Tag: M.W=100-150

El Hefny, Eman A. published the artcileSynthesis, characterization, antitumor evaluation and molecular docking of some triazolotriazine derivatives, Name: 2-Cyano-N-ethylacetamide, the publication is Journal of Pharma Research (2014), 3(5), 79-87, database is CAplus.

The synthesis of 4-amino-[1,2,4]triazolo[5,1-c][1,2,4]triazine derivatives I (R = CN, COOC₂H₅, CONH₂) using readily available starting materials is described. In this study, six selected derivatives, compounds I (R = CN), II, III, IV (Ar = 4-ClC₆H₄, 2-ClC₆H₄) and V were subjected to a screening system for investigation of their antitumor potency against liver (HEPG2) cell line in comparison to known anticancer drugs, 5-fluorouracil and Doxorubicin. The antitumor activity results indicated that the selected compounds I (R = CN), II, III, IV (Ar = 4-ClC₆H₄, 2-ClC₆H₄) and V derivatives showed growth inhibition activity against the tested cell line but with varying intensities in comparison to 5-fluorouracil and Doxorubicin. Compounds II and III were investigated for the binding affinity of c-Kit tyrosine kinases receptor.

Journal of Pharma Research 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, Name: 2-Cyano-N-ethylacetamide.

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

El-Faham, Ayman published the artcileSynthesis, characterization and anti-proliferation activity of novel cyano oximino sulfonate esters, Name: 2-Cyano-N-ethylacetamide, the publication is Chemical & Pharmaceutical Bulletin (2014), 62(4), 373-378, database is CAplus and MEDLINE.

A series of cyano oximino sulfonate derivatives RS(O)2ON:C(CN)X (R = 4-CH₃C₆H₅, naphthalen-2-yl; X = C₆H₅, C₂H₅NH₂, NH₂, etc). were prepared from the reaction of arylsulfonyl chloride with different cyanoacetamide-based oximes ranging from the simplest unsubstituted amide to analogs containing N-Et (mimicking the Oxyma template), N-piperidinyl and N-morpholinyl chains. In addition, the cyano oximes, N-hydroxybenzimidoyl cyanide and N-hydroxy picolinimidoyl cyanide were also used in the synthesis of cyano oximino sulfonate derivatives The preliminary bioassays showed that some of the title compounds, such as (TsPipOx), (TsPhOX), (NpsPipOx) etc, showed anti-proliferation effect on the mouse fibroblast L929. The calculated IC₅₀-values were ranging between 36.5 μg/mL and 0.235 mg/mL. However the anti-proliferation effects seem to be cytostatic rather than cytotoxic. The compounds only minimize the growth activity without completely killing the cells.

Chemical & Pharmaceutical Bulletin 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, Name: 2-Cyano-N-ethylacetamide.

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

Liu, Shiyuan published the artcileChitosan hydrogel for controlled crystallization of loaded drug: Role of interplay of assembly processes, Recommanded Product: Isonicotinamide, the publication is Colloids and Surfaces, A: Physicochemical and Engineering Aspects (2022), 128824, database is CAplus.

The utilization of natural polymer gel to achieve drug polymorph control is usually a challenging issue, and the interplay of gelation and crystallization has been neglected in many studies. In this work, a modified chitosan (Cs) hydrogel was used to encapsulate drug Isonicotinamide (IN), where competitive crystallization and gelation was constructed for a better control of different assembly processes. It was found that the crystalline outcome of drug (cocrystals or IN Form I) depends on different crosslinking agents used. Spectral anal. and MD simulation reveal that the interplay of crosslinking effect of Cs, dimerization of crosslinking agents and aggregation of IN determines the crystalline outcome, among which the affinity to crosslinking agents of Cs chain plays the significant role. To our knowledge, it is the first time that Cs hydrogel acts as a template to regulate polymorphism of drug. This work offers a promising way for drug delivery system design.

Colloids and Surfaces, A: Physicochemical and Engineering Aspects 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, Recommanded Product: Isonicotinamide.

