Conformational restriction: an effective tactic in 'follow-on'-based drug discovery

Conformational restriction approach to BACE1 inhibitors II: SAR study of the isocytosine derivatives fixed with a cis-cyclopropane ring

(2013) Shuji Yonezawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Recent Advances in the Discovery and Development of Novel HIV-1 NNRTI Platforms (Part II): 2009-2013 Update#

(2013) Yu’ning Song et al.   CURRENT MEDICINAL CHEMISTRY

Carbamoyl Pyridone HIV-1 Integrase Inhibitors. 2. Bi- and Tricyclic Derivatives Result in Superior Antiviral and Pharmacokinetic Profiles

(2013) Takashi Kawasuji et al.   JOURNAL OF MEDICINAL CHEMISTRY

A conformationally fixed analog of the peptide mimic Grb2–SH2 domain: synthesis and evaluation against the A431 cancer cell

(2013) Takayuki Iwata et al.   Molecular BioSystems

Discovery of an HIV integrase inhibitor with an excellent resistance profile

(2013) David C. Pryde et al.   MedChemComm

A Conformationally Frozen Peptoid Boosts CXCR4 Affinity and Anti-HIV Activity

(2012) Oliver Demmer et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection

(2012) Jason J Schafer et al.   ANTIVIRAL THERAPY

Antagonists of 5-HT6 receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines—Synthesis and ‘structure–activity’ relationship

(2012) Alexandre V. Ivachtchenko et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Finger-loop inhibitors of the HCV NS5b polymerase. Part 1: Discovery and optimization of novel 1,6- and 2,6-macrocyclic indole series

(2012) David McGowan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2–P4 linkers

(2012) Michael T. Rudd et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

6,7-Dihydroxy-1-oxoisoindoline-4-sulfonamide-containing HIV-1 integrase inhibitors

(2012) Xue Zhi Zhao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055

(2012) Sandrine Vendeville et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis, Anti-HIV Activity Studies, and in silico Rationalization of Cyclobutane-Fused Nucleosides

(2012) Antoni Figueras et al.   ChemMedChem

Conformationally Constrained Peptides as Protein Tyrosine Kinase Inhibitors

(2012) Rakesh K. Tiwari et al.   CURRENT PHARMACEUTICAL DESIGN

Recent Progress in Small Molecule CCR5 Antagonists as Potential HIV-1 Entry Inhibitors

(2012) Wenwen Chen et al.   CURRENT PHARMACEUTICAL DESIGN

Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors

(2012) Shuang-Xi Gu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of a Novel Series of Bicyclic Heterocycles As Potent γ-Secretase Modulators

(2012) Francois Bischoff et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rational Design of Conformationally Constrained Cyclopentapeptide Antagonists for C-X-C Chemokine Receptor 4 (CXCR4)

(2012) Jignesh Mungalpara et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme-1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation

(2012) Mihirbaran Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Pharmacological Evaluation of Piperidin-4-yl amino aryl sulfonamides: Novel, Potent, Selective, Orally Active, and Brain Penetrant 5-HT6 Receptor Antagonists

(2012) Ramakrishna Nirogi et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-(Alkyl/Aryl)Amino-6-Benzylpyrimidin-4(3H)-ones as Inhibitors of Wild-Type and Mutant HIV-1: Enantioselectivity Studies

(2012) Dante Rotili et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conformational Restriction Approach to β-Secretase (BACE1) Inhibitors: Effect of a Cyclopropane Ring To Induce an Alternative Binding Mode

(2012) Shuji Yonezawa et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Rigid Bicyclic Platform for the Generation of Conformationally Locked Neuraminidase Inhibitors

(2012) Michael G. Brant et al.   ORGANIC LETTERS

Novel Cyclopropyl-Indole Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors

(2012) Mohammad Hassam et al.   ACS Medicinal Chemistry Letters

A 40-Year Journey in Search of Selective Antiviral Chemotherapy*

(2011) Erik De Clercq   Annual Review of Pharmacology and Toxicology

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

(2011) Kenneth M. Boy et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a novel series of cyclic urea as potent CCR5 antagonists

