Tag: M.W=100-150

Salome, Christophe published the artcileBenzofuran derivatives as a novel class of inhibitors of mTOR signaling, Recommanded Product: Piperidine-4-carboxamide, the publication is European Journal of Medicinal Chemistry (2014), 41-49, database is CAplus and MEDLINE.

High-throughput screening (HTS) hit (I) was previously identified as an inhibitor of the Akt/mTOR (Akt/mammalian target of rapamycin) signaling, which is a major target in oncol. The cytotoxicity of I was determined on a panel of human cancer cells lines with an IC₅₀ comprised between 30 and 140 μM. Subsequent structure-activity relation (SAR) studies led us to the identification of compounds that displayed an enhanced cytotoxicity. We demonstrated also that these mols. directly bind to mTOR complex 1 (mTORC1) and inhibit its kinase activity.

European Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Recommanded Product: Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wu, Qiong published the artcileCo-culture of Bacillus amyloliquefaciens ACCC11060 and Trichoderma asperellum GDFS1009 enhanced pathogen-inhibition and amino acid yield, Application In Synthesis of 39546-32-2, the publication is Microbial Cell Factories (2018), 155, database is CAplus and MEDLINE.

Bacillus spp. are a genus of biocontrol bacteria widely used for antibiosis, while Trichoderma spp. are biocontrol fungi that are abundantly explored. In this study, a liquid co-cultivation of these two organisms was tried firstly. Through liquid chromatog.-mass spectrometry/mass spectrometry (LC-MS/MS), it was discovered that with an inoculation in the ratio of 1.9:1, the antimicrobial effect of the co-cultured fermentation liquor of Bacillus amyloliquefaciens ACCC11060 and Trichoderma asperellum GDFS1009 was found to be significantly higher than that of pure-cultivation. A raise in the synthesis of antimicrobial substances contributed to this significant increase. Addnl., a co-culture with the inoculation of the two organisms in the ratio of 1:1 was found to enhance the production of specific amino acids. This technique could be further explored for either a large scale production of amino acids or could serve as a theor. base for the generation of certain rare amino acids. This work clearly demonstrated that co-cultivation of B. amyloliquefaciens ACCC11060 and T. asperellum GDFS1009 could produce more specific biocontrol substances and amino acids.

Microbial Cell Factories published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C17H18N2O6, Application In Synthesis of 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Asif, Kanwal published the artcileSolid phase syntheses of peptoid like arylureido compounds and sequencing of isobars without molecular encoding, Computed Properties of 39546-32-2, the publication is Organic & Biomolecular Chemistry (2019), 17(17), 4204-4207, database is CAplus and MEDLINE.

Arylureido-backbone containing peptoid-like trimers were prepared using the one-bead-one-compound approach. Isobaric mols. were synthesized from isocyanate precursors that contain alkyl halide handles at the ortho and para-positions in the Ph ring. After chain extension with a primary amine, the piperazine-capped mols. were sequenced using tandem mass spectrometry and successfully identified based on their fragmentation pattern without a need for internal mol. encoding.

Organic & Biomolecular Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Computed Properties of 39546-32-2.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Blazenovic, Ivana published the artcileEffects of Gut Bacteria Depletion and High-Na⁺ and Low-K⁺ Intake on Circulating Levels of Biogenic Amines, Name: Piperidine-4-carboxamide, the publication is Molecular Nutrition & Food Research (2019), 63(4), n/a, database is CAplus and MEDLINE.

Scope : High-sodium and low-potassium (HNaLK) content in Western diets increases the risk of hypertension and cardiovascular disease (CVD). It is investigated if the dietary minerals interact with gut bacteria to modulate circulating levels of biogenic amines, which are implicated in various pathologies, including hypertension and CVD. Methods and results : Using a metabolomic approach to target biogenic amines, the effects of gut bacteria depletion and HNaLK intake on circulating levels of biogenic amines in rats are examined Forty-five metabolites whose plasma levels are significantly altered by gut bacteria depletion (p < 0.05) are found, indicating their regulation by gut bacteria. Many of them are not previously linked to gut bacteria; therefore, these data provide novel insights into physiol. or pathol. roles of gut bacteria. A number of plasma metabolites that are altered both by gut bacteria and HNaLK intake are also found, suggesting possible interactions of the diet and gut bacteria in the modulation of these metabolites. The diet effects are observed with significant changes in the gut bacterial taxa Porphyromonadaceae and Prevotellaceae (p < 0.05). Conclusion : The dietary minerals may regulate abundances of certain gut bacteria to alter circulating levels of biogenic amines, which may be linked to host physiol. or pathol.

