All Stories

  1. Diazaborines as New Inhibitors of Human Neutrophil Elastase
  2. Starch nanocapsules containing a novel neutrophil elastase inhibitor with improved pharmaceutical performance
  3. Design of Modular G-quadruplex Ligands
  4. Drug discovery in tuberculosis. New drug targets and antimycobacterial agents
  5. Endoperoxide-8-aminoquinoline hybrids as dual-stage antimalarial agents with enhanced metabolic stability
  6. Spirotriazoline oxindoles: A novel chemical scaffold with in vitro anticancer properties
  7. Dipeptidyl Vinyl Sulfone as a Novel Chemical Tool to Inhibit HMGB1/NLRP3-Inflammasome and Inflamma-miRs in Aβ-Mediated Microglial Inflammation
  8. Targeting Gliomas: Can a New Alkylating Hybrid Compound Make a Difference?
  9. Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites
  10. Clickable 4-Oxo-β-lactam-Based Selective Probing for Human Neutrophil Elastase Related Proteomes
  11. Chemical Variations on the p53 Reactivation Theme
  12. Novel squaramides with in vitro liver stage antiplasmodial activity
  13. 11th National Meeting of Organic Chemistry and 4th Meeting of Therapeutic Chemistry
  14. Spirooxadiazoline oxindoles with promising in vitro antitumor activities
  15. Enantiopure Indolizinoindolones with in vitro Activity against Blood- and Liver-Stage Malaria Parasites
  16. Stabilization of porcine pancreatic elastase crystals by glutaraldehyde cross-linking
  17. Deoxycholic acid modulates cell death signaling through changes in mitochondrial membrane properties
  18. Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype
  19. From hybrid compounds to targeted drug delivery in antimalarial therapy
  20. Targeting KRAS Oncogene in Colon Cancer Cells with 7-Carboxylate Indolo[3,2-b]quinoline Tri-Alkylamine Derivatives
  21. KRAS oncogene repression in colon cancer cell lines by G-quadruplex binding indolo[3,2-c]quinolines
  22. N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: Design, synthesis and antiplasmodial activity
  23. Indolo[3,2-c]quinoline G-Quadruplex Stabilizers: a Structural Analysis of Binding to the Human Telomeric G-Quadruplex
  24. Targeting the Erythrocytic and Liver Stages of Malaria Parasites withs-Triazine-Based Hybrids
  25. 1.2 Designing Covalent Inhibitors: A Medicinal Chemistry Challenge
  26. Activity-based probes as molecular tools for biomarker discovery
  27. A unified approach toward the rational design of selective low nanomolar human neutrophil elastase inhibitors
  28. Discovery of C-shaped aurone human neutrophil elastase inhibitors
  29. The Cytotoxic Bile Acid DCA Modulates Apoptotic Signalling through Alteration of Mitochondrial Membrane Properties
  30. Analytical profiles of “legal highs” containing cathinones available in the area of Lisbon, Portugal
  31. Antiplasmodial Drugs in the Gas Phase: A CID and DFT Study of Quinolon-4(1H)-Imine Derivatives
  32. Tetraoxane–Pyrimidine Nitrile Hybrids as Dual Stage Antimalarials
  33. Probing the aurone scaffold against Plasmodium falciparum: Design, synthesis and antimalarial activity
  34. Bis-alkylamine Indolo[3,2- b ]quinolines as Hemozoin Ligands: Implications for Antimalarial Cytostatic and Cytocidal Activities
  35. Novel Endoperoxide-Based Transmission-Blocking Antimalarials with Liver- and Blood-Schizontocidal Activities
  36. Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents
  37. Optimization of O 3 -Acyl Kojic Acid Derivatives as Potent and Selective Human Neutrophil Elastase Inhibitors
  38. Flavones as isosteres of 4(1H)-quinolones: Discovery of ligand efficient and dual stage antimalarial lead compounds
  39. Squaric acid/4-aminoquinoline conjugates: Novel potent antiplasmodial agents
  40. Structural Optimization of Quinolon-4(1 H )-imines as Dual-Stage Antimalarials: Toward Increased Potency and Metabolic Stability
