Month: December 2022

Pejman, Laleh published the artcileThe effect of adenosine A2A and A2B antagonists on tracheal responsiveness, serum levels of cytokines and lung inflammation in guinea pig model of asthma, Formula: C27H29N5O5, the publication is Advanced Pharmaceutical Bulletin (2014), 4(2), 131-138, 8 pp., database is CAplus and MEDLINE.

Nowadays adenosine is specified as an important factor in the pathophysiol. of asthma. For determining the effect of different A2 receptors, in this investigation the effect of single dose of selective adenosine A2A and A2B antagonists (ZM241385 and MRS1706) on different inflammatory parameters; tracheal responsiveness to methacholine and ovalbumin, total and differential cell count in bronchoalveolar lavage (BAL), blood levels of IL-4 and IFN-γ and lung pathol. of guinea pig model of asthma were assessed. All mentioned parameters were evaluated in 2 sensitized groups of guinea pigs pretreated with A2A and A2B antagonists (S+Anta A2A, S+Anta A2B) compared with sensitized (S) and control (C) groups. The tracheal responsiveness to methacholine and OA, total cell and eosinophil and basophil count in BAL, blood IL-4 level and pathol. changes in pretreated group with MRS1706 (S+Anta A2B) was significantly lower than those of sensitized group. In pretreated group with Anta A2A(S+Anta A2A), all the above changes were reversed. These results showed a preventive effect of A2B antagonist (MRS1706) on tracheal responsiveness to methacholine and OA, total and differential cell count in bronchoalveolar lavage, blood cytokines and pathol. changes. Administration of ZM241385, selective A2A antagonist, deteriorated the induction effect of ovalbumin.

Advanced Pharmaceutical Bulletin 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, Formula: C27H29N5O5.

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

Sabeti Azad, Mahnaz published the artcileFluorescent Aminoglycoside Antibiotics and Methods for Accurately Monitoring Uptake by Bacteria, Recommanded Product: 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, the publication is ACS Infectious Diseases (2020), 6(5), 1008-1017, database is CAplus and MEDLINE.

Characterizing how multidrug-resistant bacteria circumvent the action of clin. used or novel antibiotics requires a detailed understanding of how the antibiotics interact with and cross bacterial membranes to accumulate in the cells and exert their action. When monitoring the interactions of drugs with bacteria, it remains challenging to differentiate functionally relevant internalized drug levels from nonspecific binding. Fluorescence is a method of choice for observing dynamics of biomols. In order to facilitate studies involving aminoglycoside antibiotics, we have generated fluorescently labeled aminoglycoside derivatives with uptake and bactericidal activities similar, albeit with a moderate loss, to those of the parent drug. The method combines fluorescence microscopy with fluorescence-activated cell sorting (FACS) using neomycin coupled to nonpermeable cyanine dyes. Fluorescence imaging allowed membrane-bound antibiotic to be distinguished from mols. in the cytoplasm. Patterns of uptake were assigned to different populations in the FACS anal. Our study illustrates how fluorescent derivatives of an aminoglycoside enable a robust characterization of the three components of uptake: membrane binding, EDPI, and EDPII. Because EDPI levels are weak compared to the two other types of accumulation and critical for the action of these drugs, the three components of uptake must be taken into account sep. when drawing conclusions about aminoglycoside function.

ACS Infectious Diseases published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, Recommanded Product: 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide.

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

Odiaka, Timothy I. published the artcileNew tricarbonyl(amido-substituted-1,3-diene)iron complexes, Related Products of amides-buliding-blocks, the publication is Journal of Organometallic Chemistry (1985), 288(2), C30-C32, database is CAplus.

Benzamides I (R = H, 2-OH, 4-MeO, 3-MeO, 3,5-(MeO)₂, 4-Cl, 2,4-Cl₂) added reversibly to the dienyl rings of II (R¹ = H, MeO; n = 1, 2) to give III.

Journal of Organometallic Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Related Products of amides-buliding-blocks.

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

Ogami, Keisuke published the artcileA pot-economical liquid-phase peptide nucleic acid synthesis enabled by a soluble tag-assisted method, Computed Properties of 186046-83-3, the publication is Chemistry Letters (2018), 47(2), 138-140, database is CAplus.