Molecular Nutrition & Food Research published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Name: Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Abood, L. G. published the artcileStructure-activity relationships of 3-piperidyl benzilates with psychotogenic properties, Related Products of piperidines, the publication is Archives Internationales de Pharmacodynamie et de Therapie (1959), 186-200, database is CAplus.

Correlation of pharmacol. and psychotogenic properties of compounds of structure CH₂.CH₂.CH₂NA.CH₂.CHOCOC(Ph)(B)(R) was attempted. In addition to auditory and visual hallucinations, mood changes, disorientation, hypochondriacal and paranoid delusions, and partial loss of contact were observed on administration of such compounds The most effective compound was N-methyl-3-piperidyl phenylcyclohexyl glycolate (I). Other materials studied included (given in order are A, B, and R): Me, OH, cyclohexyl (II); Et, OH, II; Et, OH, cyclopentyl; Me, OH, Ph; Me, OH, 2-thienyl; Et, OH, Ph; CH₂CH₂NMe₂, OH, Ph; 1,2,2,6,6-pentamethyl (3-piperidyl isomer), OH, Ph; Me, OH, Ph; Et, OH, Pr; H, OH, Ph; Et, H, Ph; (CH₃)₂, OH, Ph; and (C₂H₅)CH₃, OH, Ph. These compounds were potent anticholinergic agents, the best being the 2-thienyl compound Most compounds were antihistamines. Physostigmine counteracted anticholinergic effects but potentiated muscular ones. These compounds effectively blocked mydriasis, tachycardia, and hyperemia. Substitution of H for OH abolishes psychotogenic properties as does quaternization of the piperidyl ring. Replacement of Ph with II in compounds containing N-Me or N-Et enhances psychotogenic effects. Substitution of 2-thienyl for Ph diminishes reaction duration but increases anticholinergic and antihistaminic potencies. The psychotogenic properties do not correlate with toxicity, antispasmodic potency, of mydriasis.

Archives Internationales de Pharmacodynamie et de Therapie published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, Related Products of piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Abood, L. G. published the artcileA new class of psychotogenic substances, Computed Properties of 13444-24-1, the publication is Mol. Mental Health, Papers Sci. Congrs. Brain Research Foundation; New York and Chicago (1959), 69-76, database is CAplus.

Piperidyl benzilate derivatives of formula CH₂(CH₂)₂NACH₂CHOCOCBRC₆H₅ were tested on humans for psychotogenic effects. With A, B, and R, resp., Et, OH, cyclohexyl; Et, OH, cyclopentyl; Me, OH, Ph; Me, OH, 2-thienyl; Et, OH, Ph; Et, OH, Pr; Et, H, Ph; 2Me, OH, Ph; and Et and Me, OH, Ph. With R as some cycloalkyl group the psychotogenic potency is greater than with phenyl substitution. If R is a thienyl group, the duration of the response is considerably less, although the psychotogenic effectiveness is about the same. The 4-piperidine linked isomers are less active than the 3 isomers. If A is Me, the maximum potency is obtained; with higher aliphatic chains the potency decreases. Replacement of H in the benzilic acid moiety by OH leads to a disappearance of potency. The same effect occurs if the piperidine N is made quaternary. No correlation between psychotogenic and anticholinergic potency was found.

Mol. Mental Health, Papers Sci. Congrs. Brain Research Foundation; New York and Chicago published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, Computed Properties of 13444-24-1.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Sklavounos, Constantine published the artcileD-α-Aminoadipic acid from cephalosporin C, Computed Properties of 72002-30-3, the publication is Organic Preparations and Procedures International (1984), 16(3-4), 165-9, database is CAplus.

The title compound (I) ([α]_D²⁵ = -25.7°, 2% 6N HCl) was prepared by deacylating cephalosporin C via the imino chloride and imino ether to give Me D-α-aminoadipate which was converted to lactam by treatment of base, crystallized, and hydrolyzed to I.

Organic Preparations and Procedures International published new progress about 72002-30-3. 72002-30-3 belongs to piperidines, auxiliary class Piperidine,Chiral,Carboxylic acid,Amide, name is (R)-6-Oxopiperidine-2-carboxylic acid, and the molecular formula is C11H8O3, Computed Properties of 72002-30-3.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Schultz, Otto E. published the artcileMechanism of local anesthetic action. 1. Receptor problem, SDS of cas: 13444-24-1, the publication is Pharmazie (1970), 25(8), 472-80, database is CAplus and MEDLINE.

