Month: December 2022

Hall, David Ross published the artcileMonohaloacetic Acids and Monohaloacetamides Attack Distinct Cellular Proteome Thiols, Recommanded Product: 2-Chloroacetamide, the publication is Environmental Science & Technology (2020), 54(23), 15191-15201, database is CAplus and MEDLINE.

Disinfection byproduct (DBP) exposure has been linked to multiple adverse health outcomes. However, the mol. initiating events by which DBPs induce their toxicities remain unclear. Herein, we combined reporter cell lines and activity-based protein profiling (ABPP) chem. proteomics to identify the protein targets of three monohaloacetic acids (mHAAs) and three monohaloacetamides (mHAMs), at the proteome-wide level. While mHAAs and mHAMs have similar potencies in reducing MTT activity, mHAMs induced greater Nrf2-mediated oxidative stress responses, demonstrating their distinct toxicity pathways. ABPP on crude cell lysates suggested that general proteome thiol reactivity correlates with cytotoxicity. Interestingly, live cell ABPP results revealed class-specific proteins attacked by mHAMs or mHAAs. Subsequent proteomic anal. identified >100 unique targets per DBP. mHAMs preferentially react with redox proteins including disulfide oxidoreductase enzymes, accounting for their stronger Nrf2 responses. To further probe alkylation mechanisms, we directly monitored protein adducts and identified 120 and 37 unique peptides with iodoacetamide and iodoacetic acid adducts, resp. Of the latter, we confirmed glyceraldehyde-3-phosphate dehydrogenase as a key target of IAA, specifically attacking the catalytic Cys 152. This is the first study reporting the distinct cellular protein targets of mHAAs and mHAMs at the proteome-wide level, which highlights their different toxicity pathways despite their similar structures.

Environmental Science & Technology 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 C2H4ClNO, Recommanded Product: 2-Chloroacetamide.

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

Lin, Yu-Wei published the artcileImprovement After Celecoxib Treatment in Patients with Thalamic Hemorrhage – A Case Report., Name: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Acta neurologica Taiwanica (2022), 84-89, database is MEDLINE.

PURPOSE: Perihematomal edema of intracerebral hemorrhage (ICH) is caused by a hematoma-induced inflammatory reaction, which usually contributes to delayed deterioration of neurological function and poor outcomes. Celecoxib is a commonly used nonsteroidal anti-inflammatory drug that selectively inhibits cyclooxygenase-2. High-dose celecoxib (400 mg twice daily) for 14 days has been shown to reduce perihematomal edema and hematoma enlargement in patients with ICH, but without improvement in long-term functional outcome, which may be confounded by the heterogeneity of hematoma location. Low-dose celecoxib may be an effective management for symptoms caused by perihematomal edema in patients with ICH, particularly those involving the thalamus. CASE REPORT: We reported two patients with acute thalamic ICH; a common symptom between the two was delayed onset of drowsiness caused by perihematomal edema involving the thalamus. Their consciousness improved after low-dose celecoxib (200 mg once daily) administration for 3 and 2 days in case A and B, respectively. Furthermore, other symptoms that concomitantly improved included poor appetite caused by perihematomal edema involving the left hypothalamus in case A, and limb weakness caused by perihematomal edema of the internal capsule in case B. CONCLUSION: These cases revealed that low-dose celecoxib may be an effective management for symptoms caused by perihematomal edema in patients with ICH, particularly those involving the thalamus.

Acta neurologica Taiwanica 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, Name: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

Shaik, Jeelan Basha published the artcileSynthesis and biological evaluation of flavone-8-acrylamide derivatives as potential multi-target-directed anti Alzheimer agents and investigation of binding mechanism with acetylcholinesterase, Related Products of amides-buliding-blocks, the publication is Bioorganic Chemistry (2019), 102960, database is CAplus and MEDLINE.

In a search for novel multifunctional anti-Alzheimer agents, a congeneric set of seventeen flavone-8-acrylamide derivatives (8a-q) were synthesized and evaluated for their cholinesterase inhibitory, antioxidant, neuroprotective and modulation of Aβ aggregation activities. The target compounds showed effective and selective inhibitory activity against the AChE over BuChE. In addition, the target compounds also showed moderate anti-oxidant activity and strong neuroprotective capacities, and accelerated dosage-dependently the Aβ aggregation. Also, we presented here a complete study on the interaction of 8a, 8d, 8e, 8h and 8i (I; NR₁R₂ correspond to methanamine, cyclopropamine, cyclohexamine, benzenemethanamine, and α-methylbenzenemethanamine, resp.) with AChE. Through fluorescence emission studies, the binding sites number found to be 1, binding constants were calculated as 2.04 × 10⁴, 2.22 × 10⁴, 1.18 × 10⁴, 9.8 × 10³ and 3.2 × 10⁴ M^-1 and free energy change as -5.83, -5.91, -5.51, -5.41 and -6.12 kcal M^-1 at 25 °C which were well agreed with the computational calculations indicating a strong binding affinity of flavones and AChE. Furthermore, the CD studies revealed that the secondary structure of AChE became partly unfolded upon binding with I.

