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The Baylis-Hillman reaction: a novel source of attraction, opportunities, and challenges in synthetic chemistry

Chemical Society reviews, 2007-01, Vol.36 (10), p.1581-1588

2007

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GRL-09510, a Unique P2-Crown-Tetrahydrofuranylurethane -Containing HIV-1 Protease Inhibitor, Maintains Its Favorable Antiviral Activity against Highly-Drug-Resistant HIV-1 Variants in vitro

Scientific reports, 2017-09, Vol.7 (1), p.12235-12, Article 12235

2017

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Single atom changes in newly synthesized HIV protease inhibitors reveal structural basis for extreme affinity, high genetic barrier, and adaptation to the HIV protease plasticity

Scientific reports, 2020-06, Vol.10 (1), p.10664-10664, Article 10664

2020

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Structure-Based Design of Highly Selective β‑Secretase Inhibitors: Synthesis, Biological Evaluation, and Protein–Ligand X‑ray Crystal Structure

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9195-9207

2012

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Activity and structural analysis of GRL-117C: a novel small molecule CCR5 inhibitor active against R5-tropic HIV-1s

Scientific reports, 2019-03, Vol.9 (1), p.4828, Article 4828

2019

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GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants

Science advances, 2023-07, Vol.9 (28), p.eadg2955

2023

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Novel P2 Tris-tetrahydrofuran Group in Antiviral Compound 1 (GRL-0519) Fills the S2 Binding Pocket of Selected Mutants of HIV‑1 Protease

Journal of medicinal chemistry, 2013-02, Vol.56 (3), p.1074-1083

2013

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GRL-0519, a Novel Oxatricyclic Ligand-Containing Nonpeptidic HIV-1 Protease Inhibitor (PI), Potently Suppresses Replication of a Wide Spectrum of Multi-PI-Resistant HIV-1 Variants In Vitro

Antimicrobial Agents and Chemotherapy, 2013-05, Vol.57 (5), p.2036-2046

2013

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(2 S)-2-Anilinomethylpyrrolidine: an efficient in situ recyclable chiral catalytic source for the borane-mediated asymmetric reduction of prochiral ketones in refluxing toluene

Tetrahedron: asymmetry, 2006-04, Vol.17 (7), p.1041-1044

2006

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Chiral diamides as efficient catalytic precursors for the borane-mediated asymmetric reduction of prochiral ketones

Tetrahedron: asymmetry, 2007-05, Vol.18 (8), p.968-974

2007

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(5 S)-1,3-Diaza-2-imino-3-phenylbicyclo[3.3.0]octane: first example of guanidine based in situ recyclable chiral catalytic source for borane-mediated asymmetric reduction of prochiral ketones

Tetrahedron: asymmetry, 2006-04, Vol.17 (7), p.1036-1040

2006

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(5 S)-1-Aza-2-imino-3-oxa-4,4-diphenylbicyclo(3.3.0)octane: a novel chiral catalytic source containing the N–(C NH)–O moiety for the borane-mediated asymmetric reduction of prochiral ketones

Tetrahedron: asymmetry, 2007-05, Vol.18 (8), p.963-967

2007

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Toward effective chiral catalysts containing the NPO structural framework for the borane-mediated asymmetric reduction of prochiral ketones

Tetrahedron: asymmetry, 2004-06, Vol.15 (12), p.1881-1888

2004

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Design and Development of Highly Potent HIV‑1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants

Journal of medicinal chemistry, 2017-05, Vol.60 (10), p.4267-4278

2017

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Severe Acute Respiratory Syndrome Coronavirus Papain-like Novel Protease Inhibitors: Design, Synthesis, Protein−Ligand X-ray Structure and Biological Evaluation

Journal of medicinal chemistry, 2010-07, Vol.53 (13), p.4968-4979

2010

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Halogen Bond Interactions of Novel HIV-1 Protease Inhibitors (PI) (GRL-001-15 and GRL-003-15) with the Flap of Protease Are Critical for Their Potent Activity against Wild-Type HIV-1 and Multi-PI-Resistant Variants

Antimicrobial agents and chemotherapy, 2019-06, Vol.63 (6)

2019

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Design and Synthesis of Highly Potent HIV‑1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure–Activity Studies, Biological and X‑ray Structural Analysis

Journal of medicinal chemistry, 2018-05, Vol.61 (10), p.4561-4577

2018

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An enantioselective synthesis of a MEM-protected aetheramide A derivative

Tetrahedron letters, 2014-09, Vol.55 (37), p.5191-5194

2014

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Design of Highly Potent, Dual‐Acting and Central‐Nervous‐System‐Penetrating HIV‐1 Protease Inhibitors with Excellent Potency against Multidrug‐Resistant HIV‐1 Variants

ChemMedChem, 2018-04, Vol.13 (8), p.803-815

2018

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Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes

