Wagner, Gabor et al. published their research in Archiv der Pharmazie (Weinheim, Germany) | CAS: 5472-49-1

1-(3-Chloropropyl)piperidine hydrochloride (cas: 5472-49-1) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Name: 1-(3-Chloropropyl)piperidine hydrochloride

SAR exploration of the non-imidazole histamine H3 receptor ligand ZEL-H16 reveals potent inverse agonism was written by Wagner, Gabor;Mocking, Tamara A. M.;Ma, Xiaoyuan;Slynko, Inna;Da Costa Pereira, Daniel;Breeuwer, Robin;Rood, Niek J. N.;van der Horst, Cas;Vischer, Henry F.;de Graaf, Chris;de Esch, Iwan J. P.;Wijtmans, Maikel;Leurs, Rob. And the article was included in Archiv der Pharmazie (Weinheim, Germany).Name: 1-(3-Chloropropyl)piperidine hydrochloride This article mentions the following:

Histamine H3 receptor (H3R) agonists without an imidazole moiety remain very scarce. Of these, ZEL-H16 (1) has been reported previously as a high-affinity non-imidazole H3R (partial) agonist. Our structure-activity relationship anal. using derivatives of 1 identified both basic moieties as key interaction motifs and the distance of these from the central core as a determinant for H3R affinity. However, in spite of the reported H3R (partial) agonism, in our hands, 1 acts as an inverse agonist for G伪i signaling in a CRE-luciferase reporter gene assay and using an H3R conformational sensor. Inverse agonism was also observed for all of the synthesized derivatives of 1. Docking studies and mol. dynamics simulations suggest ionic interactions/hydrogen bonds to H3R residues D1143.32 and E2065.46 as essential interaction points. In the experiment, the researchers used many compounds, for example, 1-(3-Chloropropyl)piperidine hydrochloride (cas: 5472-49-1Name: 1-(3-Chloropropyl)piperidine hydrochloride).

1-(3-Chloropropyl)piperidine hydrochloride (cas: 5472-49-1) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Name: 1-(3-Chloropropyl)piperidine hydrochloride

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The instant invention describes compounds having IL-6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by IL-6.

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The present invention relates to a compound of formula (I) wherein: Formula (II) means an aromatic ring wherein V is C or N and when V is N; Q is N or O, provided that R” does not exist when Q is O; R’ independently represent a hydrogen atom or a group chosen among a (C1-C3)alkyl group, a halogen atom, a hydroxy. group, a – COOR1 group, a -NO2 group, a -NR1R2 group, a morpholinyl or a morpholino group, a N- methylpiperazinyl group, a (Ci-C3)fluoroalkyl group, a -O-P(=O)-(OR3XOR4) group, a (C1-C4)alkoxy group and a -CN group, and can further be a group chosen among:(IIa), (IIIa) or anyone of its pharmaceutically acceptable salt, for use in the treatment and/or prevention of an inflammatory disease.

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A process for preparing a pyridone derivative (4), which comprises reacting the compound (1) with a hypochlorite or a hypobromite or with lead tetraacetate to give the compound (2), and reacting the compound (2) with the compound (3). Said process is preferably especially from the standpoint of safety. wherein R1 is hydrogen, alkyl, substituted alkyl, etc.; Y1 is hydrogen, alky, substituted alky, etc.; Y2 and Y3 are indenpently hydrogen, halogen, etc.; and L is alkyl, substituted alky, etc.

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A series of 9-acetamido-1,2,3 4-tetrahydrocarbazoles (2) and 9-(aminoalkyloxyethyl)-1,2,3,4-tetrahydrocarbazoles (4) were prepared and tested for their in vitro antitumor activity. Compounds 4 are highly cytotoxic in almost all subpanel cell lines when tested at 10-4 M, but showed a weak activity at the lowest concentrations employed.

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The therapy of complex neurodegenerative diseases requires the development of multitarget-directed drugs (MTDs). Novel indole derivatives with inhibitory activity towards acetyl/butyrylcholinesterases and monoamine oxidases A/B as well as the histamine H3 receptor (H3R) were obtained by optimization of the neuroprotectant ASS234 by incorporating generally accepted H3R pharmacophore motifs. These small-molecule hits demonstrated balanced activities at the targets, mostly in the nanomolar concentration range. Additional in vitro studies showed antioxidative neuroprotective effects as well as the ability to penetrate the blood?brain barrier. With this promising in vitro profile, contilisant (at 1 mg kg?1 i.p.) also significantly improved lipopolysaccharide-induced cognitive deficits.

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5-Acetyl-2-aroyl-beta-methyl-6-(beta-t-alkylaminoaldoxy)benzofurans (Va-g) have been synthesised by condensing 5-acetyl-2-aroyl-beta-methyl-6-hydroxybenzofuran (IIIa) with beta-t-alkylaminoalkyl halide hydrochlorides (IVa-g) in the presence of dry acetone-freshly baked potassium carbonate.The compounds (IIa,b) were obtained by refluxing resdiacetophenone (I) with omega-bromoacetophenones (IIa, b).Dibenzoylbenzo<1,2-b:5,4-b'>difurans (VIa, b) and their basic ethers (VIIa-g) have also been synthesised.Condensation of IIa with 5-acetyl-6-hydroxy-2,3-diphenylbenzofuran (VIII) results in 6-benzoyl-5-methyl-2,3-diphenylbenzo<1,2-b:5,4-b'>difuran (IX).

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The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.

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The invention provides a compound of formula I: STR1 or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.

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Chloroquine (CQ) has been used as first line malaria therapeutic drug for decades. Emergence of CQ drug-resistant Plasmodium falciparum malaria throughout endemic areas of the world has limited its clinical value. Mefloquine (MQ) has been used as an effective malaria prophylactic drug due to its being long-acting and having a high potency against blood stage P. falciparum (Pf). However, serious CNS toxicity of MQ has compromised its clinical value as a prophylaxis drug. Therefore, new and inexpensive antimalarial drugs with no cross-resistance to CQ or CNS toxicity are urgently needed to combat this deadly human disease. In this study, a series of new 4-amidinoquinoline (4-AMQ) and 10-amidinobenzonaphthyridine (10-AMB) derivatives were designed, prepared, and assessed to search for new therapeutic agents to replace CQ and MQ. The new derivatives displayed high activity in vitro and in vivo, with no cross-resistance to CQ, and none were toxic in mice up to 160 mpk × 3. The best compound shows IC50 < 1 ng/mL against D6, W2 and C235 Pf clones, low inhibitory activity in hERG K+ channel blockage testing, negativity in the Ames test, and 5/5 cure @ <15 mpk × 3 in mice infected with Plasmodium berghei. In addition to these desirable pharmacological profiles, compound 13b, one of the most active compounds, is metabolically stable in both human and mouse liver microsomal preparations and has a plasma t1/2 of 50 h in mice, which made it a good MQ replacement candidate. We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 5472-49-1, and how the biochemistry of the body works.Related Products of 5472-49-1

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