Month: November 2022

Appukkuttan, Prasad published the artcileMicrowave-assisted transition-metal-catalyzed synthesis of N-shifted and ring-expanded buflavine analogues, Formula: C11H16BNO3, the publication is Chemistry – A European Journal (2007), 13(22), 6452-6460, database is CAplus and MEDLINE.

Buflavine analogs I (R = H, MeO) and II (R = H, MeO) are prepared using microwave-assisted Suzuki-Miyaura coupling reactions and ring-closing metathesis reactions as key steps. Suzuki-Miyaura coupling of the bromostyrenes III (R = H, MeO) with an (allyl)(pivaloyl)aminoboronic acid provides a biaryl which undergoes selective ring-closing metathesis in the presence of either the first or the second-generation Grubbs catalysts followed by olefin hydrogenation to yield I (R = H, MeO); attempted reduction of a related vinylnitrostyrene gives inseparable mixtures of the desired biphenylamines along with phenanthridines generated by reductive cyclization. Suzuki-Miyaura coupling of III (R = H, MeO) with 2-formylbenzeneboronic acid, reductive amination with allylamine followed by reductive methylation of the amines, ring-closing metathesis with the second-generation Grubbs catalyst, and olefin hydrogenation provides II (R = H, MeO).

Chemistry – A European Journal 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, Formula: C11H16BNO3.

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

Chavan, Sunil S. published the artcileIonic liquid-catalyzed 4,6-disubstituted-3-cyano-2-pyridone synthesis under solvent-free conditions, Safety of 2-Cyano-N-ethylacetamide, the publication is Catalysis Letters (2011), 141(11), 1693-1697, database is CAplus.

A green protocol for the synthesis of 4,6-disubstituted-3-cyano-2-pyridones from cyanoacetamides and 1,3-dicarbonyl compounds or chalcones using guanidine-based ionic liquid as catalyst was developed. In solvent-free conditions at 30 °, 1,1,3,3-tetramethylguanidine lactate had the highest catalytic activity among the ionic liquids including 1,1,3,3-tetramethylguanidine acetate, 1,1,3,3-tetramethylguanidine propionate, 1,1,3,3-tetramethylguanidine n-butyrate, and 1,1,3,3-tetramethylguanidine trifluoroacetate. The catalyst was recovered and recycled several times without significant loss of catalytic activity.

Catalysis Letters 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

Kheradmand, Farrah published the artcileLeukotriene A₄ hydrolase: the janus enzyme shows its ugly side in smokers, Synthetic Route of 321673-30-7, the publication is American Journal of Respiratory and Critical Care Medicine (2014), 190(1), 5-7, database is CAplus and MEDLINE.

This paper describes the cigarette smoke chem. acetylates proline-glycine-proline, enhancing its chemotactic activity and protecting it from degradation by LTA4H. And also biochem. and preliminary murine studies suggest that cigarette smoke can selectively abrogate the peptidase activity of LTA4H, with minimal effect on the hydrolase activity.

American Journal of Respiratory and Critical Care Medicine 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 C12H23N3S, Synthetic Route of 321673-30-7.

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

Bastos, Gustavo A. published the artcileA convenient Hofmann reaction of carboxamides and cyclic imides mediated by trihaloisocyanuric acids, SDS of cas: 2447-79-2, the publication is Tetrahedron Letters (2021), 153422, database is CAplus.

A simple, efficient and pot-economic approach in a single vessel has been developed for conversion of aromatic and aliphatic carboxamides into primary amines with one fewer carbom atom (Hofmann reaction) in 38-89% yield by reacting with trichloro- or tribromoisocyanuric acid and sodium hydroxide in aqueous acetonitrile. Under the same reaction conditions, cyclic imides gave amino acids (69-83%). The role of the trihaloisocyanuric acids is the in situ generation of N-haloamides, key-intermediates for the Hofmann reaction. The scalability of the methodol. was demonstrated by a multigram-scale transformation of phthalimide into anthranilic acid in 77% yield.

Tetrahedron 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, SDS of cas: 2447-79-2.

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

Mehuys, Els published the artcilePrevalence and management of drug interactions between nonsteroidal anti-inflammatory drugs and antithrombotics in ambulatory care, Application In Synthesis of 169590-42-5, the publication is British Journal of Clinical Pharmacology (2022), 88(8), 3896-3902, database is CAplus and MEDLINE.