In a peptide nucleic acid (PNA), the base sequences are arranged onto a backbone of repeating units of N-(2-aminoethyl)glycine instead of on phosphodiester-linked riboses. PNA is a promising platform for the design of novel chem. probes because PNAs can form complementary base pairs with DNA and RNA that exhibit high enzymic stability. Described herein is a pot-economical liquid-phase PNA synthesis achieved using a soluble tag-assisted method. Intramol. trapping of the activated PNA monomer occurs much faster than the undesired intermol. “double hit”. Consequently, excess PNA monomers do not have to be rinsed away after each coupling, enabling one-pot coupling and deprotection without the need for precipitation

Chemistry Letters 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, Computed Properties of 186046-83-3.

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

Raza, Shaneabbas published the artcileThe cholesterol metabolite 27-hydroxycholesterol regulates p53 activity and increases cell proliferation via MDM2 in breast cancer cells, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, the publication is Molecular and Cellular Biochemistry (2015), 410(1-2), 187-195, database is CAplus and MEDLINE.

Estrogen is synthesized from cholesterol and high cholesterol levels are suggested to be associated with increased risk of estrogen receptor(ER)-pos. breast cancer. The cholesterol metabolite 27-hydroxycholesterol (27-OHC) was recently identified as a selective estrogen receptor modulator (SERM) and may therefore impact breast cancer progression. However, the mechanisms by which 27-OHC may contribute to breast cancer are not all known. We determined the extent to which 27-OHC regulates cell proliferation in MCF7 ER-pos. breast cancer cell line involving the tumor suppressor protein p53. We found that treatment of MCF7 cells with 27-OHC resulted reduced p53 transcriptional activity. Conversely, treatment of the ER-neg. MDA-MB 231 cells with 27-OHC induced no significant change in p53 activity. Exposure of MCF7 cells to 27-OHC was also associated with increased protein levels of the E3 ubiquitin protein ligase MDM2 and decreased levels of p53. Moreover, 27-OHC also enhanced phys. interaction between p53 and MDM2. Furthermore, 27-OHC-induced proliferation was attenuated using either the p53 activator Tenovin-1 or the MDM2 inhibitor Nutlin-3 and Mdm2 siRNA. Taken together, our results indicate that 27-OHC may contribute to ER-pos. breast cancer progression by disrupting constitutive p53 signaling in an MDM2-dependent manner.

Molecular and Cellular Biochemistry 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, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide.

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

Mukaiyama, Teruaki published the artcileThe effects of substituents on the hydrolysis of substituted cyanamides in sulfuric acid solution, Category: amides-buliding-blocks, the publication is Bulletin of the Chemical Society of Japan (1954), 416-21, database is CAplus.

The following RR’NCN were prepared either from RR’NH and BrCN, or (where R and R’ are the same) from the corresponding halide and Na₂NCN [R, R’, b.p. (mm.) given, resp.]: Et, H, 94-5° (4); Bu, H, 117° (14); n-heptyl, H, nondistillable; iso-Pr, H, 108° (10); tert-Bu, H, 109-10° (11); allyl, H, 92° (3); Ph, H, -, m. 42°; Et, Et, 78° (16); Bu, Bu, 120-1° (16); iso-Pr, iso-Pr, 93-4° (25); allyl, allyl, 107-8° (18); PhCH₂, PhCH₂, m. 53.5°. The hydrolysis of 0.1M solutions of the RR’NCN in 3:1 dioxane-water containing 20% by weight of H₂SO₄ was followed kinetically by contraction in volume, measured with a dilatometer. All of the ureas thus produced were known compounds except N,N-diallylurea, m. 64° (from petr. ether). Tables of rate constants at different temperatures, activation energies, and entropies of activation are given for hydrolysis of the various cyanamides. The rate of reaction increases in the series: (iso-Pr)₂, Et₂, Ph, tert.-Bu, H₂, iso-Pr, Et, heptyl. From these results it is proposed that the rate-determining step in the hydrolysis mechanism is the protonation of the cyanamide bisulfate, RR’NC(:NH)OSO₃H, which is in turn dependent upon the basic strength of the cyanamide. This hypothesis is not in accord with the mechanism proposed by Kilpatrick (C.A. 41, 1916g).

