Bioorganic and medicinal Chemistry

Development of CXCR3 antagonists. Part 2: Identification of 2-amino(4-piperidinyl)azoles as potent CXCR3 antagonists

Organic Chemistry / Water / Humans / Mice / Animals / Amination / Bioorganic and medicinal Chemistry / Structure activity Relationship / Molecular Structure / Piperidines / Amination / Bioorganic and medicinal Chemistry / Structure activity Relationship / Molecular Structure / Piperidines

Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics

Organic Chemistry / Streptococcus pneumoniae / Amines / Staphylococcus aureus / Peptides / Antibacterial activity / Anti-Bacterial Agents / Enterococcus faecalis / Microbial Sensitivity Tests / Bioorganic and medicinal Chemistry / Biological activity / Structure activity Relationship / Molecular Structure / Antibacterial activity / Anti-Bacterial Agents / Enterococcus faecalis / Microbial Sensitivity Tests / Bioorganic and medicinal Chemistry / Biological activity / Structure activity Relationship / Molecular Structure

N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists

Organic Chemistry / Drug interactions / Chemokines and chemokine receptors / Humans / Calcium Signaling / Urea / Eosinophils / Bioorganic and medicinal Chemistry / Structure activity Relationship / Protein Binding / Piperidines / Urea / Eosinophils / Bioorganic and medicinal Chemistry / Structure activity Relationship / Protein Binding / Piperidines

Insecticidal anthranilic diamides: A new class of potent ryanodine receptor activators

Organic Chemistry / Calcium / Lepidoptera / Insecticides / Pesticide / Pesticides / Animals / Insects / Ryanodine Receptor / Amination / Receptor / Bioorganic and medicinal Chemistry / Structure activity Relationship / Chemical Synthesis / Calcium Ions / Molecular Structure / Intracellular / Pesticides / Animals / Insects / Ryanodine Receptor / Amination / Receptor / Bioorganic and medicinal Chemistry / Structure activity Relationship / Chemical Synthesis / Calcium Ions / Molecular Structure / Intracellular

Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist

Organic Chemistry / Pharmaceutical Chemistry / Mice / Animals / Drug Design / Molecular Conformation / Bioorganic and medicinal Chemistry / Pyrazoles / CB 1 receptor / Piperidines / Molecular Conformation / Bioorganic and medicinal Chemistry / Pyrazoles / CB 1 receptor / Piperidines

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy

Organic Chemistry / Cell line / Humans / Mice / Animals / Anti-inflammatory agents / Lipopolysaccharides / Rats / Tumor necrosis factor-alpha / Bioorganic and medicinal Chemistry / Heterocyclic compounds / Glucocorticoids / Anti-inflammatory agents / Lipopolysaccharides / Rats / Tumor necrosis factor-alpha / Bioorganic and medicinal Chemistry / Heterocyclic compounds / Glucocorticoids

Imidazopyridines as VLA-4 integrin antagonists

Organic Chemistry / Pharmaceutical Chemistry / Humans / Mice / Animals / Drug Design / Rats / Phenylalanine / Pyridines / Molecular Conformation / Bioorganic and medicinal Chemistry / Structure activity Relationship / Protein Binding / Drug Design / Rats / Phenylalanine / Pyridines / Molecular Conformation / Bioorganic and medicinal Chemistry / Structure activity Relationship / Protein Binding

Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors

Organic Chemistry / Animals / Rats / Bioorganic and medicinal Chemistry / Structure activity Relationship / Serine Protease / Molecular Structure / Serine Protease / Molecular Structure

7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: Design, synthesis, and biological activity

Organic Chemistry / Mice / Animals / Drug Design / Kinase inhibitor / Bioorganic and medicinal Chemistry / Biological activity / Aurora kinases / Structure activity Relationship / Molecular Structure / Vascular endothelial growth factor receptor / Bioorganic and medicinal Chemistry / Biological activity / Aurora kinases / Structure activity Relationship / Molecular Structure / Vascular endothelial growth factor receptor

Orally Efficacious NR2B-Selective NMDA Receptor Antagonists

Organic Chemistry / Pain / Animals / Motor Coordination / Rats / Carrageenan / Side Effect / Bioorganic and medicinal Chemistry / Structure activity Relationship / Hyperalgesia / Psychomotor Performance / Carrageenan / Side Effect / Bioorganic and medicinal Chemistry / Structure activity Relationship / Hyperalgesia / Psychomotor Performance

Insecticidal anthranilic diamides: A new class of potent ryanodine receptor activators

Organic Chemistry / Calcium / Lepidoptera / Insecticides / Pesticide / Pesticides / Animals / Insects / Ryanodine Receptor / Amination / Receptor / Bioorganic and medicinal Chemistry / Structure activity Relationship / Chemical Synthesis / Calcium Ions / Molecular Structure / Intracellular / Pesticides / Animals / Insects / Ryanodine Receptor / Amination / Receptor / Bioorganic and medicinal Chemistry / Structure activity Relationship / Chemical Synthesis / Calcium Ions / Molecular Structure / Intracellular

N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists

Organic Chemistry / Kinetics / Serotonin / Cell line / Humans / Drug Design / Serotonin Receptors / Radioligand Assay / Transfection / Molecular Conformation / Bioorganic and medicinal Chemistry / Structure activity Relationship / Recombinant Proteins / Serotonin antagonists / Tryptamines / Drug Design / Serotonin Receptors / Radioligand Assay / Transfection / Molecular Conformation / Bioorganic and medicinal Chemistry / Structure activity Relationship / Recombinant Proteins / Serotonin antagonists / Tryptamines

3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists

Organic Chemistry / Kinetics / Pharmacokinetics / Peroxidase / Cell line / In Vitro / Humans / Animals / Neutrophils / Rats / Rat / Bioorganic and medicinal Chemistry / Oxides / Structure activity Relationship / Chemical Synthesis / Interleukin / Binding affinity / In Vitro / Humans / Animals / Neutrophils / Rats / Rat / Bioorganic and medicinal Chemistry / Oxides / Structure activity Relationship / Chemical Synthesis / Interleukin / Binding affinity

Altertoxins with potent anti-HIV activity from Alternaria tenuissima QUE1Se, a fungal endophyte of Quercus emoryi

Organic Chemistry / HIV / Humans / Endophytes / Quercus / T lymphocytes / Bioorganic and medicinal Chemistry / Perylene / Alternaria / T lymphocytes / Bioorganic and medicinal Chemistry / Perylene / Alternaria

Aza-bicyclic amino acid carboxamides as α4β1/α4β7 integrin receptor antagonists

Organic Chemistry / Multiple sclerosis / Rheumatoid Arthritis / Inflammatory Bowel Disease / Mice / Female / Animals / Male / Integrins / Rats / Amino Acid Profile / Bioorganic and medicinal Chemistry / Lymphocytes / Structure activity Relationship / Molecular Structure / Female / Animals / Male / Integrins / Rats / Amino Acid Profile / Bioorganic and medicinal Chemistry / Lymphocytes / Structure activity Relationship / Molecular Structure

4-Alkyl- and 3,4-dialkyl-1,2,3,4,-tetrahydro-8-pyridono[5,6-g]quinolines: Potent, nonsteroidal androgen receptor agonists

Organic Chemistry / Kinetics / Humans / Animals / Androgens / Quinolones / Androgen Receptor / Bioorganic and medicinal Chemistry / Protein Binding / Dihydrotestosterone / Quinolones / Androgen Receptor / Bioorganic and medicinal Chemistry / Protein Binding / Dihydrotestosterone

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