Author: Jessica.F

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

Delehanty, James B. published the artcileSynthesis of a reactive oxygen species-responsive doxorubicin derivative, COA of Formula: C4H6F3NOS, the publication is Molecules (2018), 23(7), 1809/1-1809/5, database is CAplus and MEDLINE.

A heterobifunctional reactive oxygen species (ROS)-responsive linker for directed drug assembly onto and delivery from a quantum dot (QD) nanoparticle carrier was synthesized and coupled to doxorubicin using N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (EDC)/sulfo-NHS coupling. The doxorubicin conjugate was characterized using 1H NMR and LC-MS and subsequently reacted under conditions of ROS formation (Cu2+/H2O2) resulting in successful and rapid thioacetal oxidative cleavage, which was monitored using 1H NMR.

Molecules published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, COA of Formula: C4H6F3NOS.

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

Alexeev, Vladimir L. published the artcilePhotonic crystal glucose-sensing material for noninvasive monitoring of glucose in tear fluid, Name: (3-Fluoro-4-(methylcarbamoyl)phenyl)boronic acid, the publication is Clinical Chemistry (Washington, DC, United States) (2004), 50(12), 2353-2360, database is CAplus and MEDLINE.

Background: We recently developed a photonic crystal glucose-sensing material, which consists of a crystalline colloidal array embedded within a polymer network of a polyacrylamide-poly(ethylene glycol) hydrogel with pendent phenylboronic acid groups. The aim of the present work was to improve this approach for application to noninvasive or minimally invasive monitoring of glucose. Methods: We used new boronic acid derivatives such as 4-amino-3-fluorophenylboronic acid and 4-carboxy-3-fluorophenylboronic acid as the mol. recognition elements to achieve sensing at physiol. pH values. Results: The improved photonic glucose-sensing material sensed glucose in the range of the 100 μmol/L concentrations found in tear fluid. The detection limits were ∼1 μmol/L in synthetic tear fluid. The visually evident diffraction color shifted across the entire visible spectral region from red to blue over the physiol. relevant tear-fluid glucose concentrations This sensing material is selective for glucose over galactose, mannose, and fructose. Conclusions: These new glucose sensors have properties appropriate for use in such glucose-sensing applications as ocular inserts or diagnostic contact lenses for patients with diabetes mellitus.

Clinical Chemistry (Washington, DC, United States) published new progress about 849833-86-9. 849833-86-9 belongs to amides-buliding-blocks, auxiliary class Fluoride,Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester, name is (3-Fluoro-4-(methylcarbamoyl)phenyl)boronic acid, and the molecular formula is C8H9BFNO3, Name: (3-Fluoro-4-(methylcarbamoyl)phenyl)boronic acid.

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

Sahoo, Daisy published the artcileScavenger receptor class B Type I (SR-BI) assembles into detergent-sensitive dimers and tetramers, Name: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids (2007), 1771(7), 807-817, database is CAplus and MEDLINE.

High d. lipoproteins (HDL) are protective against cardiovascular disease due to their important role in the reverse cholesterol transport (RCT) pathway. The selective transfer of cholesteryl ester (CE) from the HDL core to cells, the last step in RCT, is mediated by scavenger receptor class B type I (SR-BI). SR-BI is a heavily glycosylated cell surface receptor that is highly expressed in the liver, ovaries, testes and adrenal glands, where selective uptake of HDL-CE is most prevalent. Previous studies have shown that SR-BI oligomerizes with itself in steroidogenic tissues as well as in diverse cell lines. In the present study, we provide further evidence for the homo-oligomerization of SR-BI. We show by FPLC and blue native PAGE that SR-BI forms complexes whose sizes suggest the formation of monomers, dimers, and tetramers. Interestingly, homo-oligomerization occurs even with the absence of SR-BI’s C-terminal cytoplasmic domain. Finally, we report that an inhibitor of SR-BI-mediated cholesterol transport, BLT-1, and mutations in the putative leucine zipper region of SR-BI have profound effects on SR-BI function, however, they do not affect receptor self-association These observations indicate that SR-BI homo-oligomerization occurs even when the receptor is non-functional.

Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids 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, Name: [(2-Hexylcyclopentylidene)amino]thiourea.