Chemical science (Cambridge), 2016-01, Vol.7 (5), p.3117-3122

2016

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Extreme Multidrug Resistant HIV‑1 Protease with 20 Mutations Is Resistant to Novel Protease Inhibitors with P1′-Pyrrolidinone or P2-Tris-tetrahydrofuran

Journal of medicinal chemistry, 2013-05, Vol.56 (10), p.4017-4027

2013

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Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potent β-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2012-09, Vol.22 (17), p.5460-5465

2012

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Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes† †Electronic supplementary information (ESI) available: Experimental procedure and characterization data of new compounds. See DOI: 10.1039/c5sc03718b

Chemical science (Cambridge), 2016-02, Vol.7 (5), p.3117-3122

2016

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Front Cover: Design of Highly Potent, Dual‐Acting and Central‐Nervous‐System‐Penetrating HIV‐1 Protease Inhibitors with Excellent Potency against Multidrug‐Resistant HIV‐1 Variants (ChemMedChem 8/2018)

ChemMedChem, 2018-04, Vol.13 (8), p.762-762

2018

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The Baylis-Hillman reaction: a novel source of attraction, opportunities, and challenges in synthetic chemistry

GRL-09510, a Unique P2-Crown-Tetrahydrofuranylurethane -Containing HIV-1 Protease Inhibitor, Maintains Its Favorable Antiviral Activity against Highly-Drug-Resistant HIV-1 Variants in vitro

Single atom changes in newly synthesized HIV protease inhibitors reveal structural basis for extreme affinity, high genetic barrier, and adaptation to the HIV protease plasticity

A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency

Structure-Based Design of Highly Selective β‑Secretase Inhibitors: Synthesis, Biological Evaluation, and Protein–Ligand X‑ray Crystal Structure

Activity and structural analysis of GRL-117C: a novel small molecule CCR5 inhibitor active against R5-tropic HIV-1s

GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants

Novel P2 Tris-tetrahydrofuran Group in Antiviral Compound 1 (GRL-0519) Fills the S2 Binding Pocket of Selected Mutants of HIV‑1 Protease

GRL-0519, a Novel Oxatricyclic Ligand-Containing Nonpeptidic HIV-1 Protease Inhibitor (PI), Potently Suppresses Replication of a Wide Spectrum of Multi-PI-Resistant HIV-1 Variants In Vitro

(2 S)-2-Anilinomethylpyrrolidine: an efficient in situ recyclable chiral catalytic source for the borane-mediated asymmetric reduction of prochiral ketones in refluxing toluene

Chiral diamides as efficient catalytic precursors for the borane-mediated asymmetric reduction of prochiral ketones

(5 S)-1,3-Diaza-2-imino-3-phenylbicyclo[3.3.0]octane: first example of guanidine based in situ recyclable chiral catalytic source for borane-mediated asymmetric reduction of prochiral ketones

(5 S)-1-Aza-2-imino-3-oxa-4,4-diphenylbicyclo(3.3.0)octane: a novel chiral catalytic source containing the N–(C NH)–O moiety for the borane-mediated asymmetric reduction of prochiral ketones

Toward effective chiral catalysts containing the NPO structural framework for the borane-mediated asymmetric reduction of prochiral ketones

Design and Development of Highly Potent HIV‑1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants

Severe Acute Respiratory Syndrome Coronavirus Papain-like Novel Protease Inhibitors: Design, Synthesis, Protein−Ligand X-ray Structure and Biological Evaluation

Halogen Bond Interactions of Novel HIV-1 Protease Inhibitors (PI) (GRL-001-15 and GRL-003-15) with the Flap of Protease Are Critical for Their Potent Activity against Wild-Type HIV-1 and Multi-PI-Resistant Variants

Design and Synthesis of Highly Potent HIV‑1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure–Activity Studies, Biological and X‑ray Structural Analysis

An enantioselective synthesis of a MEM-protected aetheramide A derivative

Design of Highly Potent, Dual‐Acting and Central‐Nervous‐System‐Penetrating HIV‐1 Protease Inhibitors with Excellent Potency against Multidrug‐Resistant HIV‐1 Variants

Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes

Extreme Multidrug Resistant HIV‑1 Protease with 20 Mutations Is Resistant to Novel Protease Inhibitors with P1′-Pyrrolidinone or P2-Tris-tetrahydrofuran

Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potent β-secretase inhibitors

Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes† †Electronic supplementary information (ESI) available: Experimental procedure and characterization data of new compounds. See DOI: 10.1039/c5sc03718b

Front Cover: Design of Highly Potent, Dual‐Acting and Central‐Nervous‐System‐Penetrating HIV‐1 Protease Inhibitors with Excellent Potency against Multidrug‐Resistant HIV‐1 Variants (ChemMedChem 8/2018)

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