxylic acids with amines or ammonium hydroxide for the synthesis of thioamides was described. Simple and mild reaction conditions tolerate a wide variety of functional groups such as hydroxyl, ester, tertiary amine, ketone, and amide moieties. Readily available NaSH served as the sulfur source, avoiding the use of toxic, expensive, and malodorous organic sulfur reagents and making this strategy environmentally friendly and practical. Importantly, the stereochem. integrity of α-chiral monothiocarboxylic acids was maintained during the activation step and subsequent aminolysis process, which offers a racemization-free strategy for peptide and protein C-terminal modification. Furthermore, a number of thioamide-modified drugs were prepared in good yields by this protocol and the synthesized primary thioamides were transformed into backbone thiazolyl modification peptides.

Journal of Organic Chemistry published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C15H20O6, Safety of 3-Methoxybenzothioamide.

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

Yengoyan, Aleksandr P. published the artcileSynthesis of 4,6-Dimethylpyrimidine 2-Thiosubstituted Derivatives and Their Preliminary Biological Evaluation, COA of Formula: C2H4ClNO, the publication is Letters in Organic Chemistry (2021), 18(4), 311-317, database is CAplus.

Based on 4,6-dimethylpyrimidine-2-thiol hydrochloride a series of its novel S-substituted derivatives including bi- and tricyclic heterosystems with a combination of azines and pyrazole cycles I (R = H, Me; R¹ = H, Ph, 3,4-dichlorophenyl, etc.), were synthesized. The preliminary biol. screening has shown that the obtained compounds have a pronounced plants growth-stimulating activity, which is a new property for these heterosystems. This fact indicates the prospectivity of further development of synthesized systems for the search for new plants growth stimulators.

Letters in Organic Chemistry 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 C6H12Br2, COA of Formula: C2H4ClNO.

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

Aiba, Yuichiro published the artcilePNA-NLS conjugates as single-molecular activators of target sites in double-stranded DNA for site-selective scission, SDS of cas: 186046-83-3, the publication is Organic & Biomolecular Chemistry (2013), 11(32), 5233-5238, database is CAplus and MEDLINE.

Artificial DNA cutters have been developed by us in our previous studies by combining two strands of pseudo-complementary peptide nucleic acid (pcPNA) with Ce(iv)-EDTA-promoted hydrolysis. The pcPNAs have two modified nucleobases (2,6-diaminopurine and 2-thiouracil) instead of conventional A and T, and can invade double-stranded DNA to activate the target site for the scission. This system has been applied to site-selective scissions of plasmid, λ-phage, E. coli genomic DNA, and human genomic DNA. Here, we have reported a still simpler and more convenient DNA cutter obtained by conjugating peptide nucleic acid (PNA) with a nuclear localization signal (NLS) peptide. This new DNA cutter requires only one PNA strand (instead of two) bearing conventional (non-pseudo-complementary) nucleobases. This PNA-NLS conjugate effectively activated the target site in double-stranded DNA and induced site-selective scission by Ce(iv)-EDTA. The complex formation between the conjugate and DNA was concretely evidenced by spectroscopic results based on time-resolved fluorescence. The target scission site of this new system was straightforwardly determined by the Watson-Crick base pairing rule, and mismatched sequences were clearly discriminated. Importantly, even highly GC-rich regions, which are difficult to be targeted by a previous strategy using pcPNA, were successfully targeted. All these features of the present DNA cutter make it promising for various future applications.

Organic & Biomolecular 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, SDS of cas: 186046-83-3.

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

Certal, Victor published the artcilePreparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors, Related Products of amides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(6), 1506-1510, database is CAplus and MEDLINE.

In the authors’ continuous efforts to identify and develop novel targeted cancer treatments, a new morpholino-thiazole scaffold active against PI3Kβ was identified. This Letter reports the optimization of this compound class to develop PI3Kβ isoform-selective inhibitors with suitable pharmacol. properties.

Bioorganic & Medicinal Chemistry Letters published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Related Products of amides-buliding-blocks.

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

Csanyi, D. published the artcileSynthesis of two new heteroaromatic β-carboline-fused pentacycles. observation of a new intercalating agent, Product Details of C11H16BNO3, the publication is Bioorganic & Medicinal Chemistry Letters (2000), 10(15), 1767-1769, database is CAplus and MEDLINE.

Five-step synthetic routes of two new polyfused heterocycles: indazolo[3,2-a]-ss-carboline (3) and benzo[4′,5′][1,2,3]triazino[6,1-a]-ss-carbolinium salt (10) applying Pd(0)-catalyzed cross-coupling reaction were elaborated.

Bioorganic & Medicinal Chemistry Letters 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, Product Details of C11H16BNO3.

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

Bhat, Tahir Saleem published the artcileSafety and efficacy of ARNI (valsartan/sacubitril) vs ACEI (enalapril) in acute heart failure – A prospective observational study., Synthetic Route of 137862-53-4, the publication is Indian heart journal (2022), 74(3), 178-181, database is MEDLINE.

OBJECTIVE: To compare the safety and efficacy of valsartan/sacubitril (angiotensin receptor neprilysin inhibitor [ARNI]) against enalapril (angiotensin-converting enzyme inhibitor [ACEI]) in patients with acute heart failure at 6-month follow-up. METHODS: In this prospective, single centre, and observational study conducted between September 2017 and February 2020 in India, patients with acute decompensated heart failure with reduced ejection fraction (<40%) were included. Patients were divided in two groups: valsartan/sacubitril (ARNI) group and enalapril (ACEI). Patients were followed up for at least 6 months after administration of first dose and were evaluated for safety, efficacy, and tolerability of target drug. Student’s independent t-test was employed for comparing continuous variables. Chi-square test or Fisher’s exact test, whichever appropriate, was applied for comparing categorical variables. RESULTS: A total of 200 patients were included in the present study, 100 each in ARNI and ACEI group. The mean age of the population was 61.2 ± 8.4 years and 62.6 ± 8.6 years in ARNI group and ACEI group, respectively. The mean maximum tolerated dose by population in ARNI group was 203.6 mg and 8.9 mg in ACEI group. Readmission for heart failure were seen significantly higher in ACEI group than ARNI group (p value = 0.001). Parameters like ejection fraction, left ventricular end diastolic and systolic dimensions, 6 min walk test and Kansas City Cardiomyopathy Questionnaires (KCCQ) showed p values < 0.05 between the groups. CONCLUSION: The ARNI study group showed better safety and efficacy outcomes at the end of 6 months follow-up compared to ACEI group.

Indian heart 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, Synthetic Route of 137862-53-4.

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

Pontiki, Eleni published the artcileHistone deacetylase inhibitors (HDACIs). Structure-activity relationships: history and new QSAR perspectives, HPLC of Formula: 380315-80-0, the publication is Medicinal Research Reviews (2012), 32(1), 1-165, database is CAplus and MEDLINE.

A review. Histone deacetylase (HDAC) inhibition is a recent, clin. validated therapeutic strategy for cancer treatment. HDAC inhibitors (HDACIs) block angiogenesis, arrest cell growth, and lead to differentiation and apoptosis in tumor cells. In this article, a survey of published quant. structure-activity relationships (QSARs) studies are presented and discussed in the hope of identifying the structural determinants for anticancer activity. Secondly a two-dimensional QSAR study was carried out on biol. results derived from various types of HDACIs and from different assays using the C-QSAR program of Biobyte. The QSAR anal. presented here is an attempt to organize the knowledge on the HDACIs with the purpose of designing new chem. entities with enhanced inhibitory potencies and to study the mechanism of action of the compounds This study revealed that lipophilicity is one of the most important determinants of activity. Addnl., steric factors such as the overall molar refractivity (CMR), molar volume (MgVol), the substituent’s molar refractivity (MR) (linear or parabola), or the sterimol parameters B₁ and L are important. Electronic parameters indicated as σ_p, are found to be present only in one case. © 2010 Wiley Periodicals, Inc. Med Res Rev 32:1-165, 2012.

Medicinal Research Reviews published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C20H23N3O2S, HPLC of Formula: 380315-80-0.

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