Furfuryl alc. was treated 1 hr at -5° with PBr3 and the product treated with MeNH2 and alc. NaI 72 hr at 100-20° to give I. Treatment of I with HBr-HOAc gave a ring-opened product which was cyclized with KOH to give 63% II. Similarly prepared were 10 other compounds including III, IV, V, VI, and VII. The local anesthetic activity of these compounds vs. procaine-HCl (III) was determined III had 80% of the VIII activity. The mechanism of local anesthetic activity is discussed.

Pharmazie published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C8H5F3O2S, SDS of cas: 13444-24-1.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Fuson, Reynold C. published the artcileRing enlargement by rearrangement of the 1,2-aminochloroalkyl group; rearrangement of 1-ethyl-2-(chloromethyl)pyrrolidine to 1-ethyl-3-chloropiperidine, HPLC of Formula: 13444-24-1, the publication is Journal of the American Chemical Society (1948), 2760-2, database is CAplus.

Reduction of 1,2-dicarbethoxypyrrole over Raney Ni in dry MeOH at 70°/1500 lb. gives 95% 1,2-dicarbethoxypyrrolidine; further reduction over Cu chromite in EtOH at 250°/100 atm. gives 31% 1-ethyl-2-hydroxypyrrolidine (I); the HCl salt and benzoate-HCl are oils; benzoate picrate, m. 170.5-1.5°. Diethyl(tetrahydrofurfuryl)amine yields 43% 1-ethyl-3-hydroxypiperidine, which forms a HCl salt (II), m. 157-8°, and a benzoate picrate, yellow, m. 181.5-2.5°. I (4 g.) in 25 ml. CHCl₃ at 0°, treated with HCl to form the HCl salt and then with 4.8 g. SOCl₂ in CHCl₃, and the mixture stirred 30 min. at room temperature and refluxed 1 hr., gives 56% 1-ethyl-2-(chloromethyl)pyrrolidine-HCl (III), m. 165-70° (heated 20°/min.), solidifies, and m. 153.5-4°; slowly heated, III contracts at 165° and m. 193.5-4°; picrate, m. 128.5-9.5°. The Me₂CO used to wash the crude III yields 1.4 g. 1-methyl-2-(chloromethyl)pyrrolidine picrate (?) (IV), m. 163.5-4.5°; it is possible that I contained some 1-ethyl-2-(hydroxymethyl)pyrrolidine. II (5 g.) and 3.7 g. SOCl₂ in 50 ml. PhMe, refluxed 3 hrs., give 87% 1-ethyl-3-chloropiperidine (V) as the HCl salt (VI), m. 193.5-4°; a mixture of III and VI also m. 193.5-4°. The base from III appears to undergo rearrangement to V as rapidly as it is liberated, an ethylenimonium ion probably being an intermediate. The base (V) from VI does not undergo rearrangement on liberation. The attempt to prepare 1-methyl-3-chloropiperidine from IV was inconclusive.

Journal of the American Chemical Society published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, HPLC of Formula: 13444-24-1.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Abood, L. G. published the artcilePossible role of brain mitochondria in psychopharmacology, Application In Synthesis of 13444-24-1, the publication is Journal of Neuropsychiatry (1959), 92-5, database is CAplus.

cf. CA 53, 22487b. Experiments were performed on rat-brain mitochondria to determine the presence of cholinergic receptor sites. It was observed that the distribution of tritiated N-ethyl-3-piperidyl benzilate (JB-318) (I) was similar to that of acetylcholine in the cellular fractions of rat brain. The largest concentration was found in the mitochondria. It was concluded that the cholinergic receptor sites were in this fraction or granules associated with this fraction. The inhibition of a number of drugs upon the binding of I to mitochondria was chlorpromazine 80, 3-piperidyl benzilate (JB-305) and N,N’-piperazinodiethyl dibenzilate 50, hydroxyzine 44, and dinitrophenol 20%. It was suggested that if the receptor sites are confined to cytoplasmic particles, then the phenothiazine types of tranquilizers and the psycho-mimetic agents act at the mitochondrial level of the cell.

Journal of Neuropsychiatry published new progress about 13444-24-1. 13444-24-1 belongs to piperidines, auxiliary class Piperidine,Alcohol, name is 1-Ethylpiperidin-3-ol, and the molecular formula is C7H15NO, Application In Synthesis of 13444-24-1.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem