Category: 120570-05-0

Demian, Iulia; Gripshover, David F. published the artcile< High-performance liquid chromatographic determination of enantiomeric purity of 1-methyl-3-pyrrolidinol via derivatization with (R,R)-O,O-dibenzoyltartaric acid anhydride>, Application In Synthesis of 120570-05-0, the main research area is methylpyrrolidinol enantiomeric purity determination HPLC; liquid chromatog methylpyrrolidinol enantiomeric purity; benzoyltartaric acid anhydride derivatization methylpyrrolidinol.

The enantiomeric purity of 1-methyl-3-pyrrolidinol was determined by its diastereomeric derivatization with (R,R)-O,O-dibenzoyltartaric acid anhydride followed by reversed-phase HPLC separation with UV detection. The column used was packed with Zorbax C8, and the mobile phase was 50:50 MeOH-0.1% triethylamine solution (pH 4.2).

Journal of Chromatography published new progress about 120570-05-0. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Application In Synthesis of 120570-05-0.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Koltun, Elena; Richards, Steven; Chan, Vicky; Nachtigall, Jason; Du, Hongwang; Noson, Kevin; Galan, Adam; Aay, Naing; Hanel, Art; Harrison, Amanda; Zhang, Jeff; Won, Kwang-Ai; Tam, Danny; Qian, Fawn; Wang, Tao; Finn, Patricia; Ogilvie, Kathleen; Rosen, Jon; Mohan, Raju; Larson, Christopher; Lamb, Peter; Nuss, John; Kearney, Patrick published the artcile< Discovery of a new class of glucosylceramide synthase inhibitors>, Product Details of C7H14N2, the main research area is glucosylceramide synthase inhibitor heterocycle preparation SAR.

A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochem. and cellular potency as well as ADME properties led to compound 23c (I). Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo.

Bioorganic & Medicinal Chemistry Letters published new progress about Diabetes mellitus. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Product Details of C7H14N2.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Janetka, James W.; Almeida, Lynsie; Ashwell, Susan; Brassil, Patrick J.; Daly, Kevin; Deng, Chun; Gero, Thomas; Glynn, Roberta E.; Horn, Candice L.; Ioannidis, Stephanos; Lyne, Paul; Newcombe, Nicholas J.; Oza, Vibha B.; Pass, Martin; Springer, Stephanie K.; Su, Mei; Toader, Dorin; Vasbinder, Melissa M.; Yu, Dingwei; Yu, Yan; Zabludoff, Sonya D. published the artcile< Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors>, Computed Properties of 120570-05-0, the main research area is ureido thiophene carboxamide preparation checkpoint kinase inhibitor SAR.

Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Computed Properties of 120570-05-0.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Ni, Zhi-Jie; Barsanti, Paul; Brammeier, Nathan; Diebes, Anthony; Poon, Daniel J.; Ng, Simon; Pecchi, Sabina; Pfister, Keith; Renhowe, Paul A.; Ramurthy, Savithri; Wagman, Allan S.; Bussiere, Dirksen E.; Le, Vincent; Zhou, Yasheen; Jansen, Johanna M.; Ma, Sylvia; Gesner, Thomas G. published the artcile< 4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors>, Computed Properties of 120570-05-0, the main research area is aminobenzimidazolylquinolinone preparation CHK1 inhibitor; quinolinone amino benzimidazolyl preparation CHK1 inhibitor.

CHK-1 is one of the key enzymes regulating checkpoints in cellular growth cycles. Novel 4-(aminoalkylamino)-3-benzimidazolyl-2-quinolinones were prepared and assayed for their ability to inhibit CHK-1. These compounds are potent cell permeable CHK-1 inhibitors and showed a synergistic effect with a DNA-damaging agent, camptothecin.

Bioorganic & Medicinal Chemistry Letters published new progress about Cell cycle. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Computed Properties of 120570-05-0.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Kowalczyk, Bruce A.; Rohloff, John C.; Dvorak, Charles A.; Gardner, John O. published the artcile< Improved preparation of (R)- and (S)-3-aminoquinuclidine dihydrochloride>, Application In Synthesis of 120570-05-0, the main research area is quinuclidine amino hydrochloride preparation.

An improved procedure for the synthesis of either (R)- or (S)-3-aminoquinuclidine was developed. Key intermediate imine (I) was made in a one pot process using lithium oxide as the base and mol. sieves.

Synthetic Communications published new progress about 120570-05-0. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Application In Synthesis of 120570-05-0.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Demian, Iulia; Gripshover, David F. published the artcile< Enantiomeric purity determination of 3-aminoquinuclidine by diastereomeric derivatization and high-performance liquid chromatographic separation>, Related Products of 120570-05-0, the main research area is aminoquinuclidine enantiomer resolution HPLC; liquid chromatog aminoquinuclidine enantiomer resolution; benzoyltartaric anhydride chiral derivatization aminoquinuclidine resolution.

Four different diastereomeric derivatization methods were used for the HPLC and TLC separation of 3-aminoquinuclidine enantiomers. The chiral reagents used were S(-)-1-phenylethyl isocyanate, R(-)-1-naphthylethyl isocyanate, 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate, and the anhydrides of R,R(+)- and S,S(-)-O,O-dibenzoyltartaric acid (DBTAA). The TLC separations were carried out on silica gel plates; the HPLC used a Zorbax C8 and Zorbax Sil phase. All diastereomeric derivatives were strong UV absorbers at 254 nm. The best separation was achieved by HPLC with DBTAA, which allowed detection of the minor enantiomer down to 10-3 enantiomeric ratio.

Journal of Chromatography published new progress about Chromatographic chiral resolution. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Related Products of 120570-05-0.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Yang, Zhicai; Fairfax, David J.; Maeng, Jun-Ho; Masih, Liaqat; Usyatinsky, Alexander; Hassler, Carla; Isaacson, Soshanna; Fitzpatrick, Kevin; De Orazio, Russell J.; Chen, Jianqing; Harding, James P.; Isherwood, Matthew; Dobritsa, Svetlana; Christensen, Kevin L.; Wierschke, Jonathan D.; Bliss, Brian I.; Peterson, Lisa H.; Beer, Cathy M.; Cioffi, Christopher; Lynch, Michael; Rennells, W. Martin; Richards, Justin J.; Rust, Timothy; Khmelnitsky, Yuri L.; Cohen, Marlene L.; Manning, David D. published the artcile< Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists>, Recommanded Product: (S)-3-Amino-1-azabicyclo[2.2.2]octane, the main research area is irritable bowel syndrome IBS serotonin receptor antagonist 5HT3 antagonist; benzoxaole derivative SAR preparation.

A new class of 2-substituted benzoxazole carboxamides are presented as potent functional 5-HT3 receptor antagonists. The chem. series possesses nanomolar in vitro activity against human 5-HT3A receptors. A chem. optimization program was conducted and identified 2-aminobenzoxazoles as orally active 5-HT3 receptor antagonists with good metabolic stability. These novel analogs possess drug-like characteristics and have potential utility for the treatment of diseases attributable to improper 5-HT3 receptor function, especially diarrhea predominant irritable bowel syndrome (IBS-D).

Bioorganic & Medicinal Chemistry Letters published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Recommanded Product: (S)-3-Amino-1-azabicyclo[2.2.2]octane.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Feng, Li; Yu, Shujia; Wang, Hai; Yang, Shengwei; Li, Xue; Dai, Hongjuan; Zhao, Liwen; Jiang, Cheng; Wang, Yazhou published the artcile< Synthesis and biological evaluation of spirocyclic chromane derivatives as a potential treatment of prostate cancer>, Category: quinuclidine, the main research area is spirocyclic chromane preparation antitumor prostate cancer; HAT inhibitors; antitumor activity; p300/CBP.

Herein, new compounds from the lead compound A-485 were designed using mol. dynamic simulations. A series of new spirocyclic chroman derivatives was prepared, characterized and proven to be a potential treatment of prostate cancer. The most potent compound I inhibited the proliferation of enzalutamide-resistant 22Rv1 cells with an IC50 value of 96 nM. Furthermore, one of diastereomers of the compound I displayed favorable overall pharmacokinetic profiles, and better tumor growth inhibition than A-485 in an in vivo xenograft model.

