Category: amides-buliding-blocks

Wang, Sen-Lin published the artcileSynthesis and bioactivity of novel pyrazole oxime derivatives containing oxazole ring, Formula: C7H5Cl2NO, the publication is Chinese Chemical Letters (2015), 26(6), 672-674, database is CAplus.

A series of novel pyrazole oxime derivatives containing oxazole ring were designed and synthesized. The title compounds were structurally confirmed by ¹H NMR, ¹³C NMR spectra and elemental analyses. Preliminary bioassay results showed that some of the title compounds displayed promising fungicidal activity besides insecticidal and acaricidal activity. Particularly, compound 8c exhibited potent fungicidal activity against cucumber Pseudoperonospora cubensis beyond good insecticidal activity against Aphis craccivora and Nilaparvata lugens.

Chinese Chemical Letters 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 C25H47NO8, Formula: C7H5Cl2NO.

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

Metcalf, Gavin A. D. published the artcileAmplification-Free Detection of Circulating microRNA Biomarkers from Body Fluids Based on Fluorogenic Oligonucleotide-Templated Reaction between Engineered Peptide Nucleic Acid Probes: Application to Prostate Cancer Diagnosis, Computed Properties of 186046-83-3, the publication is Analytical Chemistry (Washington, DC, United States) (2016), 88(16), 8091-8098, database is CAplus and MEDLINE.

Highly abundant in cells, microRNAs (or miRs) play a key role as regulators of gene expression. A proportion of them are also detectable in biofluids making them ideal noninvasive biomarkers for pathologies in which miR levels are aberrantly expressed, such as cancer. Peptide nucleic acids (PNAs) are engineered uncharged oligonucleotide analogs capable of hybridizing to complementary nucleic acids with high affinity and high specificity. Herein, novel PNA-based fluorogenic biosensors have been designed and synthesized that target miR biomarkers for prostate cancer (PCa). The sensing strategy is based on oligonucleotide-templated reactions where the only miR of interest serves as a matrix to catalyze an otherwise highly unfavorable fluorogenic reaction. Validated in vitro using synthetic RNAs, these newly developed biosensors were then shown to detect endogenous concentrations of miR in human blood samples without the need for any amplification step and with minimal sample processing. This low-cost, quant., and versatile sensing technol. has been tech. validated using gold-standard RT-qPCR. Compared to RT-qPCR however, this enzyme-free, isothermal blood test is amenable to incorporation into low-cost portable devices and could therefore be suitable for widespread public screening.

Analytical Chemistry (Washington, DC, United States) 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

Tanaka, Masayoshi published the artcileAdenosine A_2B receptor down-regulates metabotropic glutamate receptor 5 in astrocytes during postnatal development, HPLC of Formula: 264622-53-9, the publication is Glia (2021), 69(11), 2546-2558, database is CAplus and MEDLINE.

Metabotropic glutamate receptor 5 (mGluR5) in astrocytes is a key mol. for controlling synapse remodeling. Although mGluR5 is abundant in neonatal astrocytes, its level is gradually down-regulated during development and is almost absent in the adult. However, in several pathol. conditions, mGluR5 re-emerges in adult astrocytes and contributes to disease pathogenesis by forming uncontrolled synapses. Thus, controlling mGluR5 expression in astrocyte is critical for several diseases, but the mechanism that regulates mGluR5 expression remains unknown. Here, we show that ATP (ATP)/adenosine-mediated signals down-regulate mGluR5 in astrocytes. First, in situ Ca2+ imaging of astrocytes in acute cerebral slices from post-natal day (P)7-P28 mice showed that Ca2+ responses evoked by (S)-3,5-dihydroxyphenylglycine (DHPG), a mGluR5 agonist, decreased during development, whereas those evoked by ATP or its metabolite, adenosine, increased. Second, ATP and adenosine suppressed expression of the mGluR5 gene, Grm5, in cultured astrocytes. Third, the decrease in the DHPG-evoked Ca2+ responses was associated with down-regulation of Grm5. Interestingly, among several adenosine (P1) receptor and ATP (P2) receptor genes, only the adenosine A2B receptor gene, Adora2b, was up-regulated in the course of development. Indeed, we observed that down-regulation of Grm5 was suppressed in Adora2b knockout astrocytes at P14 and in situ Ca2+ imaging from Adora2b knockout mice indicated that the A2B receptor inhibits mGluR5 expression in astrocytes. Furthermore, deletion of A2B receptor increased the number of excitatory synapse in developmental stage. Taken together, the A2B receptor is critical for down-regulation of mGluR5 in astrocytes, which would contribute to terminate excess synaptogenesis during development.

