Biological activities of guanidine compounds, 2008 – 2012 update

Hedgehog pathway inhibitors: a patent review (2009 – present)

(2013) Matthew Kyle Hadden   EXPERT OPINION ON THERAPEUTIC PATENTS

Aminoalkyl Derivatives of Guanidine Diaromatic Minor Groove Binders with Antiprotozoal Activity

(2013) Caitriona McKeever et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lower Rim Guanidinocalix[4]arenes: Macrocyclic Nonviral Vectors for Cell Transfection

(2012) Valentina Bagnacani et al.   BIOCONJUGATE CHEMISTRY

Transition metal-catalyzed N-arylations of amidines and guanidines

(2012) Tom R. M. Rauws et al.   CHEMICAL SOCIETY REVIEWS

Amidines, isothioureas, and guanidines as nucleophilic catalysts

(2012) James E. Taylor et al.   CHEMICAL SOCIETY REVIEWS

1-(2-Mercaptobenzenesulfonyl)-3-hydroxyguanidines – Novel potent antiproliferatives, synthesis and in vitro biological activity

(2012) Kamil Brożewicz et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Histone deacetylase inhibitors: a patent review (2009 – 2011)

(2012) Vincenzo Carafa et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Histamine H4 receptor ligands and their potential therapeutic applications: an update

(2012) Róbert Kiss et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Small-molecule BACE1 inhibitors: a patent literature review (2006 – 2011)

(2012) Gary Probst et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Novel NMDA receptor modulators: an update

(2012) Rose M Santangelo et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Synthesis of a C-Iminoribofuranoside Analog of the Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitor FK866

(2012) Annabelle Gillig et al.   HELVETICA CHIMICA ACTA

Rational Design of a Low Molecular Weight, Stable, Potent, and Long-Lasting GPR103 Aza-β3-pseudopeptide Agonist

(2012) Cindy Neveu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enhanced Anti-influenza Agents Conjugated with Anti-inflammatory Activity

(2012) Kung-Cheng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Inhibitors of Amyloid β-Peptide 1–42 Aggregation

(2012) Laura C. López et al.   JOURNAL OF MEDICINAL CHEMISTRY

Acyl Guanidine Inhibitors of β-Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis

(2012) Samuel W. Gerritz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Oseltamivir Phosphonate Congeners as Anti-influenza Agents

(2012) Ting-Jen R. Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of High-Affinity Macrocyclic Peptidomimetics to Block the Menin-Mixed Lineage Leukemia 1 (MLL1) Protein–Protein Interaction

(2012) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

The NAMPT inhibitor FK866 reverts the damage in spinal cord injury

(2012) Emanuela Esposito et al.   Journal of Neuroinflammation

Synthesis of Symmetrical and Unsymmetrical N,N′-Diaryl Guanidines via Copper/N-Methylglycine-Catalyzed Arylation of Guanidine Nitrate

(2012) Hui Xing et al.   JOURNAL OF ORGANIC CHEMISTRY

The Utility of Hedgehog Signaling Pathway Inhibition for Cancer

(2012) S. Sahebjam et al.   ONCOLOGIST

Palladium-Catalyzed C–H Functionalization Using Guanidine as a Directing Group: Ortho Arylation and Olefination of Arylguanidines

(2012) Jiaan Shao et al.   ORGANIC LETTERS

Small molecules aimed at type III secretion systems to inhibit bacterial virulence

(2012) Lun K. Tsou et al.   MedChemComm

Design and Synthesis of Potent, Selective Inhibitors of Matriptase

(2012) Éloïc Colombo et al.   ACS Medicinal Chemistry Letters

Polyamine analogs modulate gene expression by inhibiting lysine-specific demethylase 1 (LSD1) and altering chromatin structure in human breast cancer cells

(2011) Qingsong Zhu et al.   AMINO ACIDS

N-Hydroxy-N′-aminoguanidines as anti-cancer lead molecule: QSAR, synthesis and biological evaluation

(2011) Arijit Basu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Understanding the benefit of metformin use in cancer treatment

(2011) Ryan JO Dowling et al.   BMC Medicine

Guanylated Diamines, Triamines, and Polyamines: Chemistry and Biological Properties

(2011) Daniele Castagnolo et al.   CHEMICAL REVIEWS

Molecular modeling study and synthesis of novel dicationic flexible triaryl guanidines and imidamides as antiprotozoal agents