Molecules published new progress about Antitumor agents. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Category: quinuclidine.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Kuroita, Takanobu; Marubayashi, Nobuhiro; Sano, Mitsuharu; Kanzaki, Kouji; Inaba, Kenichi; Kawakita, Takeshi published the artcile< Benzoxazines. II. Synthesis, conformational analysis, and structure-activity relationships of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives as potent and long-acting serotonin-3 (5-HT3) receptor antagonists>, SDS of cas: 120570-05-0, the main research area is serotonin antagonist antiemetic benoxazinecarboxamide analog preparation; structure activity serotonin antagonist benoxazinecarboxamide analog; conformation serotonin antagonist benoxazinecarboxamide analog preparation.

A series of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for S3 serotonin (5-HT3) receptor antagonistic activities by means of assays of 5-HT3 receptor binding and the ability to antagonize the von Bezold-Jarisch reflex in rats. The target compounds were analogs and derivatives of (S)-N-1-azabicyclo[2.2.2]oct-3-yl-6-chloro-3,4-dihydro-4-methyl-2H-1,4-benzoxazine-8-carboxamide (I). Replacement of the 1,4-benzoxazine ring with a 1,4-benzthiazine ring or seven-membered ring (i.e., 1,5-benzoxepine or 1,5-benzthiepine) resulted in decreased affinity for 5-HT3 receptor. Introduction of substituents at the 2 position of the 1,4-benzoxazine ring increased the antagonistic activities (di-Me > Me > dihydro > phenyl). Compounds bearing a 9-methyl-9-azabicyclo[3.3.1]non-3-yl moiety as the basic part of 3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide derivatives were equipotent to those bearing 1-azabicyclo[2.2.2]oct-3-yl moiety. The 9-methyl-9-azabicyclo[3.3.1]non-3-yl moiety was confirmed to adopt a boat-chair conformation on the basis of both NMR studies and X-rays anal. In this series, endo-6-chloro-3,4-dihydro-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-2,2,4-trimethyl-2H-1,4-benzoxazine-8-carboxamide showed the highest affinity for 5-HT3 receptors (Ki = 0.019 nM), and a long-lasting 5-HT3 receptor antagonistic activity as evidenced by antagonism to the von Bezold-Jarisch reflex in rats. Such a long-lasting 5-HT3 receptor antagonism would be attributed to the introduction of both two Me groups at the 2 position of the benzoxazine ring and the 9-methyl-9-azabicyclo[3.3.1]non-3-yl moiety, which adopted the boat-chair conformation.

Chemical & Pharmaceutical Bulletin published new progress about 5-HT3 antagonists. 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, SDS of cas: 120570-05-0.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider

Bodnar, Alice L.; Cortes-Burgos, Luz A.; Cook, Karen K.; Dinh, Dac M.; Groppi, Vincent E.; Hajos, Mihaly; Higdon, Nicole R.; Hoffmann, William E.; Hurst, Raymond S.; Myers, Jason K.; Rogers, Bruce N.; Wall, Theron M.; Wolfe, Mark L.; Wong, Erik published the artcile< Discovery and Structure-Activity Relationship of Quinuclidine Benzamides as Agonists of α7 Nicotinic Acetylcholine Receptors>, Quality Control of 120570-05-0, the main research area is quinuclidine benzamide library preparation nicotinic receptor agonist.

A library of benzamides was tested for α7 nicotinic acetylcholine receptor (nAChR) agonist activity using a chimeric receptor in a functional, cell-based, high-throughput assay. From this library, quinuclidine benzamides were found to have α7 nAChR agonist activity. The SAR diverged from the activity of this compound class verses the 5-HT3 receptor, a structural homolog of the α7 nAChR. PNU-282987 (I), the most potent compound from this series, was also shown to open native α7 nAChRs in cultured rat neurons and to reverse an amphetamine-induced gating deficit in rats.

Journal of Medicinal Chemistry published new progress about 5-HT3 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 120570-05-0 belongs to class quinuclidine, and the molecular formula is C7H14N2, Quality Control of 120570-05-0.

Referemce:
Quinuclidine – Wikipedia,
Quinuclidine | C7H13N | ChemSpider