Bulletin of the Chemical Society of Japan published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Category: amides-buliding-blocks.

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

Escobedo, Ericson published the artcileActivation of hydrogen peroxide, persulfate, and free chlorine by steel anode for treatment of municipal and livestock wastewater: Unravelling the role of oxidants speciation, Product Details of C24H29N5O3, the publication is Water Research (2022), 118305, database is CAplus and MEDLINE.

Despite the extensive application of electrochem. advanced oxidation processes (EAOPs) in wastewater treatment, the exact speciation of oxidants and their effects on pollutants removal efficiency, byproducts formation, and effluent toxicity are largely unknown. In this study, galvanostatic steel anodes were used to drive the electrochem. activation of hydrogen peroxide (EAHP), persulfate (EAP), and free chlorine (EAFC), for industrial-scale treatment of municipal and livestock wastewater with a focus on micropollutants and transformation products (MTPs) and effluent toxicity. Response surface methodol. determined the optimized conditions for each treatment towards total organic carbon ([TOC]₀ = 180 mg/L) removal at pH 3.0: persulfate dose = 0.12 mmol/min, 26.5 mA/cm²; free chlorine dose = 0.29 mmol/min, 37.4 mA/cm²; H₂O₂ dose = 0.20 mmol/min, 45 mA/cm². Probe-compound degradation revealed that HO^•, SO^•-₄ and Fe^IVO²⁺ species were simultaneously generated in EAP, whereas HO^• and Fe^IVO²⁺ were the principal oxidants in EAHP and EAFC, resp. Samples were analyzed via liquid and gas chromatog. in non-target screening (NTS) mode to monitor the generation or removal of MTPs and byproducts including compounds that have not been reported previously. The speciation of oxidants, shifted in presence of halide ions (Cl^–, Br^–) in real wastewater samples, significantly affected the mineralization efficiency and byproduct formation. The production of halogenated byproducts in EAFC and EAP substantially increased the effluent toxicity, whereas EAHP provided non-toxic effluent and the highest mineralization efficiency (75 – 80%) to be nominated as the best strategy.

Water Research 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, Product Details of C24H29N5O3.

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

Scott, Ingrid U. published the artcileSCORE2 Report 17: Macular thickness fluctuations in anti-VEGF-treated patients with central or hemiretinal vein occlusion, Application of (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, the publication is Graefe’s Archive for Clinical and Experimental Ophthalmology (2022), 260(5), 1491-1500, database is CAplus and MEDLINE.

To evaluate macular thickness fluctuations and their association with visual acuity outcome in eyes with macular edema (ME) secondary to central (CRVO) or hemiretinal vein occlusion (HRVO) treated initially with intravitreal aflibercept or bevacizumab. Post hoc anal. of 362 patients with ME secondary to CRVO or HRVO initially randomized to six monthly intravitreal injections of aflibercept or bevacizumab. Three spectral domain optical coherence tomog. (SD-OCT) central subfield thickness (CST) fluctuation measures were investigated over Months 1-12: standard deviation (SD), number of turning points (T) for each participant, and a measure denoted as Zigzag reflecting the magnitude of alternating ups and downs in a participant’s CST. Main outcome measure is Month 12 visual acuity letter score (VALS). More fluctuations occurred in eyes randomized to bevacizumab than aflibercept: SD (59.98 vs 32.12; p<0.0001), T (4.03 vs 3.53; p = 0.02) and Zigzag (24.91 vs 11.60; p =0.0003). Month 12 VALS is significantly lower for the 4th (highest) quartile of the CST fluctuation measure than for the 1st (lowest) quartile for both SD (mean difference in VALS of 7.87; 95% confidence interval: 3.03, 12.70) and Zigzag (mean difference in VALS of 5.11; 95% confidence interval: 0.29, 9.93). SD and Zigzag quartiles were no longer significantly different after Month 1 VALS was added to the regression anal. Greater CST fluctuation as assessed by SD and Zigzag was neg. associated with Month 12 VALS. However, early post-treatment VALS is a stronger predictor of VALS outcomes than the CST fluctuation measures.