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

Shcherbakov, Nikolay V. published the artcileHetero-Tetradehydro-Diels-Alder Cycloaddition of Enynamides and Cyanamides: Gold-Catalyzed Generation of Diversely Substituted 2,6-Diaminopyridines, Synthetic Route of 2451-91-4, the publication is Journal of Organic Chemistry (2021), 86(10), 7218-7228, database is CAplus and MEDLINE.

The reaction proceeds under very mild conditions (DCM, rt) with high functional group tolerance. The obtained 2,6-diaminopyridines I and II represent a useful synthetic platform with an easily modulated substitution pattern for subsequent functionalizations of both the pyridine core and the N-substituents. Gold(I)-catalyzed hetero-tetradehydro-Diels-Alder cycloaddition of enynamides R¹CH=C(R²)CCN(R³)R⁴ [R¹ = C₆H₅, 2-thienyl, 1-naphthyl, etc.; R² = H, Me; R³ = Me, Ph, Bn, Ts; R⁴ = 4-MeC₆H₄S(O)₂, MeS(O)₂, 4-FC₆H₄S(O)₂, CH₂CH=CH₂, 2-(2H-1,3-benzodioxol-5-yl)ethyl; R³R⁴ = -C(O)O(CH₂)₂-] and cyanamides R⁵R⁶NCN (R⁵ = Me, Et, Bn, Ph; R⁶ = Me, Et, Bn, Ph; R⁵R⁶ = -(CH₂)₄-, -(CH₂)₅-, -(CH₂)₂O(CH₂)₂-) and 3,4-dihydro-2(1H)-Isoquinolinecarbonitrile comprises an efficient route to diversely substituted 2,6-diaminopyridines I and II (yields up to 99%).

Journal of Organic Chemistry 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 C18H24N6O6S4, Synthetic Route of 2451-91-4.

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

Raffa, Demetrio published the artcileNovel 4-(3-phenylpropionamido), 4-(2-phenoxyacetamido) and 4-(cinnamamido) substituted benzamides bearing the pyrazole or indazole nucleus: synthesis, biological evaluation and mechanism of action, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, the publication is Bioorganic Chemistry (2019), 367-379, database is CAplus and MEDLINE.

Based on some common structural features of known compounds interfering with p53 pathways and our previously synthesized benzamides, we synthesized new Et 5-(4-substituted benzamido)-1-phenyl-1H-pyrazole-4-carboxylates 26a-c, Et 5-(4-substituted benzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxylates 27a-c and N-(1H-indazol-6-yl)-4-substituted benzamides 31a,b bearing in the 4 position of the benzamido moiety the 2-phenylpropanamido or 2-phenoxyacetamido or cinnamamido groups. A preliminary test to evaluate the antiproliferative activity against human lung carcinoma H292 cells highlighted how compound 26c showed the best activity. This last was therefore selected for further studies with the aim to find the mechanism of action. Compound 26c induces intrinsic apoptotic pathway by activating p53 and is also able to activate TRAIL-inducing death pathway by promoting increase of DR4 and DR5 death receptors, downregulation of c-FLIP_L and caspase-8 activation.

Bioorganic Chemistry 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 C20H23N3O2S, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide.

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

Raffa, Demetrio published the artcileNovel 4-(3-phenylpropionamido), 4-(2-phenoxyacetamido) and 4-(cinnamamido) substituted benzamides bearing the pyrazole or indazole nucleus: synthesis, biological evaluation and mechanism of action, Related Products of amides-buliding-blocks, the publication is Bioorganic Chemistry (2019), 367-379, database is CAplus and MEDLINE.

Based on some common structural features of known compounds interfering with p53 pathways and our previously synthesized benzamides, we synthesized new Et 5-(4-substituted benzamido)-1-phenyl-1H-pyrazole-4-carboxylates 26a-c, Et 5-(4-substituted benzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxylates 27a-c and N-(1H-indazol-6-yl)-4-substituted benzamides 31a,b bearing in the 4 position of the benzamido moiety the 2-phenylpropanamido or 2-phenoxyacetamido or cinnamamido groups. A preliminary test to evaluate the antiproliferative activity against human lung carcinoma H292 cells highlighted how compound 26c showed the best activity. This last was therefore selected for further studies with the aim to find the mechanism of action. Compound 26c induces intrinsic apoptotic pathway by activating p53 and is also able to activate TRAIL-inducing death pathway by promoting increase of DR4 and DR5 death receptors, downregulation of c-FLIP_L and caspase-8 activation.

