Regioselective Oxidative Arylation of Indoles Bearing <i>N-</i>Alkyl Protecting Groups: Dual C−H Functionalization via a Concerted Metalation−Deprotonation Mechanism

Shathaverdhan Potavathri, Kyle C. Pereira, Serge I. Gorelsky, +3

Journal of the American Chemical Society

Chemical EngineeringCross-coupling ReactionEngineeringAlkene MetathesisOxidative Cross-coupling +12

Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride (LY 156758), a remarkably effective estrogen antagonist with only minimal intrinsic estrogenicity

Charles D. Jones, Mary G. Jevnikar, Andrew Pike, +5

Journal of Medicinal Chemistry

TPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2 H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an Agonist Selective for α2- and α3-Containing GABAA Receptors, Is a Nonsedating Anxiolytic in Rodents and Primates

John Atack, Keith A. Wafford, Spencer J. Tye, +15

Journal of Pharmacology and Experimental Therapeutics

Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines

Per Sauerberg, Preben H. Olesen, Susanne Nielsen, +6

Journal of Medicinal Chemistry

Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT_1D Receptor Ligands with Improved Pharmacokinetic Profiles

Monique B. van Niel, Ian Collins, Margaret S. Beer, +18

Journal of Medicinal Chemistry

Combinatorial ChemistryMolecular PharmacologyMedicinal ChemistryPharmaceutical Science5-Ht1d Receptor Ligands +13

Imidazo[1,2<i>-a</i>]pyrimidines as Functionally Selective and Orally Bioavailable GABA_Aα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

Simon Goodacre, Leslie J. Street, David J. Hallett, +16

Journal of Medicinal Chemistry

PsychopharmacologyPharmacotherapyExperimental PharmacologySocial SciencesMolecular Pharmacology +17

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-<i>N</i>-methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Jeffrey W. Johannes, Amber Balazs, Derek Barratt, +40

Journal of Medicinal Chemistry

3-Heteroaryl-2-pyridones:  Benzodiazepine Site Ligands with Functional Selectivity for α2/α3-Subtypes of Human GABA_A Receptor-Ion Channels

Ian Collins, Christopher R. Moyes, William B. Davey, +13

Journal of Medicinal Chemistry

PharmacotherapySocial SciencesMolecular PharmacologyMedicinal ChemistryLow Binding Selectivity +14

Nonsteroidal inhibitors of human type I steroid 5-.alpha.-reductase

Charles D. Jones, James E. Audia, David E. Lawhorn, +7

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryMedicineAltmetric Attention ScoreClinical Pharmacology +9

The discovery of fused pyrrole carboxylic acids as novel, potent d-amino acid oxidase (DAO) inhibitors

Tim Sparey, Pravien Abeywickrema, Sarah Almond, +14

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistryMedicineNatural Sciences +5