(2011) Reem K. Arafa et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, structural characterization and in vitro biological screening of some homoleptic copper(II) complexes with substituted guanidines

(2011) Ghulam Murtaza et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Mechanistic enhancement of the intestinal absorption of drugs containing the polar guanidino functionality

(2011) Jing Sun et al.   Expert Opinion on Drug Metabolism & Toxicology

Chemical Conjugation of the Neuropeptide Kyotorphin and Ibuprofen Enhances Brain Targeting and Analgesia

(2011) Marta M. B. Ribeiro et al.   MOLECULAR PHARMACEUTICS

An Amino Acid-based Amphoteric Liposomal Delivery System for Systemic Administration of siRNA

(2011) Roger C Adami et al.   MOLECULAR THERAPY

Once-daily treatment of ADHD with guanfacine: patient implications

(2011) Brandon Strange   Neuropsychiatric Disease and Treatment

Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents

(2010) Yong Qian et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and in vitro evaluation of 18F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET

(2010) Edward G. Robins et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small-Molecule Inhibitors of the Hedgehog Signaling Pathway as Cancer Therapeutics

(2010) Stefan Peukert et al.   ChemMedChem

Efficacy of Combining GMX1777 with Radiation Therapy for Human Head and Neck Carcinoma

(2010) H. Kato et al.   CLINICAL CANCER RESEARCH

Review article: Asymmetric dimethylarginine as a mediator of vascular dysfunction and a marker of cardiovascular disease and mortality: an intriguing interaction with diabetes mellitus

(2010) Maike Anderssohn et al.   Diabetes & Vascular Disease Research

Chemical Delivery System of Metaiodobenzylguanidine (MIBG) to the Central Nervous System

(2010) Fabienne Gourand et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of the First Low-Molecular-Weight Inhibitors of Matriptase-2

(2010) Mihiret Tekeste Sisay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of Guanidines From Azides: A General and Straightforward Methodology In Carbohydrate Chemistry

(2010) Andrés G. Santana et al.   JOURNAL OF ORGANIC CHEMISTRY

Pharmacology and Antitumor Activity of ABC294640, a Selective Inhibitor of Sphingosine Kinase-2

(2010) K. J. French et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The chemistry and biology of organic guanidine derivatives

(2010) Roberto G. S. Berlinck et al.   NATURAL PRODUCT REPORTS

Alzheimer's disease: strategies for disease modification

(2010) Martin Citron   NATURE REVIEWS DRUG DISCOVERY

Synoxazolidinones A and B: Novel Bioactive Alkaloids from the AscidianSynoicum pulmonaria

(2010) Margey Tadesse et al.   ORGANIC LETTERS

Molecular Dendritic Transporter Nanoparticle Vectors Provide Efficient Intracellular Delivery of Peptides

(2009) Sharon K. Hamilton et al.   ACS Nano

Symmetric dimethylarginine, an endogenous marker of glomerular filtration rate, and the risk for microalbuminuria in young people with type 1 diabetes

(2009) M L. Marcovecchio et al.   ARCHIVES OF DISEASE IN CHILDHOOD

Developing Dual and Specific Inhibitors of Dimethylarginine Dimethylaminohydrolase-1 and Nitric Oxide Synthase: Toward a Targeted Polypharmacology To Control Nitric Oxide

(2009) Yun Wang et al.   BIOCHEMISTRY

Discovery and structure–activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers

(2009) Han-Zhong Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Tethered thiazolidinone dimers as inhibitors of the bacterial type III secretion system

(2009) Toni Kline et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

(2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors

(2009) Sunkyung Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Sulfonamides with the N-alkyl-N′-dialkylguanidine moiety as 5-HT7 receptor ligands

(2009) Paweł Zajdel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430

(2009) Herman D Lim et al.   BRITISH JOURNAL OF PHARMACOLOGY

Bicyclic-guanidines, -guanidinates and -guanidinium salts: wide ranging applications from a simple family of molecules

(2009) Martyn P. Coles   CHEMICAL COMMUNICATIONS

Synthesis and Na+/H+Exchanger-1 Inhibitory Activity of Substituted (Quinolinecarbonyl)guanidine Derivatives

