- New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives
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Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a receptor antagonists which can improve deteriorated social behavior in humans and can treat the core symptoms of
- Baska, Ferenc,Bata, Imre,Bozó, éva,Cselenyák, Attila,Domány-Kovács, Katalin,Kordás, Krisztina Szondiné,Kurkó, Dalma,Makó, Attila,Mohácsi, Réka,Szántó, Gábor
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- Structure-activity relationships of highly cytotoxic copper(II) complexes with modified indolo[3,2- c ]quinoline ligands
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A number of indolo[3,2-c]quinolines were synthesized and modified at the lactam unit to provide a peripheral binding site able to accommodate metal ions. Potentially tridentate ligands HL1a-HL4a and HL 1b-HL4b w
- Primik, Michael F.,Goeschl, Simone,Jakupec, Michael A.,Roller, Alexander,Keppler, Bernhard K.,Arion, Vladimir B.
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- "Methylene Bridge" to 5-HT3 Receptor Antagonists: Conformationally Constrained Phenylguanidines
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Arylguanidines, depending upon their aromatic substitution pattern, display varying actions at 5-HT3 receptors (e.g., partial agonist, agonist, superagonist). Here, we demonstrate that conformational constraint of these agents as dihydroquinazo
- Abdelkhalek, Ahmed S.,Alley, Genevieve S.,Alwassil, Osama I.,Khatri, Shailesh,Mosier, Philip D.,Nyce, Heather L.,White, Michael M.,Schulte, Marvin K.,Dukat, Ma?gorzata
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p. 1380 - 1389
(2018/11/23)
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- Base-Promoted Synthesis of 2-Aryl Quinazolines from 2-Aminobenzylamines in Water
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A transition-metal-free procedure for the synthesis of a highly valuable class of heteroaromatics, quinazolines, was developed by using easily available 2-aminobenzylamines and α,α,α-trihalotoluenes. The transformation proceeded smoothly in the presence of only sodium hydroxide and molecular oxygen in water at 100 °C, furnishing a variety of 2-aryl quinazolines. The crystallization process of the crude reaction mixture for the purification of the solid products circumvents huge solvent-consuming workup and column chromatographic techniques, which make the overall process more sustainable and economical.
- Chatterjee, Tanmay,Kim, Dong In,Cho, Eun Jin
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p. 7423 - 7430
(2018/07/29)
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- Preparation of triazolobenzodiazepine derivatives as Vasopressin V1a antagonists
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This Letter describes the synthesis of a number of fused tricyclic and bicyclic triazolobenzodiazepines for the Vasopressin V1a antagonist programme.
- Beal, David M.,Bryans, Justin S.,Johnson, Patrick S.,Newman, Julie,Pasquinet, Christelle,Peakman, Torren M.,Ryckmans, Thomas,Underwood, Toby J.,Wheeler, Simon
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p. 5913 - 5917
(2011/11/14)
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- Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: Structure-activity relationship elucidation
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The optimisation of affinity and selectivity in a novel series of dual 5-HT5A/5-HT7 receptor ligands is described. Brain penetrant 2-aminodihydroquinazolines with low nanomolar affinities were identified.
- Peters, Jens-Uwe,Luebbers, Thomas,Alanine, Alexander,Kolczewski, Sabine,Blasco, Francesca,Steward, Lucinda
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p. 256 - 261
(2008/12/23)
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- TRIAZOLE COMPOUNDS USEFUL IN THERAPY
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A compound of formula (I), or a pharmaceutically acceptable derivative thereof, wherein V represents -(CH2)d(O)e-, -CO-, or -CH(C1-6 alkyl)-; W is -0-, -S(O)a , or -N(R1')-R1 rep
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- New Synthesis of Fused Pyrimidine Derivatives via ortho-(Isocyanomethyl)nitroaromatic Compounds
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An efficient synthesis of functionalized fused pyrimidine derivatives from the respective ortho-(isocyanomethyl)nitroarenes is described.Hydrolysis of the isocyano group in the title isonitriles followed by catalytic reduction of the nitro group and subsequent cyclocondensation of the diamine formed with orthoesters leads to the final products.
- Ostrowski, Stanislaw
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p. 180 - 187
(2007/10/03)
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