Concomitant use of nonsteroidal anti-inflammatory drugs (NSAIDs) and antithrombotic agents is associated with increased risks of both bleeding and thromboembolism. In this prospective intervention study, community pharmacists screened for NSAID-antithrombotic interactions and contacted the prescribing physician to discuss interaction management. We included 782 interactions; these were found in an older, polymedicated patient population (mean age: 68 y, median of 5 other drugs). Ibuprofen (in 43.0% of cases) and low-dose aspirin (78.8%) were the most frequently involved NSAID and antithrombotic, resp. Anticoagulants were involved in 16.1% of interaction cases. For 61% of cases, the interacting drugs were prescribed by the same physician. The pharmacist-physician discussion about how to manage the interaction mostly resulted in no change of pharmacotherapy (60.7%); the most frequent reason given by physicians was that the NSAID was for short-term use only. In 39.3% of cases the discussion resulted in a pharmacotherapy change; replacing the NSAID by paracetamol was the most common change.

British Journal of Clinical Pharmacology 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, Application In Synthesis of 169590-42-5.

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

Arya, V. P. published the artcilePsychoactive agents: part VIII. Isothiazoles: part VIII. Synthesis and biological activity of 4-(2-amino-4-thiazolyl)isothiazoles, Product Details of C5H10N2OS, the publication is Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (1978), 16B(5), 402-4, database is CAplus.

RR¹NH (NRR¹ = morpholino, hexahydro-1-azepinyl, octahydro-1-azocinyl, 3-azabicyclo[3.2.2]nonan-3-yl, 4-(4-fluorophenyl)piperazin-1-yl) were treated with tert-BuNCS to give RR¹NCSNHCMe₃, which ws debutylated to give RR¹NCSNH₂. This and R²CSNH² (R² = NH₂, NHMe, NHBu, NHCH₂CH:CH₂, NHCH₂Ph, etc.) were cyclized with I (R³ = H, Me, Et) to give the corresponding II. Among II, 4-(2-amino-4-thiazolyl)-3,5-dimethylisothiazole showed the highest analgesic activity and 4-(2-amino-4-thiazolyl)-3-methylisothiazole had the highest antiinflammatory activity.

Indian Journal of Chemistry, Section B: Organic Chemistry Including 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 C5H10N2OS, Product Details of C5H10N2OS.

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

Ough, Cornelius S. published the artcileIdentification of new volatile amines in grapes and wines, Quality Control of 360-92-9, the publication is Journal of Agricultural and Food Chemistry (1981), 29(5), 938-41, database is CAplus and MEDLINE.

A number of amines were identified for the 1st time in grapes. These include MeNH₂ [74-89-5], EtNH₂ [75-04-7], Et₂NH [109-89-7], PrNH₂ [107-10-8], isobutylamine [78-81-9], α-amylamine [96-15-1], isoamylamine [107-85-7], pyrrolidine [123-75-1], and 2-phenethylamine [64-04-0]. The trifluoroacetamides of the isolated amines were separated on Carbowax 20M or SE54 fused silica capillary columns and identified by retention times and mass spectra. Two amines, di-Et and α-amyl, were identified in wine for the 1st time. Mass spectra of the pure trifluoroacetyl derivatives of these amines are given. In a recent review, P. Schreier (1979) compiled a list of the volatile amines found in wines. The volatile amines he summarized plus others detected in wines are given.

Journal of Agricultural and Food Chemistry published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Quality Control of 360-92-9.

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

Wu, Danchen published the artcileIdentification of novel dynamin-related protein 1 (Drp1) GTPase inhibitors: Therapeutic potential of Drpitor1 and Drpitor1a in cancer and cardiac ischemia-reperfusion injury, Computed Properties of 530-40-5, the publication is FASEB Journal (2020), 34(1), 1447-1464, database is CAplus and MEDLINE.

