All Stories

  1. The critical role of PSAC channel in malaria parasite survival is driven home by phenotypic screening under relevant nutrient levels
  2. High Throughput Screening to Identify Selective and Nonpeptidomimetic Proteasome Inhibitors As Antimalarials
  3. Structural Insights into PROTAC-Mediated Degradation of Bcl-xL
  4. A decade of malaria phenotypic screenings: Key lessons on the discovery and development of new antimalarial drugs
  5. Efforts Aimed To Reduce Attrition in Antimalarial Drug Discovery: A Systematic Evaluation of the Current Antimalarial Targets Portfolio
  6. The first example in literature of a termination of an oral drug based on IV microdose data
  7. The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold
  8. Hundreds of dual-stage antimalarial molecules discovered by a functional gametocyte screen
  9. Case Study of Small Molecules As Antimalarials: 2-Amino-1-phenylethanol (APE) Derivatives
  10. A New In Vivo Screening Paradigm to Accelerate Antimalarial Drug Discovery
  11. A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold
  12. Cyclopropyl Carboxamides, a Chemically Novel Class of Antimalarial Agents Identified in a Phenotypic Screen
  13. Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS)
  14. An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS
  15. Corrections to Falcipain Inhibitors: Optimization Studies of the 2-Pyrimidinecarbonitrile Lead Series
  16. Falcipain Inhibitors: Optimization Studies of the 2-Pyrimidinecarbonitrile Lead Series†
  17. Synthesis and Structure–Activity Relationships of 4-Pyridones as Potential Antimalarials
  18. 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
  19. 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
  20. Solid-phase versus solution synthesis of asymmetrically disubstituted furazano[3,4-b]pyrazines
  21. An improved two-resin method for the cleavage of tertiary amines from REM resin
  22. 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...
  23. 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 ...
  24. 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
  25. 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...
  26. 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
  27. 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...
  28. 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...
  29. 1H and13C NMR Spectra ofN- Ethyl- andN-Phenyl-β-carboline-1- carboxamides. Assignments by One- and Two-Dimensional Methods
  30. .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.
  31. Reaction of 6-Hydroxytetrahydro-.BETA.-carboline-3-carboxylic Acids with Isocyanates and Isothiocyanates.