  41. Novel anti-Plasmodial hits identified by virtual screening of the ZINC database
  42. Cytotoxic bile acids, but not cytoprotective species, inhibit the ordering effect of cholesterol in model membranes at physiologically active concentrations
  43. Synthesis, G-Quadruplex Stabilisation, Docking Studies, and Effect on Cancer Cells of Indolo[3,2-b]quinolines with One, Two, or Three Basic Side Chains
  44. An Endoperoxide‐Based Hybrid Approach to Deliver Falcipain Inhibitors Inside Malaria Parasites
  45. Torins are potent antimalarials that block replenishment of Plasmodium liver stage parasitophorous vacuole membrane proteins
  46. Exploring the Molecular Basis of Qo bc 1 Complex Inhibitors Activity to Find Novel Antimalarials Hits
  47. Quinolin-4(1 H )-imines are Potent Antiplasmodial Drugs Targeting the Liver Stage of Malaria
  48. Contribution of Mass Spectrometry to the Study of Antimalarial Agents
  49. Five-membered iminocyclitol α-glucosidase inhibitors: Synthetic, biological screening and in silico studies
  50. Discovery of new heterocycles with activity against human neutrophile elastase based on a boron promoted one-pot assembly reaction
  51. Comparative in vitro and in vivo antimalarial activity of the indole alkaloids ellipticine, olivacine, cryptolepine and a synthetic cryptolepine analog
  52. Synthetic Condensed 1,4-naphthoquinone Derivative Shifts Neural Stem Cell Differentiation by Regulating Redox State
  53. Antitrypanosomal and cysteine protease inhibitory activities of alkyldiamine cryptolepine derivatives
  54. Peptidomimetic and Organometallic Derivatives of Primaquine Active against Leishmania infantum
  55. ChemInform Abstract: Microwave-Assisted Wittig Reaction of Semistabilized Nitro-Substituted Benzyltriphenyl-Phosphorous Ylides with Aldehydes in Phase-Transfer Conditions.
  56. N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases
  57. Comparative Analysis of In Vitro Rat Liver Metabolism of the Antimalarial Primaquine and a Derived Imidazoquine
  58. ChemInform Abstract: Efficient Synthesis of Spiroisoxazoline Oxindoles.
  59. Drug Screen Targeted at Plasmodium Liver Stages Identifies a Potent Multistage Antimalarial Drug
  60. 1 H NMR spectroscopic identification of protonable sites in cryptolepines with C-11 substituents containing two amino functionalities
  61. Four-Component Assembly of Chiral N–B Heterocycles with a Natural Product-Like Framework
  62. Targeting the Liver Stage of Malaria Parasites: A Yet Unmet Goal
  63. Squaric acid: a valuable scaffold for developing antimalarials?
  64. Structure based virtual screening for discovery of novel human neutrophil elastase inhibitors
  65. A carbamate-based approach to primaquine prodrugs: Antimalarial activity, chemical stability and enzymatic activation
  66. Efficient synthesis of spiroisoxazoline oxindoles
  67. Novel Potent Metallocenes against Liver Stage Malaria
  68. Aza vinyl sulfones: Synthesis and evaluation as antiplasmodial agents
  69. Identification of new antimalarial leads by use of virtual screening against cytochrome bc1
  70. Microwave-Assisted Wittig Reaction of Semistabilized Nitro-Substituted Benzyltriphenyl-Phosphorous Ylides with Aldehydes in Phase-Transfer Conditions
  71. Design and Evaluation of Primaquine-Artemisinin Hybrids as a Multistage Antimalarial Strategy
  72. Characterizing the Dynamics and Ligand-Specific Interactions in the Human Leukocyte Elastase through Molecular Dynamics Simulations
  73. Targeting COPD: advances on low-molecular-weight inhibitors of human neutrophil elastase
  74. Aspartic vinyl sulfones: Inhibitors of a caspase-3-dependent pathway
  75. Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials
  76. Incorporation of Basic Side Chains into Cryptolepine Scaffold: Structure−Antimalarial Activity Relationships and Mechanistic Studies