(2009) Dan Mao et al.   CHEMISTRY & BIODIVERSITY

Biological activities of guanidine compounds

(2009) Franciszek Saczewski et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Gastrosplenic Fistula From Hodgkin's Lymphoma

(2009) Carolyn D. Seib et al.   JOURNAL OF CLINICAL ONCOLOGY

Benzylguanidines and Other Galegine Analogues Inducing Weight Loss in Mice

(2009) Geoffrey D. Coxon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of New Linear Guanidines and Macrocyclic Amidinourea Derivatives Endowed with High Antifungal Activity againstCandidaspp. andAspergillusspp.†

(2009) Fabrizio Manetti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of Amidine, Guanidine, and Thiourea Derivatives of 2-Amino(6-trifluoromethoxy)benzothiazole as Neuroprotective Agents Potentially Useful in Brain Diseases

(2009) Maurizio Anzini et al.   JOURNAL OF MEDICINAL CHEMISTRY

An Antimicrobial Guanidine-Bearing Sesterterpene from the Cultured CyanobacteriumScytonemasp.

(2009) Shunyan Mo et al.   JOURNAL OF NATURAL PRODUCTS

Oligocarbonate Molecular Transporters: Oligomerization-Based Syntheses and Cell-Penetrating Studies

(2009) Christina B. Cooley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhalation of sphingosine kinase inhibitor attenuates airway inflammation in asthmatic mouse model

(2008) Teruaki Nishiuma et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Anticancer agent CHS-828 inhibits cellular synthesis of NAD

(2008) Uffe Høgh Olesen et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Structure–activity relationship of novel and known inhibitors of human dimethylarginine dimethylaminohydrolase-1: Alkenyl-amidines as new leads

(2008) Jürke Kotthaus et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification of novel non-peptide CXCR4 antagonists by ligand-based design approach

(2008) Satoshi Ueda et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Serine Protease Matriptase-2 (TMPRSS6) Inhibits Hepcidin Activation by Cleaving Membrane Hemojuvelin

(2008) Laura Silvestri et al.   Cell Metabolism

CXCR4, Inhibitors and Mechanisms of Action

(2008) Xiangyang Liang   Chemical Biology & Drug Design

Discovery of Novel Anticancer Compounds Based on a Quinoxalinehydrazine Pharmacophore

(2008) Jinxia Deng et al.   ChemMedChem

Activation of AMP-Activated Protein Kinase by Metformin Improves Left Ventricular Function and Survival in Heart Failure

(2008) Susheel Gundewar et al.   CIRCULATION RESEARCH

Macrocyclization of Di-Boc-guanidino-alkylamines Related to Guazatine Components: Discovery and Synthesis of Innovative Macrocyclic Amidinoureas

(2008) Daniele Castagnolo et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Guanidine and 2-Aminoimidazoline Aromatic Derivatives as α2-Adrenoceptor Antagonists. 2. Exploring Alkyl Linkers for New Antidepressants

(2008) Fernando Rodriguez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Substituted Aminoalkylguanidines as Potential Antihyperglycemic and Food Intake-Reducing Agents

(2008) Emanuela Tassoni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Subnanomolar Arginine-Glycine-Aspartate-Based αVβ3/αVβ5Integrin Binders Embedding 4-Aminoproline Residues

(2008) Franca Zanardi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Substituted 2-Imino-5-arylidenethiazolidin-4-one Inhibitors of Bacterial Type III Secretion

(2008) Toni Kline et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Bis(2-aminoimidazoline) and Bisguanidine DNA Minor Groove Binders with Potent in Vivo Antitrypanosomal and Antiplasmodial Activity

(2008) Fernando Rodríguez et al.   JOURNAL OF MEDICINAL CHEMISTRY

The chemistry and biology of organic guanidine derivatives

(2008) Roberto G. S. Berlinck et al.   NATURAL PRODUCT REPORTS

Meta-iodobenzyl guanidine for detection and staging of neuroendocrine tumors

(2008) Daniel Pryma et al.   NUCLEAR MEDICINE AND BIOLOGY

Taming the PI3K team to hold inflammation and cancer at bay

(2008) Emilio Hirsch et al.   PHARMACOLOGY & THERAPEUTICS

Pharmacological Inhibition of Nicotinamide Phosphoribosyltransferase/Visfatin Enzymatic Activity Identifies a New Inflammatory Pathway Linked to NAD

(2008) Nathalie Busso et al.   PLoS One