Month: December 2022

Haddad, Ibrahim published the artcilePoly(arylene sulfides) with pendant cyano groups as high-temperature laminating resins. II, Application of 2,4-Dichlorobenzamide, the publication is Journal of Polymer Science, Polymer Chemistry Edition (1974), 12(6), 1301-11, database is CAplus.

The phys. properties were studied of poly(phenylene sulfides) prepared from m-benzenedithiol and p-C6H4Br2, 2,4- or 3,5-dichlorobenzonitrile, optionally selfcrosslinked or crosslinked with anthracene-9,10-bisnitrile oxide [30862-16-9]. Nitrile-containing binary copolymers had higher m.p.s than other copolymers.

Journal of Polymer Science, Polymer Chemistry Edition 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, Application of 2,4-Dichlorobenzamide.

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

Xiao, Jingbo published the artcileDiscovery, Synthesis, and Biological Evaluation of Novel SMN Protein Modulators, Recommanded Product: Morpholine-4-carbothioamide, the publication is Journal of Medicinal Chemistry (2011), 54(18), 6215-6233, database is CAplus and MEDLINE.

Spinal muscular atrophy (SMA) is an autosomal recessive disorder affecting the expression or function of survival motor neuron protein (SMN) due to the homozygous deletion or rare point mutations in the survival motor neuron gene 1 (SMN1). The human genome includes a second nearly identical gene called SMN2 that is retained in SMA. SMN2 transcripts undergo alternative splicing with reduced levels of SMN. Up-regulation of SMN2 expression, modification of its splicing, or inhibition of proteolysis of the truncated protein derived from SMN2 have been discussed as potential therapeutic strategies for SMA. In this manuscript, the discovery of a series of arylpiperidines as novel modulators of SMN protein is described. Systematic hit-to-lead efforts significantly improved potency and efficacy of the series in the primary and orthogonal assays. Structure-property relationships including microsomal stability, cell permeability, and in vivo pharmacokinetics were also investigated. In consideration to all the aspects including ADME properties, the analogs I (X = NH₂, R = 3-i-PrOC₆H₄; X = OH, R = 3,4-dihydro-2H-benzo[b][1,4]dioxepin-7-yl) possessed the best combination of potency, efficacy, mouse liver microsomal stability and cell permeability as well as good oral absorption and CNS penetration upon oral gavage administration. These compounds also showed no sign of toxicity or behavioral disturbance in animals.

Journal of Medicinal Chemistry 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 C12H10N2O5, Recommanded Product: Morpholine-4-carbothioamide.

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

Thompson, Patricia A published the artcileThe Importance of Drug Concentration at the Site of Action: Celecoxib and Colon Polyp Prevention as a Case Study., Product Details of C17H14F3N3O2S, the publication is Cancer prevention research (Philadelphia, Pa.) (2022), 15(4), 205-208, database is MEDLINE.

Celecoxib is among the more potent and better clinically studied, nonsteroidal anti-inflammatory drugs (NSAID) for use as a chemoprevention agent for colorectal cancer. Its use is associated with a 40% to 50% response rate for reduction in adenomatous polyps. However, rare serious cardiovascular effects and even death with celecoxib and other NSAIDs make it important to understand why some patients respond and others do not. Celecoxib is a selective inhibitor of COX-2. Its anticancer mechanism has largely been attributed to the inhibition of COX-2. Celecoxib also shows activity to induce apoptosis in cancer cells not expressing COX-2. This includes activity to upregulate 15-lipoxygenase-1 (15-LOX-1) independent of COX-2 and increase the synthesis of 13-S-hydroxyoctadecadienoic acid (13-S-HODE) from linoleic acid (LA) to downregulate PPAR-δ and induce apoptosis in colorectal cancer models. In examining the effect of celecoxib on 15-LOX-1 for reducing adenomatous polyps in patients with familial adenomatous polyposis (FAP), Yang and colleagues point out the potential importance of drug bioavailability in blood, normal, and neoplastic colorectal tissue in patient response. See related article, p. 217.

Cancer prevention research (Philadelphia, Pa.) 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 C4H6N2, Product Details of C17H14F3N3O2S.

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

Roseti, Cristina published the artcileAdenosine receptor antagonists alter the stability of human epileptic GABA_A receptors, COA of Formula: C27H29N5O5, the publication is Proceedings of the National Academy of Sciences of the United States of America (2008), 105(39), 15118-15123, database is CAplus and MEDLINE.

We examined how the endogenous anticonvulsant adenosine might influence γ-aminobutyric acid type A (GABA_A) receptor stability and which adenosine receptors (ARs) were involved. Upon repetitive activation (GABA 500 μM), GABA_A receptors, microtransplanted into Xenopus oocytes from neurosurgically resected epileptic human nervous tissues, exhibited an obvious GABA_A-current (I_GABA) run-down, which was consistently and significantly reduced by treatment with the nonselective adenosine receptor antagonist CGS15943 (100 nM) or with adenosine deaminase (ADA) (1 units/mL), that inactivates adenosine. It was also found that selective antagonists of A2B (MRS1706, 10 nM) or A3 (MRS1334, 30 nM) receptors reduced I_GABA run-down, whereas treatment with the specific A1 receptor antagonist DPCPX (10 nM) was ineffective. The selective A2A receptor antagonist SCH58261 (10 nM) reduced or potentiated IGABA run-down in ≈40% and ≈20% of tested oocytes, resp. The ADA-resistant, AR agonist 2-chloroadenosine (2-CA) (10 μM) potentiated I_GABA run-down but only in ≈20% of tested oocytes. CGS15943 administration again decreased I_GABA run-down in patch-clamped neurons from either human or rat neocortex slices. I_GABA run-down in pyramidal neurons was equivalent in A1 receptor-deficient and wt neurons but much larger in neurons from A2A receptor-deficient mice, indicating that, in mouse cortex, GABA_A-receptor stability is tonically influenced by A2A but not by A1 receptors. I_GABA run-down from wt mice was not affected by 2-CA, suggesting maximal ARs activity by endogenous adenosine. Our findings strongly suggest that cortical A2-A3 receptors alter the stability of GABA_A receptors, which could offer therapeutic opportunities.