Bioorganic 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 C7H5ClN2S, Related Products of amides-buliding-blocks.

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

Mallikarjuna, Rangisetty published the artcileSynthesis and biological evaluation of some new 3-cyano-2-amino substituted chromene derivatives, Recommanded Product: 2-Cyano-N-ethylacetamide, the publication is Pharma Chemica (2015), 7(11), 117-129, database is CAplus.

Chromenes are the one of the important class of heterocyclic compounds which poses wide range of pharmaceutical and biol. importance. Different functional groups at different positions in the core structure of chromene deliberately yields novel derivatives which play a prominent role in in the field of medicinal chem. One pot synthesis of a few new series of 2-amino-3-cyano-4H-chromene derivatives were designed, synthesized, characterized and biol. activity like anti-bacterial and anti-fungal studies were screened, where most of the compounds showed good growth inhibition activity.

Pharma Chemica 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

Hu, Jingyan published the artcileAmidation Reaction of Quinoline-3-carboxylic Acids with Tetraalkylthiuram Disulfides under Simple Conditions: A facile Synthesis of Quinoline-3-carboxamides, SDS of cas: 530-40-5, the publication is Asian Journal of Organic Chemistry (2020), 9(12), 2191-2195, database is CAplus.

A highly efficient and simple procedure for the synthesis quinoline-3-carboxamides and their analogs via amidation reaction of quinoline-3-carboxylic acids with tetraalkylthiuram disulfides was developed. The reaction proceeded efficiently under simple reaction conditions and featured the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for the synthesis of various aza-heteroaromatic carboxamides, which is of pharmaceutical interest.

Asian Journal of Organic Chemistry published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, SDS of cas: 530-40-5.

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

Li, Qilan published the artcileZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A_2B receptor, Recommanded Product: N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide, the publication is Journal of Pharmacology and Experimental Therapeutics (2007), 320(2), 637-645, database is CAplus and MEDLINE.

The human adenosine A_2B receptor belongs to class A G protein-coupled receptors (GPCRs). In our previous work, constitutively active mutant (CAM) human adenosine A_2B receptors were identified from a random mutation bank. In the current study, three known A_2B receptor antagonists, 4-{2-[7-amino-2-(2-furyl)[1,2,4]triazolo-[2,3-a][1,3,5]triazin-5-yl-amino]ethyl}phenol (ZM241385), 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), and N-(4-acetylphenyl)-2-[4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)phenoxy]acetamide (MRS1706) were tested on wild-type and nine CAM A_2B receptors with different levels of constitutive activity in a yeast growth assay. All three compounds turned out to be inverse agonists for the adenosine A_2B receptor because they were able to fully reverse the basal activity of four low-level constitutively active A_2B receptor mutants and to partially reverse the basal activity of three medium-level constitutively active A_2B receptor mutants. We also discovered two highly constitutively active mutants whose basal activity could not be reversed by any of the three compounds A two-state receptor model was used to explain the exptl. observations; fitting these yielded the following relative intrinsic efficacies for the three inverse agonists ZM241385, DPCPX, and MRS1706: 0.14±0.03, 0.35±0.03, and 0.31±0.02, resp. Moreover, varying L, the ratio of active vs. inactive receptors in this model, from 0.11 for mutant F84L to 999 for two highly constitutively active mutants yielded simulated dose-response curves that mimicked the exptl. curves. This study is the first description of inverse agonists for the human adenosine A_2B receptor. Moreover, the use of receptor mutants with varying levels of constitutive activity enabled us to determine the relative intrinsic efficacy of these inverse agonists.

Journal of Pharmacology and Experimental Therapeutics 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, Recommanded Product: N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide.

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

Shemesh, Yossi published the artcilePNA-Rose Bengal Conjugates as Efficient DNA Photomodulators, SDS of cas: 186046-83-3, the publication is Bioconjugate Chemistry (2015), 26(9), 1916-1922, database is CAplus and MEDLINE.