Glia 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 C14H31NO2, HPLC of Formula: 264622-53-9.

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

Rossi, Steven A. published the artcileSelective Formation of Secondary Amides via the Copper-Catalyzed Cross-Coupling of Alkylboronic Acids with Primary Amides, Category: amides-buliding-blocks, the publication is Organic Letters (2013), 15(9), 2314-2317, database is CAplus and MEDLINE.

For the first time, a general catalytic procedure for the cross-coupling of primary amides and alkylboronic acids is demonstrated. The key to the success of this reaction was the identification of a mild base (NaOSiMe₃) and oxidant (di-tert-Bu peroxide) to promote the copper-catalyzed reaction in high yield. This transformation provides a facile, high-yielding method for the monoalkylation of amides.

Organic Letters 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, Category: amides-buliding-blocks.

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

Suzuki, Hirotsugu published the artcileDealkoxylation of N-alkoxyamides without an external reductant driven by Pd/Al cooperative catalysis, Synthetic Route of 100377-32-0, the publication is Organic & Biomolecular Chemistry (2020), 18(38), 7545-7548, database is CAplus and MEDLINE.

Lewis acid-assisted palladium-catalyzed dealkoxylation of N-alkoxyamides has been developed. This reaction proceeded smoothly with a range of N-alkoxyamides in the absence of an external reductant, thereby establishing a convenient and reductant-free protocol. In addition, a gram-scale reaction could be achieved. Preliminary mechanistic investigations indicated that β-hydrogen elimination from a palladium alkoxide intermediate generated an intramol. hydride source.

Organic & Biomolecular Chemistry 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 C9H9BrO2, Synthetic Route of 100377-32-0.

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

Shimbori, Chiko published the artcileInvolvement of leukotrienes in the pathogenesis of silica-induced pulmonary fibrosis in mice, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Experimental Lung Research (2010), 36(5), 292-301, database is CAplus and MEDLINE.

The authors investigated the role of leukotrienes (LTs) in the pathogenesis of silica-induced pulmonary fibrosis in mice during the progression from acute to chronic phases. Intratracheal instillation of silica particles induced progressive pulmonary fibrosis. The tissue content of cysteinyl (Cys) LTs and LTB₄ was markedly increased in the acute phase after silica instillation, concurrently with the up-regulation of LTB₄ receptor, transforming growth factor (TGF)-β1, and tumor necrosis factor (TNF)-α, along with down-regulation of the CysLT type 2 receptor. Importantly, the tissue content of CysLTs and mRNA levels of TGF-β1 and TNF-α were increased in the fibrotic lung in the chronic phase. Furthermore, strong immunohistochem. staining for the CysLT type 1 receptor, TNF-α, and TGF-β1, but not for the CysLT type 2 receptor, was codetected in the pathol. lesions during both acute and chronic phases. These findings suggest that an increase in LT production in the lung and modulation of homeostatic balance among LT receptors may contribute to the progression of pulmonary fibrosis.

Experimental Lung Research 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 C8H11BO2, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

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

Devani, M. B. published the artcileSynthesis and pharmacological properties of some 4-amino-5-substituted thiazole-2(3H)-thiones and thiazolo(4,5-d)pyrimidin-7(6H)-one-2(3H)-thiones, Recommanded Product: 2-Cyano-N-ethylacetamide, the publication is Arzneimittel-Forschung (1977), 27(9), 1652-5, database is CAplus and MEDLINE.

Twenty-six aminothiazolethiones I (R = Et, benzyl, allyl, Ph, tolyl, etc.; R1 = NH2, NHMe, piperidino, morpholino, PhNHNH) were prepared in 40-90% yield by reaction of RNCS with NCCH2CONHR1. Eleven thiazolopyrimidinones II (R = benzyl, tolyl, Ph, Me, Et, R2 = H, Me, Et, Ph, anilino) were prepared in 55-70% yield by reaction of the appropriate I with HC(OEt)2 in Ac2O. I and II were screened for antimicrobial and pharmacol. activities. Maximum antiinflammatory activity was found in I (R = o-tolyl, R1 = morpholino); at 200 mg/kg its activity was almost equal to phenylbutazone at 100 mg/kg. I (R = allyl, R1 = PhNHNH) was the most active antimicrobial of the series. I (R = benzyl, R1 = NH2) was the most potent analgesic.