Graefe’s Archive for Clinical and Experimental Ophthalmology 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 C14H18BClO4, Application of (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

Scott, Ingrid U published the artcileBaseline Characteristics and Outcomes After Anti-Vascular Endothelial Growth Factor Therapy for Macular Edema in Participants With Hemiretinal Vein Occlusion Compared With Participants With Central Retinal Vein Occlusion: Study of Comparative Treatments for Retinal Vein Occlusion 2 (SCORE2) Report 18., COA of Formula: C24H29N5O3, the publication is JAMA ophthalmology (2022), 140(5), 458-464, database is MEDLINE.

Importance: Intravitreal anti-vascular endothelial growth factor (VEGF) injections are commonly used to treat eyes with macular edema secondary to hemiretinal vein occlusion (HRVO) or central retinal vein occlusion (CRVO). Information on whether differences exist in outcomes after anti-VEGF therapy can help guide treatment for each of the different disease types. Objective: To compare baseline characteristics, treatment burden, and outcomes of macular edema treatment in participants with HRVO with those of participants with CRVO. Design, Setting, and Participants: This post hoc outcome analysis from the Study of Comparative Treatments for Retinal Vein Occlusion 2 randomized clinical trial included 362 participants with macular edema caused by HRVO or CRVO treated at 66 US sites. Randomization began in September 2014, and the last month 24 follow-up visit occurred in February 2018. Data were analyzed from April 2020 to May 2021. Interventions: Eyes were initially randomized to 6 monthly intravitreal injections of aflibercept or bevacizumab and were treated according to protocol between months 6 to 12 depending on 6-month outcome. After month 12, patients were treated per investigator discretion and observed through month 60. Main Outcomes and Measures: Mean visual acuity letter score (VALS). Results: Of 362 included patients, 157 (43.4%) were female, and the mean (SD) age was 68.9 (12.0) years. Outcome data were analyzed up to month 24 owing to substantial missing data at later visits. A significantly greater proportion of participants with HRVO than those with CRVO were Black (37% vs 11%). Treatment rates between months 12 to 23 were 0.36 (95% CI, 0.32-0.40) injections per month for patients with CRVO and 0.28 (95% CI, 0.19-0.36) for patients with HRVO (P = .11). The mean VALS from months 1 to 24 of an HRVO study eye exceeded that of a CRVO study eye by 5.5 (95% CI, 1.5-9.5; P = .01), consistent with the magnitude of the VALS difference between eyes with CRVO and HRVO at baseline. Eyes with CRVO presented at baseline with more macular edema than eyes with HRVO (difference in central subfield thickness [CST], 86 μm; 95% CI, 48-124; P < .001), with no difference in CST between the groups throughout months 1 to 24. Conclusions and Relevance: Black race was more prevalent among participants with HRVO than CRVO, and no differences were observed in the frequency of treatments for macular edema between eyes with CRVO and HRVO. Although eyes with CRVO presented with worse visual acuity and more macular edema on average than did eyes with HRVO, the magnitude of VALS improvement, central retinal thickness in response to anti-VEGF therapy, and treatment burden were similar between the groups.

JAMA ophthalmology 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 C14H18BClO4, COA of Formula: C24H29N5O3.

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

Jonczyk, Andrzej published the artcileReactions of organic anions; LXXXV. Catalytic two-phase alkylation of cyanamide, Name: N,N-Dibenzylcyanamide, the publication is Synthesis (1978), 882-3, database is CAplus.

R₂NCN (R = PhCH₂, H₂C:CHCH₂, Bu, Et, Me₂CHCH₂CH₂, Me₂CH, Me, MeOCH₂, BuOCH₂) were prepare by reaction of H₂NCN with RX (X = Cl, Br) in presence of Aliquat 336. The heterocycles I [Q = (CH₂)_n, n = 2, 3, 4; o-C₆H₄] were similarly prepared from H₂NCN and BrCH₂QCH₂Br.

Synthesis published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Name: N,N-Dibenzylcyanamide.

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