  77. New hope in the fight against malaria?
  78. C-11 diamino cryptolepine derivatives NSC748392, NSC748393, and NSC748394: Anticancer profile and G-quadruplex stabilization
  79. Endoperoxide Carbonyl Falcipain 2/3 Inhibitor Hybrids: Toward Combination Chemotherapy of Malaria through a Single Chemical Entity
  80. Bis-alkylamine quindolone derivatives as new antimalarial leads
  81. Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure–activity study
  82. A quantum mechanical study of novel potential inhibitors of cytochrome bc1 as antimalarial compounds
  83. Indoloquinolines as Scaffolds for Drug Discovery
  84. Cell Death Targets and Potential Modulators in Alzheimers Disease
  85. Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-β-lactam inhibitor of human leukocyte elastase
  86. Inhibitors of the Mitochondrial Electron Transport Chain and de novo Pyrimidine Biosynthesis as Antimalarials: The Present Status
  87. Effect of Synthesized Inhibitors on Babesipain-1, a New Cysteine Protease from the Bovine Piroplasm Babesia Bigemina
  88. 4-Oxo-β-lactams (Azetidine-2,4-diones) Are Potent and Selective Inhibitors of Human Leukocyte Elastase
  89. PRIMACENES: novel non-cytotoxic primaquine-ferrocene conjugates with anti-Pneumocystis carinii activity
  90. Reaction of naphthoquinones with substituted nitromethanes. Facile synthesis and antifungal activity of naphtho[2,3-d]isoxazole-4,9-diones
  91. Imidazoquines as Antimalarial and Antipneumocystis Agents †
  92. Anti-tumoral activity of imidazoquines, a new class of antimalarials derived from primaquine
  93. Dopamine- and tyramine-based derivatives of triazenes: Activation by tyrosinase and implications for prodrug design
  94. Design, synthesis and structure–activity relationships of (1H-pyridin-4-ylidene)amines as potential antimalarials
  95. Naphtho[2,3-d]isoxazole-4,9-dione-3-carboxylates: Potent, non-cytotoxic, antiapoptotic agents
  96. Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: Design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition
  97. Primaquine dipeptide derivatives bearing an imidazolidin-4-one moiety at the N-terminus as potential antimalarial prodrugs
  98. Structure–activity relationships for dipeptide prodrugs of acyclovir: Implications for prodrug design
  99. Primaquine revisited six decades after its discovery
  100. Bis{(E)-3-[(diethylmethylammonio)methyl]-N-[3-(N,N-dimethylsulfamoyl)-1-methylpyridin-4-ylidene]-4-methoxyanilinium} tetraiodide pentahydrate
  101. Electrospray ionization mass spectrometry as a valuable tool in the characterization of novel primaquine peptidomimetic derivatives
  102. Amino acids as selective acylating agents: regioselective N1-acylation of imidazolidin-4-one derivatives of the antimalarial drug primaquine
  103. Electrospray Ionization-Ion Trap Mass Spectrometry Study of PQAAPro and PQProAA Mimetic Derivatives of the Antimalarial Primaquine
  104. Imidazolidin-4-one peptidomimetic derivatives of primaquine: Synthesis and antimalarial activity
  105. Dipeptide Derivatives of AZT: Synthesis, Chemical Stability, Activation in Human Plasma, hPEPT1 Affinity, and Antiviral Activity
  106. Unanticipated Acyloxymethylation of Sumatriptan Indole Nitrogen Atom and its Implications in Prodrug Design
  107. Malaria Combination Therapies: Advantages and Shortcomings
  108. Azetidine-2,4-diones (4-Oxo-β-lactams) as Scaffolds for Designing Elastase Inhibitors
  109. Characterization of primaquine imidazolidin-4-ones with antimalarial activity by electrospray ionization-ion trap mass spectrometry
  110. Cryptolepine analogues containing basic aminoalkyl side-chains at C-11: Synthesis, antiplasmodial activity, and cytotoxicity
  111. Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones
  112. Cyclization-activated Prodrugs
  113. Michael Acceptors as Cysteine Protease Inhibitors
  114. The 1,4-naphthoquinone scaffold in the design of cysteine protease inhibitors
  115. Unanticipated Stereoselectivity in the Reaction of Primaquine α-Aminoamides with Substituted Benzaldehydes:  A Computational and Experimental Study †
  116. The efficiency of C-4 substituents in activating the β-lactam scaffold towards serine proteases and hydroxide ion
  117. Crystallization and Preliminary Diffraction Studies of Porcine Pancreatic Elastase in Complex with a Novel Inhibitor
  118. Aminocarbonyloxymethyl Ester Prodrugs of Flufenamic Acid and Diclofenac: Suppressing the Rearrangement Pathway in Aqueous Media
