Heterocyclic Building Blocks-piperidine

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

D’Amato, Erica M. published the artcileSelective Aromatic C-H Hydroxylation Enabled by η⁶-Coordination to Iridium(III), Formula: C11H21BF4N2O2, the publication is Organometallics (2015), 34(18), 4626-4631, database is CAplus and MEDLINE.

Authors report here an aromatic C-H hydroxylation protocol in which the arene is activated through η⁶-coordination to an iridium(III) complex. η⁶-Coordination of the arene increases its electrophilicity and allows for high positional selectivity of hydroxylation at the site of least electron d. Through investigation of intermediate η⁵-cyclohexadienyl adducts and arene exchange reactions, it was evaluated that incorporation of arene π-activation into a catalytic cycle for C-H functionalization.

Organometallics published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C11H21BF4N2O2, Formula: C11H21BF4N2O2.

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

Imberdis, Thibaut published the artcileCell models of lipid-rich α-synuclein aggregation validate known modifiers of α-synuclein biology and identify stearoyl-CoA desaturase, Safety of 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide, the publication is Proceedings of the National Academy of Sciences of the United States of America (2019), 116(41), 20760-20769, database is CAplus and MEDLINE.

Microscopy of Lewy bodies in Parkinson’s disease (PD) suggests they are not solely filamentous deposits of α-synuclein (αS) but also contain vesicles and other membranous material. We previously reported the existence of native αS tetramers/multimers and described engineered mutations of the αS KTKEGV repeat motifs that abrogate the multimers. The resultant excess monomers accumulate in lipid membrane-rich inclusions associated with neurotoxicity exceeding that of natural familial PD mutants, such as E46K. Here, we use the αS “3K” (E35K+E46K+E61K) engineered mutation to probe the mechanisms of reported small-mol. modifiers of αS biochem. and then identify compounds via a medium-throughput automated screen. αS 3K, which forms round, vesicle-rich inclusions in cultured neurons and causes a PD-like, L-DOPA-responsive motor phenotype in transgenic mice, was fused to YFP, and fluorescent inclusions were quantified. Live-cell microscopy revealed the highly dynamic nature of the αS inclusions: for example, their rapid clearance by certain known modulators of αS toxicity, including tacrolimus (FK506), isradipine, nilotinib, nortriptyline, and trifluoperazine. Our automated 3K cellular screen identified inhibitors of stearoyl-CoA desaturase (SCD) that robustly prevent the αS inclusions, reduce αS 3K neurotoxicity, and prevent abnormal phosphorylation and insolubility of αS E46K. SCD inhibition restores the E46K αS multimer:monomer ratio in human neurons, and it actually increases this ratio for overexpressed wild-type αS. In accord, conditioning 3K cells in saturated fatty acids rescued, whereas unsaturated fatty acids worsened, the αS phenotypes. Our cellular screen allows probing the mechanisms of synucleinopathy and refining drug candidates, including SCD inhibitors and other lipid modulators.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 1032229-33-6. 1032229-33-6 belongs to piperidines, auxiliary class Metabolic Enzyme,SCD, name is 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide, and the molecular formula is C20H22ClN3O3, Safety of 4-(2-Chlorophenoxy)-N-(3-(methylcarbamoyl)phenyl)piperidine-1-carboxamide.

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

Milo, Anat published the artcileA data-intensive approach to mechanistic elucidation applied to chiral anion catalysis, Recommanded Product: 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, the publication is Science (Washington, DC, United States) (2015), 347(6223), 737-743, database is CAplus and MEDLINE.

Knowledge of chem. reaction mechanisms can facilitate catalyst optimization, but extracting that knowledge from a complex system is often challenging. Here, the authors present a data-intensive method for deriving and then predictively applying a mechanistic model of an enantioselective organic reaction. As a validating case study, the authors selected an intramol. dehydrogenative C-N coupling reaction, catalyzed by chiral phosphoric acid derivatives, in which catalyst-substrate association involves weak, noncovalent interactions. Little was previously understood regarding the structural origin of enantioselectivity in this system. Catalyst and substrate substituent effects were probed by systematic phys. organic trend anal. Plausible interactions between the substrate and catalyst that govern enantioselectivity were identified and supported exptl., indicating that such an approach can afford an efficient means of leveraging mechanistic insight so as to optimize catalyst design.

Science (Washington, DC, United States) published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C11H21BF4N2O2, Recommanded Product: 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate.

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

Yousif, M. N. M. published the artcileSynthesis and Anticancer Activity of New Substituted Piperidinones Linked to Pyrimidine, Thiazole, and Triazole Glycoside Derivatives, Computed Properties of 826-36-8, the publication is Russian Journal of General Chemistry (2019), 89(8), 1673-1682, database is CAplus.

