Category: 未分类

Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi was written by Koovits, Paul J.;Dessoy, Marco A.;Matheeussen, An;Maes, Louis;Caljon, Guy;Mowbray, Charles E.;Kratz, Jadel M.;Dias, Luiz C.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.COA of Formula: C12H21NO3 This article mentions the following:

The structure-activity relationship of a 4-Azaindole-2-piperidine compound selected from GlaxoSmithKline’s recently disclosed open-resource “Chagas box” and possessing moderate activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, is presented. Despite considerable medicinal chem. efforts, a suitably potent and metabolically stable compound could not be identified to advance the series into in vivo studies. This research should be of interest to those in the area of neglected diseases and in particular anti-kinetoplastid drug discovery. In the experiment, the researchers used many compounds, for example, tert-Butyl 3-acetylpiperidine-1-carboxylate (cas: 858643-92-2COA of Formula: C12H21NO3).

tert-Butyl 3-acetylpiperidine-1-carboxylate (cas: 858643-92-2) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.COA of Formula: C12H21NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Enantioseparation of paroxetine precursors by HPLC on amylose and tartardiamide-based chiral stationary phases was written by Bao, Zongbi;Su, Baogen;Yang, Yiwen;Ren, Qilong. And the article was included in Journal of Liquid Chromatography & Related Technologies in 2008.Category: piperidines This article mentions the following:

Two important precursors of antidepressant trans-(-)-paroxetine, i.e., trans-4-(4′-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine and trans-3- ethoxycarbonyl-4-(4′-fluorophenyl)-1-methylpiperidine-2,6-dione were directly separated by HPLC on Chiralpak AD-H and Kromasil CHI-TBB columns. All the experiments were conducted in the normal phase mode. The mobile phases were mixtures of n-hexane and alc. modifiers including ethanol, 2-propanol, and 1-propanol, with or without addition of diethylamine. Excellent separation was obtained for both enantiomers. Effects and content of polar alc. modifiers on enantioseparation was studied. An unusual retention behavior was observed, i.e., the retention of enantiomers increased when the alc. modifier was changed from 2-propanol to ethanol. The elution orders of the enantiomers on both columns were examined The thermodn. parameters obtained from van’t Hoff plots were all neg., which indicated that the chiral separation were enthalpically driven. In the experiment, the researchers used many compounds, for example, ((3R,4S)-rel-4-(4-Fluorophenyl)-1-methylpiperidin-3-yl)methanol (cas: 109887-53-8Category: piperidines).

((3R,4S)-rel-4-(4-Fluorophenyl)-1-methylpiperidin-3-yl)methanol (cas: 109887-53-8) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Optimized Inhibitors of Soluble Epoxide Hydrolase Improve in Vitro Target Residence Time and in Vivo Efficacy was written by Lee, Kin Sing Stephen;Liu, Jun-Yan;Wagner, Karen M.;Pakhomova, Svetlana;Dong, Hua;Morisseau, Christophe;Fu, Samuel H.;Yang, Jun;Wang, Peng;Ulu, Arzu;Mate, Christina A.;Nguyen, Long V.;Hwang, Sung Hee;Edin, Matthew L.;Mara, Alexandria A.;Wulff, Heike;Newcomer, Marcia E.;Zeldin, Darryl C.;Hammock, Bruce D.. And the article was included in Journal of Medicinal Chemistry in 2014.Electric Literature of C16H20F3N3O3 The following contents are mentioned in the article:

Diabetes is affecting the life of millions of people. A large proportion of diabetic patients suffer from severe complications such as neuropathic pain, and current treatments for these complications have deleterious side effects. Thus, alternate therapeutic strategies are needed. Recently, the elevation of epoxy-fatty acids through inhibition of soluble epoxide hydrolase (sEH) was shown to reduce diabetic neuropathic pain in rodents. In this report, the authors describe a series of newly synthesized sEH inhibitors I [R¹ = 4-CF₃C₆H₄, 4-CF₃OC₆H₄; (CF₃)₂CFC₆H₄, etc.; R² = MeCO, MeCH₂CO, MeCH₂CH₂CO, etc.] with at least 5-fold higher potency and doubled residence time inside both the human and rodent sEH enzyme than previously reported inhibitors. These inhibitors also have better phys. properties and optimized pharmacokinetic profiles. The optimized inhibitor selected from this new series displayed improved efficacy of almost 10-fold in relieving pain perception in diabetic neuropathic rats as compared to the approved drug, gabapentin, and previously published sEH inhibitors. Therefore, these new sEH inhibitors could be an attractive alternative to treat diabetic neuropathy in humans. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Electric Literature of C16H20F3N3O3).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Electric Literature of C16H20F3N3O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A study on drug utilization evaluation in patients admitted with cardiovascular diseases at a tertiary care hospital was written by Hussain, Yousuf Md;Sultana, Syeda Juveria;Batool, Syeda;Prakash, J. Sai;Dussa, Kanchana N.;Unnisa, Mehraj. And the article was included in International Journal of Pharmacy and Pharmaceutical Research in 2021.Application of 83799-24-0 The following contents are mentioned in the article:

Cardiovascular diseases have become a major cause of morbidity and mortality globally. A prospective observational study was carried out in an inpatient department of cardiol. in a tertiary care hospital. The duration of the study was 4 mo i.e., from Oct. 2018 to Jan. 2019. The data was obtained from the patient′s medical record and was documented in the especially designed data collection form. One hundred and forty four patients were enrolled in the study. In our study 70.1% were male and 29.9% were female. Maximum number of patients i.e., 35.4% was in the age group of 51-60 years. In the present study, the prevalence of coronary artery disease was high. Hypertension and Diabetes were the most common co-morbid conditions observed The study showed higher incidence of drug use as single agents (83.36%) which is appreciable. Most commonly prescribed categories of cardiovascular drugs were antihypertensives (24.06%) and antiplatelets (23.31%) indicating high prevalence of hypertension and coronary artery disease in patients. Along with brand name, Generic name of the drug was mentioned in every prescription. Antibiotics were prescribed in 32.64% patients and injection was prescribed in 76.39% patients. Extensive polypharmacy (10.2 drugs per prescription) was noticed in the prescriptions. The prescribing pattern of drugs can be improved by reducing the number of drugs per prescription. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Application of 83799-24-0).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Canale, Vittorio published the artcileDesign, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties, Formula: C10H20N2O2, the main research area is dihydrobenzofuranoxy ethyl piperidine preparation antidepressant activity green chem SAR; 5-HT7 receptor antagonist; depression; forced swim test; medicinal mechanochemistry; α2 adrenoceptor antagonist.

The complex pathophysiol. of depression, together with the limits of currently available antidepressants, has resulted in the continuous quest for alternative therapeutic strategies. Numerous findings suggest that pharmacol. blockade ofα2-adrenoceptor might be beneficial for the treatment of depressive symptoms by increasing both norepinephrine and serotonin levels in certain brain areas. The antidepressant properties of 5-HT7 receptor antagonists have been widely demonstrated in a large set of animal models. Considering the potential therapeutic advantages in targeting both α2-adrenoceptors and 5-HT7 receptors, a small series of arylsulfonamide derivatives of (dihydrobenzofuranoxy)ethyl piperidines I (Ar = 4-fluorophenyl, naphthalen-1-yl, isoquinolin-4-yl, etc.; m = 0,1) as dually active ligands were designed. Following green chem. principles, the designed compounds were synthesized entirely using a sustainable mechanochem. approach. The identified compound I (Ar = 5-chloro-2-fluorophenyl (II)) behaved as a potent α2A/5-HT7 receptor antagonist and displayed moderate-to-high selectivity over α1-adrenoceptor subtypes and selected serotonin and dopaminergic receptors. Finally, (II) improved performance of mice in the forced swim test, displaying similar potency to the reference drug mirtazapine.

Molecules published new progress about 5-HT antagonists. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Formula: C10H20N2O2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem