Category: amides-buliding-blocks

Zeng, Hongyun published the artcileMethod for synthesis of 2,5-diaryl substituted thiazoles, Recommanded Product: 3-Methoxybenzothioamide, the publication is Youji Huaxue (2020), 40(8), 2535-2542, database is CAplus.

Thiazole ring is an important five-membered aromatic heterocyclic ring, and its derivatives have various biol. activities and are widely used in medicine. The synthesis of 2,5-diarylthiazole derivatives by acylation, thiolation, cyclization and Heck reaction using inexpensive and readily available substituted benzoic acid as raw materials was developed. The key point was to optimize the Heck reaction conditions and explore the possible reaction mechanism. The method has mild reaction conditions, simple operation, and good substrate universality, which provides a new direction for the synthesis of 2,5-diaryl substituted thiazoles.

Youji Huaxue 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 C6H12N2O, Recommanded Product: 3-Methoxybenzothioamide.

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

Wang, Lei published the artcileStructures of the Human PGD₂ Receptor CRTH2 Reveal Novel Mechanisms for Ligand Recognition, Safety of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Molecular Cell (2018), 72(1), 48-59.e4, database is CAplus and MEDLINE.

The signaling of prostaglandin D₂ (PGD₂) through G-protein-coupled receptor (GPCR) CRTH2 is a major pathway in type 2 inflammation. Compelling evidence suggests the therapeutic benefits of blocking CRTH2 signaling in many inflammatory disorders. Currently, a number of CRTH2 antagonists are under clin. investigation, and one compound, fevipiprant, has advanced to phase 3 clin. trials for asthma. Here, we present the crystal structures of human CRTH2 with two antagonists, fevipiprant and CAY10471. The structures, together with docking and ligand-binding data, reveal a semi-occluded pocket covered by a well-structured amino terminus and different binding modes of chem. diverse CRTH2 antagonists. Structural anal. suggests a ligand entry port and a binding process that is facilitated by opposite charge attraction for PGD₂, which differs significantly from the binding pose and binding environment of lysophospholipids and endocannabinoids, revealing a new mechanism for lipid recognition by GPCRs.

Molecular Cell 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 C25H47NO8, Safety of [(2-Hexylcyclopentylidene)amino]thiourea.

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

Dai, Xia-Lin published the artcileSolubility and Permeability Improvement of Allopurinol by Cocrystallization, Category: amides-buliding-blocks, the publication is Crystal Growth & Design (2020), 20(8), 5160-5168, database is CAplus.

Allopurinol is a xanthine oxidase inhibitor with poor solubility and permeability, which severely limit its drug absorption following the administration of some dosage forms, such as tablets and rectal suppositories. To improve the physicochem. properties, three cocrystals of allopurinol with isonicotinamide (ALP-INA), piperazine (ALP-PIP), and 2,4-dihydroxybenzoic acid (ALP-24DHBZA) were successfully prepared by a slurry or liquid-assisted grinding method. The obtained cocrystal materials were characterized by single-crystal X-ray diffraction, powder X-ray diffraction, IR spectroscopy, differential scanning calorimetry, and thermogravimetric analyses and were subjected to dynamic vapor sorption, dissolution, and membrane permeability studies. ALP-INA showed solubility and diffusion/membrane permeability similar to those of the parent drug. In contrast, ALP-PIP exhibited improved diffusion/membrane permeability, and ALP-24DHBZA exhibited improved dissolution behavior, resp. These results suggest that ALP-PIP and ALP-24DHBZA have the potential to be developed as new, more efficient formulations of allopurinol. Three cocrystals of allopurinol (ALP) with isonicotinamide (ALP-INA), piperazine (ALP-PIP), and 2,4-dihydroxybenzoic acid (ALP-24DHBZA) were synthesized, and ALP-PIP and ALP-24DHBZA resp. showed significant improvement in membrane permeability and dissolution behaviors in comparison to the original ALP.

Crystal Growth & Design published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Category: amides-buliding-blocks.

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

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

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

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

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

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

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