New piperidinone incorporating pyrimidine, triazine, diazipine, oxatriazine, and thiazole derivatives have been synthesized starting with tetramethylpipridin-4-one. Structures of the newly synthesized compounds are characterized on the basis of spectroscopic and anal. data. The anticancer activity of the prepared compounds has been studied in vitro against HCT-116 and MCF-7 human cancer cells using the MTT assay. A number of compounds demonstrates potent activity towards both cell lines with IC₅₀ values comparable with doxorubicin.

Russian Journal of General Chemistry published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C17H37NO3, Computed Properties of 826-36-8.

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

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

Yu, V. K. published the artcileEsters of 1-(alkoxyalkyl)-4-piperidinols, SDS of cas: 512778-95-9, the publication is Izvestiya Ministerstva Obrazovaniya i Nauki Respubliki Kazakhstan, Natsional’noi Akademii Nauk Respubliki Kazakhstan, Seriya Khimicheskaya (2002), 70-76, database is CAplus.

4-Piperidinols I (n = 2, R = Me, Et; n = 3, R = Bu, decyl) were prepared by NaBH₄ reduction of the 4-piperidinones. I were esterified with acid chlorides and anhydrides to give the acetates, propanoates, and benzoates, all isolated as the hydrochlorides. The benzoate hydrochlorides exhibited higher local anesthetic activity than lidocaine.

Izvestiya Ministerstva Obrazovaniya i Nauki Respubliki Kazakhstan, Natsional’noi Akademii Nauk Respubliki Kazakhstan, Seriya Khimicheskaya published new progress about 512778-95-9. 512778-95-9 belongs to piperidines, auxiliary class Piperidine,Alcohol,Ether, name is 1-(2-Methoxyethyl)piperidin-4-ol, and the molecular formula is C12H10O4S, SDS of cas: 512778-95-9.

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

Tarumoto, Yusuke published the artcileChemical inhibition of SIK3 as a therapeutic strategy in acute myeloid leukemia, Product Details of C32H34ClN7O3, the publication is Ketsueki Naika (2020), 81(4), 529-534, database is CAplus.

A review. Acute myeloid leukemia AML, a type of hematopoietic aneurysm, is caused by an excessive increase in undifferentiated bone marrow cells. These results suggest that SIK drugs can selectively suppress AML proliferation, indicating that SIK blockade is a candidate for an effective AML treatment strategy. Results show chem. inhibition of SIK3 as therapeutic strategy in acute myeloid leukemia.

Ketsueki Naika published new progress about 1936529-65-5. 1936529-65-5 belongs to piperidines, auxiliary class Immunology/Inflammation,SIK, name is 3-(2-Chloro-6-methylphenyl)-7-((2-methoxy-4-(1-methylpiperidin-4-yl)phenyl)amino)-1-(5-methoxypyridin-2-yl)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one, and the molecular formula is C2H2N3NaS, Product Details of C32H34ClN7O3.

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

Reitsema, Robert H. published the artcileNovel rearrangement of a piperidine ring, Application In Synthesis of 13444-24-1, the publication is Journal of the American Chemical Society (1949), 2041-3, database is CAplus.

cf. C.A. 43, 6206i. 1-Ethyl-3-chloropiperidine-HCl (I) (18.4 g.) and 21.4 g. PhCH₂NH₂ in 20 cc. H₂O, heated 48 hrs. at 65-75°, give 73.4% 1-ethyl-2-(benzylaminomethyl)pyrrolidine (II), b₁ 134° (dipicrate, m. 190-1°). 1-Methyl-3-chloropiperidine yields 42% of the 1-Me homolog of II, b_0.2-0.3 110-12° (dipicrate, m. 172-3°). II (2.18 g.) in 50 cc. absolute EtOH, shaken overnight with 2 g. Pd-C (but not with Pt oxide) at 50°, gives 1-ethyl-2-(aminomethyl)pyrrolidine (III), whose dipicrate m. 177-8.5°; III results also from I and alc. NH₃ (20 days at room temperature). I (16 g.), 30.2 g. 8-amino-6-methoxyquinoline, and 25 cc. H₂O, heated 20 hrs. at 60-70° and 2 hrs. at 110°, give 9.1 g. 6-methoxy-8-(1-ethyl-2-pyrrolidylmethylamino)quinoline (IV), b_0.2 186-90°, whose di-HCl salt m. 214-16°, and dipicrate m. 202.5-3.5°. 1-Ethyl-3-piperidone, reduced in MeOH over Raney Ni at 125° and 2270 lb., gives 1-ethyl-3-hydroxypiperidine, whose benzoate-HCl m. 197-8°. IV is less effective for clinical use than many of the new antimalarials.

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, Application In Synthesis of 13444-24-1.

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