Mitochondrial fission is important in physiol. processes, including coordination of mitochondrial and nuclear division during mitosis, and pathol. processes, such as the production of reactive oxygen species (ROS) during cardiac ischemia-reperfusion injury (IR). Mitochondrial fission is mainly mediated by dynamin-related protein 1 (Drp1), a large GTPase. The GTPase activity of Drp1 is essential for its fissogenic activity. Therefore, we aimed to identify Drp1 inhibitors and evaluate their anti-neoplastic and cardioprotective properties in five cancer cell lines (A549, SK-MES-1, SK-LU-1, SW 900, and MCF7) and an exptl. cardiac IR injury model. Virtual screening of a chem. library revealed 17 compounds with high predicted affinity to the GTPase domain of Drp1. In silico screening identified an ellipticine compound, Drpitor1, as a putative, potent Drp1 inhibitor. We also synthesized a congener of Drpitor1 to remove the methoxymethyl group and reduce hydrolytic lability (Drpitor1a). Drpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Drpitor1 and Drpitor1a have greater potency than the current standard Drp1 GTPase inhibitor, mdivi-1, (IC50 for mitochondrial fragmentation are 0.09, 0.06, and 10μM, resp.). Both Drpitors reduced proliferation and induced apoptosis in cancer cells. Drpitor1a suppressed lung cancer tumor growth in a mouse xenograft model. Drpitor1a also inhibited mitochondrial ROS production, prevented mitochondrial fission, and improved right ventricular diastolic dysfunction during IR injury. In conclusion, Drpitors are useful tools for understanding mitochondrial dynamics and have therapeutic potential in treating cancer and cardiac IR injury.

FASEB Journal 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 C10H15ClO3S, Computed Properties of 530-40-5.

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

Aitipamula, Srinivasulu published the artcileCocrystal formulations: A case study of topical formulations consisting of ferulic acid cocrystals, Application In Synthesis of 1453-82-3, the publication is European Journal of Pharmaceutics and Biopharmaceutics (2020), 95-104, database is CAplus and MEDLINE.

Renaissance of cocrystals as alternative solid forms for fine-tuning physicochem. properties of active pharmaceutical ingredients (APIs) has paved way for development of marketable cocrystals. The current literature reveals established strategies for the design, synthesis and characterization of cocrystals. However, barring a few isolated case studies, strategies for development of cocrystal formulations have been underdeveloped. Herein we report topical formulations of an antioxidant, ferulic acid (FA), which contain the active in its cocrystal form. Cocrystals of FA with the coformers relevant to skin care such as urea, nicotinamide (NA) and isonicotinamide (INA) have been prepared and oleogel formulations of these have been developed. The cocrystal with urea and an anhydrous cocrystal with INA have been identified for the first time in this study. The novel cocrystals were structurally characterized by single crystal X-ray diffraction. Solubility and stability studies have revealed higher solubility of the cocrystals with NA and INA than the parent active and greater stability of FA in formulations that contained the cocrystals with INA and urea than the corresponding formulations containing phys. mixtures or parent active. In vitro membrane permeation tests have ascertained sustained release profile of active from the formulation that contained the FA·INA cocrystal. The higher solubility, greater stability and sustained active release profile of the FA·INA cocrystal formulation make it a promising topical formulation of FA.

European Journal of Pharmaceutics and Biopharmaceutics 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, Application In Synthesis of 1453-82-3.

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

Sengupta, Manideepa published the artcileSustainable synthesis of drug intermediates via simultaneous utilization of carbon monoxide and ammonia over Pd@La-MOF, Application of Isonicotinamide, the publication is Molecular Catalysis (2022), 112212, database is CAplus.

Mitigation of carbon monoxide and ammonia to valuable primary aromatic amides is an imperative approach to control the environmentally harmful emissions thereby infusing towards sustainability. Designing of nanostructured catalyst for direct access to the synthetically valuable primary aromatic and heteroaromatic amides via carbonylative amination of aryl halides is always demanding since nano materials can bridge the gap between homogeneous and heterogeneous catalysis thus preserving the desirable attributes of both the systems towards sustainable catalysis. Herein, microwave assisted fabrication of highly uniform Pd NPs (3,4 nm) over La-MOFs has been performed and utilized efficiently for ligand free carbonylative amination of aryl iodides with carbon monoxide and ammonia. Moderate to high yields of benzamide derivatives, salicylamide, a drug having analgesic and antipyretic properties were achieved. The unsaturated metal sites in the MOF via synergistic mode of σ and π bonding binds with CO, which significantly enhances the catalytic activity of MOF-composite unlike other supported Pd NPs. DFT confirms the growth of pristine Pd₁₃ cluster within the framework, as active metal center for the carbonylative amination.

Molecular Catalysis 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 C10H15NO, Application of Isonicotinamide.

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