Bioorganic Chemistry published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Related Products of amides-buliding-blocks.

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

Palmisano, Giovanni published the artcileElectrochemical heterocyclization of o-toluenesulfonamides to 3-alkyl-4,5-dihydro-1,2,4-benzothiadiazepine 1,1-dioxides, Application In Synthesis of 489-17-8, the publication is Tetrahedron (1988), 44(5), 1545-52, database is CAplus.

Controlled potential oxidation of a variety of substituted o-toluenesulfonamides at a Pt anode in MeCN using a divided cell forms 3-methyl-4,5-dihydro-1,2,4-benzothiadiazepine-1,1-dioxides selectively and in generally good yields. The scope and limitations of this 1-step heterocyclization sequence are also discussed.

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 C7H8FNO2S, Application In Synthesis of 489-17-8.

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

Mameli, Efisio published the artcileAminolysis of ethylxanthogenamide. III, Quality Control of 14294-10-1, the publication is Annali di Chimica (Rome, Italy) (1956), 545-62, database is CAplus.

cf. C.A. 51, 3458d. EtOCSNH₂ (I) reacts with 2 moles RNH₂ at room temperature to give RNHCSNH₂ (II); the rate of reaction and yield are greatly increased by addition of 0.3 mole KOH. Yields of II obtained without and with KOH, resp., are: from MeNH₂, 61, 79; EtNH₂, 57, 61; PrNH₂, 39, 79; iso-PrNH₂, 42, 45; BuNH₂, 22, 71; PhCH₂NH₂, about 16, 61; cyclohexylamine, 12, 36. Reaction times are up to 50 days. No byproducts (except SCN^–) are found when KOH is used; the following are detected in experiments without KOH: (MeNH)₂C:NH, (EtNH)₂C:NH, BuNHCSOEt, [(PhCH₂NH)₂C:NH]₂.H₂S₂O₃ (III), C₆H₁₁NHCSOEt. Reaction between 2.1 g. I and 2 moles 33% aqueous PhCH₂NH₂ in 6 cc. EtOH gives first a precipitate of II, then (after exposure of the filtrate to air) an oil, from which III is obtained by crystallization from Me₂CO. III, m. 168-9°, is identified by conversion to (PhCH₂NH)₂C:NH and its hydrochloride; its infrared spectrum is given. Me₂NH reacts with I in aqueous EtOH to give 7% Me₂NCSOEt and 10% [Me₂NC(:NH)NH₂]₂.H₂S₂O₃, but in the presence of KOH gives 67% Me₂NCSNH₂. Et₂NH and iso-Bu₂NH fail to react. Pyrrolidine after 4 days with I in aqueous EtOH gives 30% 1-(thiocarbamyl)pyrrolidine, m. 193-7° (dependent on the rate of heating), which isomerizes to the corresponding thiocyanate above the m.p.; the same product (84%) is obtained in 1 day when KOH is added. Piperidine and I without KOH give only traces of 1-(thiocarbethoxy)piperidine and 1-(thiocarbamyl)piperidine; with KOH 27% of the latter is formed. Piperidine, I, and 1 mole 30% NH₃ in aqueous solution evaporated after 30 days give 7% 1-guanylpiperidine hyposulfite, m. 246-7° (variable). Morpholine gives approx. 20% N-(ethoxythiocarbonyl)morpholine and 15% N-guanylmorpholine hyposulfite, m. 263-5° (variable); addition of 1 mole NH₃ increases these yields to about 30% each, but addition of 0.3 mole KOH changes the reaction completely, the only product being N-(thiocarbamyl)morpholine (50%). In general, increase in KOH concentration or temperature only leads to increased decomposition of I. Attempts to make I react with (HOCH₂CH₂)₂NH or with aromatic amines at room temperature or above were unsuccessful. Formation of hyposulfites is ascribed to spontaneous oxidation of S^—, but yields are not improved by aeration or addition of H₂O₂. The variety of products obtained from I is ascribed to the possibility of tautomerism.

Annali di Chimica (Rome, Italy) 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, Quality Control of 14294-10-1.

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