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

Jackson, Grayson L. published the artcileDesigning Stress-Adaptive Dense Suspensions Using Dynamic Covalent Chemistry, Synthetic Route of 15029-36-4, the publication is Macromolecules (Washington, DC, United States) (2022), 55(15), 6453-6461, database is CAplus and MEDLINE.

The non-Newtonian behaviors of dense suspensions are central to their use in technol. and industrial applications and arise from a network of particle-particle contacts that dynamically adapt to imposed shear. Reported herein are studies aimed at exploring how dynamic covalent chem. between particles and the polymeric solvent can be used to tailor such stress-adaptive contact networks, leading to their unusual rheol. behaviors. Specifically, a room temperature dynamic thia-Michael bond is employed to rationally tune the equilibrium constant (K_eq) of the polymeric solvent to the particle interface. It is demonstrated that low K_eq leads to shear thinning, while high K_eq produces antithixotropy, a rare phenomenon where the viscosity increases with shearing time. It is proposed that an increase in K_eq increases the polymer graft d. at the particle surface and that antithixotropy primarily arises from partial debonding of the polymeric graft/solvent from the particle surface and the formation of polymer bridges between particles. Thus, the implementation of dynamic covalent chem. provides a new mol. handle with which to tailor the macroscopic rheol. of suspensions by introducing programmable time dependence. These studies open the door to energy-absorbing materials that not only sense mech. inputs and adjust their dissipation as a function of time or shear rate but also can switch between these two modalities on demand.

Macromolecules (Washington, DC, United States) 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, Synthetic Route of 15029-36-4.

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

Culbertson, Townley P. published the artcileNew 7-substituted quinolone antibacterial agents. The synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(2-thiazolyl and 4-thiazolyl)-3-quinolinecarboxylic acids, Related Products of amides-buliding-blocks, the publication is Journal of Heterocyclic Chemistry (1987), 24(6), 1509-20, database is CAplus.

A series of 1-ethyl-1,4-dihydro-4-oxo-7-(4-thiazolyl)-3-quinolinecarboxylic acids e.g. I (R = NH₂, MeNH, AcNCH₂, Me₂N, 3-pyridyl, morpholino, etc.; R¹,R² = H, F), and 1-ethyl-1,4-dihydro-4-oxo-7-(2-thiazolyl)-3-quinolinecarboxylic acids were prepared Also prepared was 10-[2-(aminomethyl)-4-thiazolyl]-9-fluoro-2,3-dihydro-3-methyl-7–oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid (II). Analogs with basic amine substituents on the thiazole moiety were found to have antibacterial activity.

Journal of Heterocyclic 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, Related Products of amides-buliding-blocks.

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

Dreyer, R. published the artcileSynthesis and characterization of cationic astatine compounds with sulfur-containing ligands stable in aqueous solutions, COA of Formula: C5H10N2OS, the publication is Journal of Radioanalytical and Nuclear Chemistry (1985), 96(3), 333-41, database is CAplus.

The formation of cationic At compounds with thiourea, thiourea derivatives and some N-acylthioureas was studied in aqueous solutions The ion mobilities in free electrolytes were determined for the detection of carrier-free At compounds and their characterization. Information about the stability of this group of compounds could be given after studies in the presence of halide and pseudohalide ions (Cl^–, Br^–, I^–, SCN^–).

Journal of Radioanalytical and Nuclear 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, COA of Formula: C5H10N2OS.

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

Kalluraya, Balakrishna published the artcileSynthesis and antibacterial activity of some 2-substituted-4-(5-nitro-2-thienyl)thiazoles, SDS of cas: 14294-10-1, the publication is Revue Roumaine de Chimie (1995), 40(11-12), 1183-1188, database is CAplus.

The preparation of 2-substituted 4-(5-nitro-2-thienyl)thiazoles I (R = Ph, chlorophenyl, phenylamino, etc.) was described. These compounds were tested for their antibacterial activity against both Gram-pos. and Gram-neg. bacteria. The results of the screening indicate that the title compounds carrying chloro substituents in the aryl moiety possess better activity against all the organisms testes.

Revue Roumaine de Chimie 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, SDS of cas: 14294-10-1.

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

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

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