212 results on '"Hale, Jeffrey J."'
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2. Current Drug Discovery
3. Chemical, Biochemical, Pharmacokinetic, and Biological Properties of L-680, 833: A Potent, Orally Active Monocyclic β-Lactam Inhibitor of Human Polymorphonuclear Leukocyte Elastase
4. Pharmacological evaluation of LH-21, a newly discovered molecule that binds to cannabinoid CB1 receptor
5. MK-7128, a novel CB1 receptor inverse agonist, improves scopolamine-induced learning and memory deficits in mice
6. Synthesis, stereochemical determination and biochemical characterization of the enantiomeric phosphate esters of the novel immunosuppressive agent FTY720
7. Chemical, biochemical, pharmacokinetic, and biological properties of L-680, 833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase
8. Synthesis of hypusine and other polyamines using dibenzyltriazones for amino protection
9. Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia
10. Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder
11. Discovery of benzamides as potent human β3 adrenergic receptor agonists
12. Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)
13. Investigation of piperazine benzamides as human β 3 adrenergic receptor agonists for the treatment of overactive bladder
14. Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1–3 (HIF PHD1–3) for the Treatment of Anemia
15. Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket
16. Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors
17. Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors
18. A new class of prolylcarboxypeptidase inhibitors, Part 1: Discovery and evaluation
19. A new class of prolylcarboxypeptidase inhibitors, Part 2: The aminocyclopentanes
20. Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors
21. Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors
22. Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine
23. The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors
24. Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: Synthesis, SAR and biological evaluation
25. Synthesis and evaluation of N-[(1 S,2 S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists
26. Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)
27. Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation
28. 1,3,8-Triazaspiro[4.5]decane-2,4-diones as Efficacious Pan-Inhibitors of Hypoxia-Inducible Factor Prolyl Hydroxylase 1–3 (HIF PHD1–3) for the Treatment of Anemia
29. Prolyl hydroxylase domain-containing protein inhibitors as stabilizers of hypoxia-inducible factor: small molecule-based therapeutics for anemia
30. Discovery ofN-[(4R)-6-(4-Chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a Novel Cannabinoid-1 Receptor (CB1R) Inverse Agonist for the Treatment of Obesity
31. ChemInform Abstract: 1,3,4-Trisubstituted Pyrrolidine CCR5 Receptor Antagonists. Part 1. Discovery of the Pyrrolidine Scaffold and Determination of Its Stereochemical Requirements.
32. ChemInform Abstract: 1,3,4-Trisubstituted Pyrrolidine CCR5 Receptor Antagonists. Part 2. Lead Optimization Affording Selective, Orally Bioavailable Compounds with Potent anti-HIV Activity.
33. Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists
34. 1-Sulfonyl-4-acylpiperazines as Selective Cannabinoid-1 Receptor (CB1R) Inverse Agonists for the Treatment of Obesity
35. SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P 1) with enhanced pharmacokinetic properties
36. A One‐Pot Synthesis of 3‐Substituted‐5‐carbonylmethyl‐1,2,4‐oxadiazoles from β‐Keto Esters and Amidoximes under Solvent‐Free Conditions.
37. SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties
38. Identification of Leu276 of the S1P1Receptor and Phe263 of the S1P3Receptor in Interaction with Receptor Specific Agonists by Molecular Modeling, Site-Directed Mutagenesis, and Affinity Studies
39. A “One‐Pot” Synthesis of α‐1,2,4‐Oxadiazolo Esters from Malonic Diesters and Amidoximes under Solvent‐Free Conditions.
40. Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes
41. Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor
42. 2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors
43. 2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists
44. Synthesis and Study of Alendronate Derivatives as Potential Prodrugs of Alendronate Sodium for the Treatment of Low Bone Density and Osteoporosis
45. Discovery of Potent 3,5-Diphenyl-1,2,4-oxadiazole Sphingosine-1-phosphate-1 (S1P1) Receptor Agonists with Exceptional Selectivity against S1P2 and S1P3
46. Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties
47. A Rational Utilization of High-Throughput Screening Affords Selective, Orally Bioavailable 1-Benzyl-3-carboxyazetidine Sphingosine-1-phosphate-1 Receptor Agonists
48. Selecting Against S1P3 Enhances the Acute Cardiovascular Tolerability of 3-(N-Benzyl)aminopropylphosphonic Acid S1P Receptor Agonists.
49. Potent S1P Receptor Agonists Replicate the Pharmacologic Actions of the Novel Immune Modulator FTY720.
50. Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors
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