Arzneimittel-Forschung 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, Recommanded Product: 2-Cyano-N-ethylacetamide.

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

Devani, M. B. published the artcileSynthesis of 2-aminothiophenes and thieno[2,3-d]pyrimidines, Safety of 2-Cyano-N-ethylacetamide, the publication is Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (1976), 14B(5), 357-60, database is CAplus.

The thienopyrimidinones I [R = Me, R1 = CO2Et, R2 = H; RR1 = (CH2)4, R2 = Ph] were prepared by treating the aminothiophenes II (R = CO2Et, CONHPh) with HCONH2 or (EtO)3CH, whereas cyclization of II [R = Me, R1 = EtO2C, R3 = cyano; RR1 = (CH2)4, R3 = cyano] with HCONH2 gave the corresponding aminothienopyrimidines III. Furthermore, the spiro[benzothienopyrimidine-2,1′-cyclohexane] IV was prepared by cyclization of NCCH2CONHNHPh with cyclohexanone in the presence of S. IV had antiinflammatory and anticonvulsant activities and II had only antiinflammatory activity.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry 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, Safety of 2-Cyano-N-ethylacetamide.

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

Xu, Liang published the artcileOxidative cyclization of N-alkyl-o-methyl-arenesulfonamides to biologically important saccharin derivatives, Application of 4-Fluoro-2-methylbenzenesulfonamide, the publication is Tetrahedron (2006), 62(33), 7902-7910, database is CAplus.

Various biol. important saccharin skeletons and their N-alkyl derivatives were efficiently prepared by Cr(VI) oxide-catalyzed H₅IO₆ oxidation of N-alkyl-o-methyl-arenesulfonamides in MeCN. N-tert-Bu saccharin skeletons were easily prepared by H₅IO₆-CrO₃ oxidation of N-tert-butyl-o-Me arenesulfonamides in the presence of acetic anhydride. The method that furnished the novel fluoro- and trifluoromethyl-substituted saccharin skeletons was characterized by two steps, a simple work-up procedure, a single purification and good overall yields from substituted toluene derivatives For example, 58 % 2-tert-butyl-6-trifluoromethyl-1,2-benzisothiazol-3-one 1,1-dioxide was obtained from 1-methyl-4-(trifluoromethyl)benzene.

Tetrahedron published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C17H20ClN3, Application of 4-Fluoro-2-methylbenzenesulfonamide.

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

Dettin, Monica published the artcileSynthesis and chromatography-free purification of PNA-PEO conjugates for the functionalisation of gold sensors, 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 Molecules (2012), 11026-11045, database is CAplus and MEDLINE.

Peptide Nucleic Acids (PNAs) linked to high mol. weight (MW) poly(ethylene oxide) (PEO) derivatives could be useful conjugates for the direct functionalisation of gold surfaces dedicated to Surface Plasmon Resonance (SPR)-based DNA sensing. However their use is hampered by the difficulty to obtain them through a convenient and economical route. In this work we compared three synthetic strategies to obtain PNA-high MW PEO conjugates composed of (a) a 15-mer PNA sequence as the probe complementary to genomic DNA of Mycobacterium tuberculosis, (b) a PEO moiety (2 or 5 KDa MW) and (c) a terminal trityl-protected thiol necessary (after acidic deprotection) for grafting to gold surfaces. The 15-mer PNA was obtained by solid-phase synthesis. Its amino terminal group was later condensed to bi-functional PEO derivatives (2 and 5 KDa MW) carrying a Trt-cysteine at one end and a carboxyl group at the other end. The reaction was carried out either in solution, using HATU or PyOxim as coupling agents or through the solid-phase approach, with 49.6%, 100% and 5.2% yield, resp. A differential solvent extraction strategy for product purification without the need for chromatog. is described. The ability of the 5 KDa PEO conjugate to function as a probe for complementary DNA detection was demonstrated using a Grating-Coupling Surface Plasmon Resonance (GC-SPR) system. The optimized PEO conjugation and purification protocols are economical and simple enough to be reproduced also within laboratories that are not highly equipped for chem. synthesis.

Molecules 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