Category: 39546-32-2

Lalut, Julien published the artcileSynthesis and evaluation of novel serotonin 4 receptor radiotracers for single photon emission computed tomography, Recommanded Product: Piperidine-4-carboxamide, the publication is European Journal of Medicinal Chemistry (2016), 90-101, database is CAplus and MEDLINE.

In this study the synthesis of iodinated benzamide and ketone analogs was described. Their affinity for the 5-HT4R and their lipophilicity were evaluated and the most promising derivatives were evaluated ex-vivo for their binding to the receptor and for their ability to displace the reference ligand [¹²⁵I]-SB207710.

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

Cotman, Andrej E. published the artcileDesign, Synthesis, and Evaluation of Novel Tyrosine-Based DNA Gyrase B Inhibitors, Safety of Piperidine-4-carboxamide, the publication is Archiv der Pharmazie (Weinheim, Germany) (2017), 350(8), n/a, database is CAplus and MEDLINE.

The discovery and synthesis of new tyrosine-based inhibitors of DNA gyrase B (GyrB), which target its ATPase subunit, is reported. Twenty-four compounds were synthesized and evaluated for activity against DNA gyrase and DNA topoisomerase IV. The antibacterial properties of selected GyrB inhibitors were demonstrated by their activity against Staphylococcus aureus and Enterococcus faecalis in the low micromolar range. The most promising compounds, 8a and 13e, inhibited Escherichia coli and S. aureus GyrB with IC₅₀ values of 40 and 30 μM. The same compound also inhibited the growth of S. aureus and E. faecalis with minimal inhibitory concentrations (MIC₉₀) of 14 and 28 μg/mL, resp.

Archiv der Pharmazie (Weinheim, Germany) 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, Safety of Piperidine-4-carboxamide.

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

Pulici, Maurizio published the artcileOptimization of Diarylthiazole B-Raf Inhibitors: Identification of a Compound Endowed with High Oral Antitumor Activity, Mitigated hERG Inhibition, and Low Paradoxical Effect, Safety of Piperidine-4-carboxamide, the publication is ChemMedChem (2015), 10(2), 276-295, database is CAplus and MEDLINE.

Aberrant activation of the mitogen-activated protein kinase (MAPK)-mediated pathway components, RAF-MEK-ERK, is frequently observed in human cancers and clearly contributes to oncogenesis. As part of a project aimed at finding inhibitors of B-Raf, a key player in the MAPK cascade, the authors originally identified a thiazole derivative endowed with high potency and selectivity, optimal in vitro ADME properties, and good pharmacokinetic profiles in rodents, but that suffers from elevated hERG inhibitory activity. An optimization program was thus undertaken, focused mainly on the elaboration of the R¹ and R² groups of the scaffold. This effort ultimately led to I, which maintains favorable in vitro and in vivo properties, but lacks hERG liability. Besides exhibiting potent antiproliferative activity against only cell lines bearing B-Raf V600E or V600D mutations, compound I also intriguingly shows a weaker “paradoxical” activation of MEK in nonmutant B-Raf cells than other known B-Raf inhibitors. It also demonstrates very good efficacy in vivo against the A375 xenograft melanoma model (tumor volume inhibition >90% at 10 mg kg^-1); it is therefore a suitable candidate for preclin. development.

ChemMedChem 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, Safety of Piperidine-4-carboxamide.

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

Jose, Gilish published the artcileNew polyfunctional imidazo[4,5-C]pyridine motifs: Synthesis, crystal studies, docking studies and antimicrobial evaluation, Related Products of piperidines, the publication is European Journal of Medicinal Chemistry (2014), 288-297, database is CAplus and MEDLINE.

New antimicrobial agents, imidazo[4,5-c]pyridine derivatives were synthesized. The authors have developed a new synthetic protocol for the final reaction, an efficient microwave-assisted synthesis of imidazo[4,5-c]pyridines from substituted 3,4-diaminopyridine and carboxylic acids in presence of DBU mediated by T3P. The chem. structures of the new compounds were characterized by IR, ¹H NMR, ¹³C NMR, mass spectral anal. and elemental anal. In addition, single crystal x-ray diffraction also was recorded for compound 1-(7-(3-Fluorophenyl)-2-(phenoxymethyl)-1H-imidazo[4,5c]pyridin-4-yl)piperidine-3-carbonitrile. The in vitro antimicrobial activities of the compounds were conducted against various Gram-neg., Gram-pos. bacteria and fungi. Amongst the tested, seven compounds displayed promising antimicrobial activity. The mol. docking of GlcN-6-P synthase with newly synthesized compounds was carried out.

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, Related Products of piperidines.

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

Jose, Gilish published the artcileSynthesis, molecular docking, antimycobacterial and antimicrobial evaluation of new pyrrolo[3,2-c]pyridine Mannich bases, HPLC of Formula: 39546-32-2, the publication is European Journal of Medicinal Chemistry (2017), 275-288, database is CAplus and MEDLINE.

In this report, we describe the synthesis and biol. evaluation of a new series of pyrrolo[3,2-c]pyridine Mannich bases. The Mannich bases were obtained in good yields by one-pot three component condensation of pyrrolo[3,2-c]pyridine scaffold with secondary amines and excess of formaldehyde solution in AcOH. The chem. structures of the compounds were characterized by ¹H NMR, ¹³C NMR, LC/MS and elemental anal. Single crystal X-ray diffraction has been recorded for compound I ([C₂₃H₂₉ClN₄]⁺², H₂O). The in vitro antimicrobial activities of the compounds were evaluated against various bacterial and fungal strains using Agar diffusion method and Broth micro dilution method. Compounds II (n = 1, R = 4-Me-piperazin-1-yl, N-Bn-ethanamino; n = 2, R = N-Me-2-Ph-ethanamine, piperidine-3-carboxamide, piperidine-4-carboxamide) were showed good Gram-pos. antibacterial activity against S. aureus, B. flexus, C. sporogenes and S. mutans. Furthermore, in vitro antimycobacterial activity was evaluated against Mycobacterium tuberculosis H37Rv (ATCC 27294) using MABA. Compounds II (n = 2, R = N-Me-2-Ph-ethanamine, piperidine-3-carboxamide, piperidine-4-carboxamide) were showed good antitubercular activity against Mtb (MIC ≥6.25 μg/mL). Among the tested compounds, II (n = 2, R = piperidine-3-carboxamide) was showed excellent antimycobacterial activity against Mtb (MIC <0.78 μg/mL) and low cytotoxicity against the HEK-293T cell line (SI >>25). Mol. docking of the active compounds against glutamate racemase (MurI) and Mtb glutamine synthetase were explained the structure-activity observed in vitro.

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, HPLC of Formula: 39546-32-2.

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

Nojiri, Masutoshi published the artcileCharacterization of an enantioselective amidase from Cupriavidus sp. KNK-J915 (FERM BP-10739) useful for enzymatic resolution of racemic 3-piperidinecarboxamide, Synthetic Route of 39546-32-2, the publication is Journal of Molecular Catalysis B: Enzymatic (2014), 136-142, database is CAplus.

A novel amidase (CsAM) acting on (R,S)-N-benzyl-3-piperidinecarboxamide was purified from Cupriavidus sp. KNK-J915 (FERM BP-10739) and characterized. The enzyme acts on (R,S)-N-benzyl-3-piperidinecarboxamide S-selectively to yield (R)-N-benzyl-3-piperidinecarboxamide. Anal. gel filtration column chromatog. and SDS-PAGE revealed that the enzyme is a tetramer with a subunit of approx. 47 kDa. It has a broad substrate spectrum against nitrogen-containing heterocyclic amides. Its optimal pH and temperature are 8.0-9.0 and 50 °C, resp. The CsAM gene was cloned and sequenced, and it was found to comprise 1341 bp and encode a polypeptide of 46,388 Da. The deduced amino acid sequence exhibited 78% identity to that of a putative amidase (CnAM) from Cupriavidus necator JMP134. The cultured cells of recombinant Escherichia coli producing CnAM could be used for the S-selective hydrolysis of (R,S)-N-benzyl-3-piperidinecarboxamide but could not be used for the S-selective hydrolysis of (R,S)-3-piperidinecarboxamide because of its very low level of selectivity. In contrast, the cultured cells of recombinant E. coli producing CsAM could hydrolyze both (R,S)-N-benzyl-3-piperidinecarboxamide and (R,S)-3-piperidinecarboxamide with high S-selectivity.

Journal of Molecular Catalysis B: Enzymatic 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, Synthetic Route of 39546-32-2.

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

Ledneczki, Istvan published the artcileDiscovery of novel steroidal histamine H₃ receptor antagonists/inverse agonists, Application In Synthesis of 39546-32-2, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(19), 4525-4530, database is CAplus and MEDLINE.