Selective photoinduced modulation of DNA may provide a powerful therapeutic tool allowing spatial and temporal control of the photochem. reaction. We have explored the photoreactivity of peptide nucleic acid (PNA) conjugates that were conjugated to a highly potent photosensitizer, Rose Bengal (RB). In addition, a short PEGylated peptide (K-PEG₈-K) was conjugated to the C-terminus of the PNA to improve its water solubility A short irradiation (visible light) of PNA conjugates with a synthetic DNA resulted in highly efficient photomodulation of the DNA as evidenced by polyacrylamide gel electrophoresis (PAGE). In addition, a PNA-RB conjugate replacing K-PEG₈-K with four L-glutamic acids (E₄) was found to be photoinactive. Irradiation of active PNA-RB conjugates with synthetic DNA in D₂0 augments the photoactivity; supporting the involvement of singlet oxygen. PAGE, HPLC, and MALDI-TOF analyses indicate that PNA-DNA photo-crosslinking is a significant pathway in the observed photoreactivity. Selective photo-crosslinking of such PNA-RB conjugates may be a novel approach to selective photodynamic therapy (sPDT) as such mols. would be sequence-specific, cell-permeable, and photoactivated in the visible region.

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 C13H16O2, SDS of cas: 186046-83-3.

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

Savvina, L. N. published the artcileDibenzylamine, Formula: C15H14N2, the publication is Metody Polucheniya Khimicheskikh Reaktivov i Preparatov (1964), 28-9, database is CAplus.

Hydrolysis of (PhCH₂)₂NCN (I) with 40% H₂SO₄ yielded (PhCH₂)₂NH (II). A mixture of 68 ml. 40% H₂SO₄ and 0.1 mole I was heated 5 hrs. at 140°, cooled to 30-40°, 26 ml. 40% H₂SO₄ added, the mixture heated 3 hrs. at 140°, cooled, and ∼1 mole 40% NaOH added dropwise to weak alkalinity The oil was removed and the alk. solution extracted with CHCl₃ to yield 66-70% II, b. 298-300°.

Metody Polucheniya Khimicheskikh Reaktivov i Preparatov 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, Formula: C15H14N2.

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

Savvina, L. N. published the artcileDibenzylcyanamide, COA of Formula: C15H14N2, the publication is Metody Polucheniya Khimicheskikh Reaktivov i Preparatov (1964), 32-3, database is CAplus.

(PhCH₂)₂– NCN (I) was synthesized from CaNCN and PhCH₂Cl (II). CaNCN (0.1 mole) was added to a mixture of 42 ml. H₂O and 10 g. ice, 0.2 mole 40% NaOH added after 30 min., the solution stirred 1 hr. at >25°, 0.02 mole II in 50 ml. alc. added, the mixture gently refluxed 3 hrs. unreacted II, alc., and oil were steam-distilled, the mixture was cooled to ∼20° and filtered, and the residue extracted with CHCl₃ to give 67.7-73.5% I, m. 47-50°.

Metody Polucheniya Khimicheskikh Reaktivov i Preparatov 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, COA of Formula: C15H14N2.

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

Wu, Shan published the artcileConnexin 32 deficiency protects the liver against ischemia/reperfusion injury, Computed Properties of 380315-80-0, the publication is European Journal of Pharmacology (2020), 173056, database is CAplus and MEDLINE.

Hepatic ischemia/reperfusion (I/R) injury is a common complication in the clin. setting. Our previous study has shown that connexin 32 (Cx32) plays a major role in renal I/R injury; however, the role of Cx32 in hepatic I/R injury remains unknown. Liver tissue and serum samples from patients undergoing orthotopic liver transplantation (OLT) were used to evaluate the function of Cx32 in OLT post-reperfusion injury. Then, partial hepatic ischemia was established in global Cx32 knockout mice and wild-type mice followed by reperfusion. Hepatic injury markers were examined Cx32 small interfering RNA and the p53 inhibitor, pifithrin-α, tenovin-1 were used to examine the relationship between Cx32 and the p53/puma pathways in the BRL-3A and murine primary hepatocytes hypoxia/reoxygenation (H/R) model. Corresponding to liver damage, Cx32 was significantly induced both during OLT in human patients and partial hepatic I/R in mice. Cx32 KO mice exhibited less liver injury than controls. Cx32 deficiency significantly suppressed the p53/puma pathways and hepatocyte apoptosis. Similar results were observed in the BRL-3A and murine primary hepatocytes H/R model. Propofol protected against OLT post-reperfusion injury and hepatocyte apoptosis by inhibiting Cx32. In conclusion Cx32 is a novel regulator of hepatic I/R injury through the modulation of hepatocyte apoptosis and damage, largely via the p53/puma signaling pathway.

European Journal of Pharmacology 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 C24H29N5O3, Computed Properties of 380315-80-0.

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