  119. Reactivity of imidazolidin-4-one derivatives of primaquine: implications for prodrug design
  120. The Bsmoc Group as a Novel Scaffold for the Design of Irreversible Inhibitors of Cysteine Proteases.
  121. Dipeptide vinyl sultams: Synthesis via the Wittig–Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum
  122. The Bsmoc group as a novel scaffold for the design of irreversible inhibitors of cysteine proteases
  123. Design, Synthesis, and Enzymatic Evaluation of N 1 -Acyloxyalkyl- and N 1 -Oxazolidin-2,4-dion-5-yl-Substituted β-lactams as Novel Inhibitors of Human Leukocyte Elastase
  124. Cyclization-activated prodrugs. Synthesis, reactivity and toxicity of dipeptide esters of paracetamol
  125. Imidazolidin-4-one Derivatives of Primaquine as Novel Transmission-Blocking Antimalarials
  126. Amidomethylation of Amodiaquine: Antimalarial N-Mannich Base Derivatives.
  127. Amidomethylation of amodiaquine: antimalarial N-Mannich base derivatives
  128. Synthesis of imidazolidin-4-one and 1H-imidazo[2,1-a]isoindole-2,5(3H,9bH)-dione derivatives of primaquine: scope and limitations
  129. Kinetics and Mechanism of Hydrolysis of N -Acyloxymethyl Derivatives of Azetidin-2-one
  130. Novel 3+1 mixed-ligand Technetium-99m complexes carrying dipeptides as monodentate ligands
  131. Improved Synthesis of Amino Acid and Dipeptide Chloromethyl Esters Using Bromochloromethane.
  132. Amino acids as selective sulfonamide acylating agents
  133. Improved Synthesis of Amino Acid and Dipeptide Chloromethyl Esters Using Bromochloromethane
  134. Synthesis, Stability and In Vitro Dermal Evaluation of Aminocarbonyloxymethyl Esters as Prodrugs of Carboxylic Acid Agents
  135. Design, Synthesis and Stability of N-Acyloxymethyl- and N-Aminocarbonyloxymethyl-2-azetidinones as Human Leukocyte Elastase Inhibitors
  136. Kinetics and mechanism of hydrolysis of N-amidomethylsulfonamides
  137. Acyloxymethyl as a drug protecting group. Part 7: Tertiary sulfonamidomethyl ester prodrugs of benzylpenicillin: chemical hydrolysis and anti-bacterial activity
  138. Acyloxymethyl as a drug protecting group. Part 6
  139. Cleavage of tertiary amidomethyl ester prodrugs of carboxylic acids by rat liver homogenates
  140. Metabolism of primaquine by liver homogenate fractions
  141. Phthalimidomethyl as a drug Pro-moiety. Probing its reactivity
  142. Acyloxymethyl as a drug protecting group. Synthesis and reactivity of N-acyloxymethylsulfonamide prodrugs
  143. A new direct synthesis of tertiary N-acyloxymethylamide prodrugs of carboxylic acid drugs
  144. Acyloxymethyl as a drug protecting group. Kinetics and mechanism of the hydrolysis of N-acyloxymethylbenzamides
  145. Triazene drug metabolites. Part 11. Synthesis of S-cysteinyl and related derivatives of N-hydroxymethyltriazenes
  146. Triazene drug metabolites. Part 10. Metal-ion catalysed decomposition of monoalkyltriazenes in ethanol solutions
  147. Synthesis of S-cysteinyl, S(N-acetylcysteinyl) and S-glutathionyl conjugates op N-hydroxymethyltriazenes
  148. Alkylating Agents