Proceedings of the National Academy of Sciences of the United States of America 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, COA of Formula: C27H29N5O5.

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

Rocca, Patrick published the artcileA short synthesis of the antimicrobial marine sponge pigment fascaplysine, Application of (2-Pivalamidophenyl)boronic acid, the publication is Tetrahedron Letters (1993), 34(49), 7917-18, database is CAplus.

A short and convergent synthesis of fascaplysine (I) was achieved from 3-fluoro-4-iodopyridine and 2-Me₃CCONHC₆H₄B(OH)₂ in 4 steps and 76% overall yield. The approach is based on recently developed methodol. including metalation, hetero cross-coupling and cyclization.

Tetrahedron 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, Application of (2-Pivalamidophenyl)boronic acid.

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

Rocca, Patrick published the artcileConnection between metalation and cross-coupling strategies. A new convergent route to azacarbazoles, Product Details of C11H16BNO3, the publication is Tetrahedron (1993), 49(1), 49-64, database is CAplus.

New convergent synthesis of azacarbazoles through metalation, cross-coupling reaction, and intramol. substitution via (2-aminobenzene)boronic acid and ortho-fluoroiodopyridines are presented. Thus, 2-(HO)₂BC₆H₄NHCOCMe₃ coupled with pyridines I (X = F, Cl, Y = iodo, Z = H; X = H, Y = F, Z = iodo; X = H, Y = iodo, Z = F; X = iodo, Y = F, Z = H) to give the corresponding (pyridylphenyl)propanamides II (R = F, Cl). The 3-fluoro-4-pyridyl derivative of II was treated with pyridinium chloride under reflux to give β-carboline III. The α-, γ-, and δ-carbolines were prepared similarly.

Tetrahedron 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

Rocca, P. published the artcileA new convergent synthesis of substituted β-carbolines, Category: amides-buliding-blocks, the publication is Tetrahedron (1993), 49(16), 3325-42, database is CAplus.

New convergent synthesis of natural α-substituted-β-carbolines, e.g. I (R = Ph, 2-pyridyl, Me, 2-quinolinyl) through metalations, cross-couplings and intramol. substitution via (2-aminobenzene)boronic acid, arylstannanes and 3,4-fluoroiodopyridines was achieved. Thus, 2,2-dimethyl-N-[2-(2-chloro-3-fluoro-4-pyridyl)phenyl]propanamide (II, R = Cl), prepared in 3 steps form 3-amino-2-chloropyridine, was coupled with 2-(trimethylstannyl)quinoline to give II (R = 2-quinolinyl), which was cyclized by treatment with pyridinium chloride to give I (R = 2-quinolinyl).

Tetrahedron 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, Category: amides-buliding-blocks.

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

Mayhoub, Abdelrahman S. published the artcileOptimizing thiadiazole analogues of resveratrol versus three chemopreventive targets, Application of 3-Methoxybenzothioamide, the publication is Bioorganic & Medicinal Chemistry (2012), 20(1), 510-520, database is CAplus and MEDLINE.

Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biol. targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-κB and inducers of quinone reductase 1 (QR1).

Bioorganic & Medicinal 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 C8H9NOS, Application of 3-Methoxybenzothioamide.

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

Mayhoub, Abdelrahman S. published the artcileOptimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1), Name: 3-Methoxybenzothioamide, the publication is Bioorganic & Medicinal Chemistry (2012), 20(24), 7030-7039, database is CAplus and MEDLINE.

NAD(P)H:quinone reductase 1 (QR1) belongs to a class of enzymes called cytoprotective enzymes. It exhibits its cancer protective activity mainly by inhibiting the formation of intracellular semiquinone radicals, and by generating α-tocopherolhydroquinone, which acts as a free radical scavenger. It is therefore believed that QR1 inducers can act as cancer chemopreventive agents. Resveratrol (1) is a naturally occurring stilbene derivative that requires a concentration of 21 μM to double QR1 activity (CD = 21 μM). The stilbene double bond of resveratrol was replaced with a thiadiazole ring and the phenols were eliminated to provide a more potent and selective derivative 2 (CD = 2.1 μM). Optimizing the substitution pattern of the two Ph rings and the central heterocyclic linker led to a highly potent and selective QR1 inducer 9o with a CD value of 0.087 μM.

Bioorganic & Medicinal 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 C8H9NOS, Name: 3-Methoxybenzothioamide.

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

Mayhoub, Abdelrahman S. published the artcileOptimizing thiadiazole analogues of resveratrol versus three chemopreventive targets, Name: 2,4-Dichlorobenzamide, the publication is Bioorganic & Medicinal Chemistry (2012), 20(1), 510-520, database is CAplus and MEDLINE.

Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biol. targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-κB and inducers of quinone reductase 1 (QR1).

Bioorganic & Medicinal 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, Name: 2,4-Dichlorobenzamide.

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