Emerging from an HTS campaign, novel steroid-based histamine H₃ receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in compound I as lead mol. During the lead optimization due to the versatile modifications of diamino steroid derivatives, several in vitro potent compounds with subnanomolar binding affinities to histamine H₃ receptors were found. The unfavorable binding to rat muscarinic receptors was successfully reduced by tuning the basicity. Compound II showed significant in vivo activity in the rat dipsogenia model and could serve as a pharmacol. tool in the future.

Bioorganic & Medicinal Chemistry Letters 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, Application In Synthesis of 39546-32-2.

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

Dhanabal, T. published the artcileGrowth, spectral, dielectric and antimicrobial studies on 4-piperidinium carboxylamide picrate crystals, Recommanded Product: Piperidine-4-carboxamide, the publication is Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy (2014), 694-700, database is CAplus and MEDLINE.

Single crystal of 4-piperidinium carboxylamide picrate was grown by slow evaporation solution growth technique at ambient temperature The average dimensions of grown crystal were 0.7 × 0.3 × 0.2 cm³. The solubility of the compound was analyzed using methanol and acetone. Optical property of the compound was ascertained by UV-visible absorption spectral study. The sharp and well defined Bragg peaks observed in the powder X-ray diffraction pattern confirm its crystallinity. The different kinds of protons and carbons in the compound were confirmed by ¹H and ¹³C NMR spectral analyses. The presence of various functional groups in the compound was assigned through polarized Raman spectral study. The mech. property of the crystal was measured by Vicker’s microhardness test and the compound was found to be soft material. The dielec. constant and dielec. loss of the crystal decrease with increase in frequency. The antibacterial and antifungal activities of the crystal were studied by disk diffusion method and found that the compound shows good inhibition efficiency against various bacteria and fungi species.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy 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

Luo, Zonghua published the artcileSynthesis and Evaluation of Multi-Target-Directed Ligands against Alzheimer’s Disease Based on the Fusion of Donepezil and Ebselen, COA of Formula: C6H12N2O, the publication is Journal of Medicinal Chemistry (2013), 56(22), 9089-9099, database is CAplus and MEDLINE.

Benzylpiperidinylalkyl benzoisoselenazolones I [R = H, MeO; R¹ = H, Cl, F, MeO; X = (CH₂)_n; n = 1-4] were prepared as donepezil-ebselen hybrids for potential use as anti-Alzheimer’s disease agents. I (R = R¹ = MeO; n = 2) was one of the most potent acetylcholinesterase inhibitors of the compounds tested (IC₅₀ values of 0.042 μM for Electrophorus electricus acetylcholinesterase and 0.097 μM for human acetylcholinesterase) and was found to be a strong butyrylcholinesterase inhibitor with an IC₅₀ value of 1.586 μM, to possess rapid H₂O₂ and peroxynitrite scavenging activity and glutathione peroxidase-like activity (ν₀ = 123.5 μM min^-1), and to be a substrate of mammalian thioredoxin reductase. I (R = R¹ = MeO; n = 2) showed no acute toxicity at doses of up to 2000 mg/kg; by comparing its permeation in an artificial blood-brain barrier permeation assay, I (R = R¹ = MeO; n = 2) was expected to be able to penetrate the central nervous system.

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, COA of Formula: C6H12N2O.

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

Beuchel, Andreas published the artcileStructure-Activity Relationship of Anti-Mycobacterium abscessus Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors, COA of Formula: C6H12N2O, the publication is ACS Medicinal Chemistry Letters (2022), 13(3), 417-427, database is CAplus and MEDLINE.

Mycobacterium abscessus causes difficult-to-cure pulmonary infections. The bacterium is resistant to most anti-infective agents, including first line antituberculosis (anti-TB) drugs. MMV688844 (844) is a piperidine-4-carboxamide (P4C) with bactericidal properties against M. abscessus. We recently identified DNA gyrase as the mol. target of 844. Here, we present in silico docking and genetic evidence suggesting that P4Cs display a similar binding mode to DNA gyrase as gepotidacin. Gepotidacin is a member of the Novel Bacterial Topoisomerase Inhibitors (NBTIs), a new class of nonfluoroquinolone DNA gyrase poisons. Thus, our work suggests that P4Cs present a novel structural subclass of NBTI. We describe structure-activity relationship studies of 844 leading to analogs showing increased antibacterial activity. Selected derivatives were tested for their inhibitory activity against recombinant M. abscessus DNA gyrase. Further optimization of the lead structures led to improved stability in mouse plasma and increased oral bioavailability.

ACS Medicinal Chemistry Letters 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, COA of Formula: C6H12N2O.

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