All Stories

  1. High Throughput Screening to Identify Selective and Nonpeptidomimetic Proteasome Inhibitors As Antimalarials
  2. Structural Insights into PROTAC-Mediated Degradation of Bcl-xL
  3. A decade of malaria phenotypic screenings: Key lessons on the discovery and development of new antimalarial drugs
  4. Efforts Aimed To Reduce Attrition in Antimalarial Drug Discovery: A Systematic Evaluation of the Current Antimalarial Targets Portfolio
  5. The first example in literature of a termination of an oral drug based on IV microdose data
  6. The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold
  7. Hundreds of dual-stage antimalarial molecules discovered by a functional gametocyte screen
  8. Case Study of Small Molecules As Antimalarials: 2-Amino-1-phenylethanol (APE) Derivatives
  9. A New In Vivo Screening Paradigm to Accelerate Antimalarial Drug Discovery
  10. A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold
  11. Cyclopropyl Carboxamides, a Chemically Novel Class of Antimalarial Agents Identified in a Phenotypic Screen
  12. Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS)
  13. An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS
  14. Corrections to Falcipain Inhibitors: Optimization Studies of the 2-Pyrimidinecarbonitrile Lead Series
  15. Falcipain Inhibitors: Optimization Studies of the 2-Pyrimidinecarbonitrile Lead Series†
  16. Synthesis and Structure–Activity Relationships of 4-Pyridones as Potential Antimalarials
  17. Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 8. Computational Simulation of Ligand−Receptor Interaction of 5-HT1AR Agonists with Selectivity over α1-Adrenoceptors
  18. Design and synthesis of S-(−)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist
  19. Solid-phase versus solution synthesis of asymmetrically disubstituted furazano[3,4-b]pyrazines
  20. An improved two-resin method for the cleavage of tertiary amines from REM resin
  21. Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 6. Study of the 5-HT1A/α1-Adrenergic Receptor Affinity by Classical Hansch Analysis, Artificial Neural Networks, and Computational Simulation of Lig...
  22. Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 5. Study of the Physicochemical Influence of the Pharmacophore on 5-HT1A/α1-Adrenergic Receptor Affinity:  Synthesis of a New Derivative with Mixed ...
  23. Design and synthesis of 2-[4-[4-(m-(ethylsulfonamido)-phenyl)piperazin-1-yl]butyl]-1,3-dioxoperhydropyrrolo[1,2-c]imidazole (EF-7412) using neural networks. A selective derivative with mixed antagonist properties
  24. Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 4. 1-[ω-(4-Arylpiperazin-1-yl)alkyl]-3-(diphenylmethylene)- 2,5-pyrrolidinediones and -3-(9H-fluoren-9-ylidene)-2,5-pyrrolidinediones: Study of the Steric Requirem...
  25. 1-[ω-(4-Arylpiperazin-1-yl)alkyl]-3-diphenylmethylene-2,5-pyrrolidinediones as 5-HT1A receptor ligands: Study of the steric requirements of the terminal amide fragment on 5-HT1A affinity/selectivity
  26. Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 3. 2-[ω-(4-Arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines:  Study of the Influence of the Terminal Amide F...
  27. Synthesis and Structure−Activity Relationships of a New Model of Arylpiperazines. 2. Three-Dimensional Quantitative Structure−Activity Relationships of Hydantoin−Phenylpiperazine Derivatives with Affinity for 5-HT1A and α1 Recepto...
  28. 1H and13C NMR Spectra ofN- Ethyl- andN-Phenyl-β-carboline-1- carboxamides. Assignments by One- and Two-Dimensional Methods
  29. .ALPHA.1-Adrenoceptor Reagents. Synthesis of Some 5,6,11,11a-Tetrahydro-1H-imidazo(1',5':1,6)pyrido and 5,6,11,11b-Tetrahydro-1H-imidazo(1',5':1,2)pyrido(3,4-b)indole-1,3(2H)-diones.
  30. Reaction of 6-Hydroxytetrahydro-.BETA.-carboline-3-carboxylic Acids with Isocyanates and Isothiocyanates.