(2011) Maosheng Duan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of pyrrolidine-based β-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency

(2011) Shawn J. Stachel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2005 – 2010)

(2011) Peng Zhan et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Synthesis, Biological Evaluation, and Automated Docking of Constrained Analogues of the Opioid Peptide H-Dmt-d-Ala-Phe-Gly-NH2Using the 4- or 5-Methyl Substituted 4-Amino-1,2,4,5-tetrahydro-2-benzazepin-3-one Scaffold

(2011) Rien De Wachter et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of NovelN-Hydroxy-Dihydronaphthyridinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors

(2011) Ted W. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Qualitative Structure–Activity Evaluations of Novel β-Secretase Inhibitors as Potential Alzheimer’s Drug Leads

(2011) Taleb H. Al-Tel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and X-ray Crystallographic Analysis of a Novel Class of HIV-1 Protease Inhibitors

(2011) Ashit K. Ganguly et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Conformationally Constrained Inhibitors of Non-Nucleoside Reverse Transcriptase

(2011) Robert Gomez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prospective CCR5 Small Molecule Antagonist Compound Design Using a Combined Mutagenesis/Modeling Approach

(2011) Markus Metz et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

HIV-1 NNRTIs: structural diversity, pharmacophore similarity, and impliations for drug design

(2011) Peng Zhan et al.   MEDICINAL RESEARCH REVIEWS

Phase 2a Randomized Controlled Trial of Short-Term Activity, Safety, and Pharmacokinetics of a Novel Nonnucleoside Reverse Transcriptase Inhibitor, RDEA806, in HIV-1-Positive, Antiretroviral-Naive Subjects

(2010) G. Moyle et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis, activity, and pharmacokinetic properties of a series of conformationally-restricted thiourea analogs as novel hepatitis C virus inhibitors

(2010) Iou-Jiun Kang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, SAR and evaluation of [1,4′]-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists

(2010) David M. Rotstein et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Double-Blind, Controlled Phase II Study of a 5-HT6 Receptor Antagonist, SB-742457, in Alzheimers Disease

(2010) G. Maher-Edwards et al.   Current Alzheimer Research

Novel conformationally restricted triazole derivatives with potent antifungal activity

(2010) Wenya Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of Aryl-phospho-indole as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

(2010) François-René Alexandre et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting CXCR4 in HIV Cell-Entry Inhibition.

(2010) A. Steen et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Synthesis of conformationally restricted sulfonamides via radical cyclisation

(2010) D. Biswas et al.   TETRAHEDRON LETTERS

Update on the use of memantine in Alzheimer’s disease

(2010) Rob Marum   Neuropsychiatric Disease and Treatment

1-Amido-1-phenyl-3-piperidinylbutanes – CCR5 antagonists for the treatment of HIV: Part 2

(2009) Christopher G. Barber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH)

(2009) Arthur E. Kümmerle et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants

(2009) Dai-Shi Su et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors

(2009) Iou-Jiun Kang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and anti-HCV activity of thiourea compounds

(2009) Iou-Jiun Kang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Recent Advances in the Discovery and Development of Novel HIV-1 NNRTI Platforms: 2006-2008 Update

(2009) Peng Zhan et al.   CURRENT MEDICINAL CHEMISTRY

Design Strategies of Novel NNRTIs to Overcome Drug Resistance

(2009) Peng Zhan et al.   CURRENT MEDICINAL CHEMISTRY

Medicinal chemistry strategies in follow-on drug discovery

(2009) Hongyu Zhao et al.   DRUG DISCOVERY TODAY

Discovery of Chiral Cyclopropyl Dihydro-Alkylthio-Benzyl-Oxopyrimidine (S-DABO) Derivatives as Potent HIV-1 Reverse Transcriptase Inhibitors with High Activity Against Clinically Relevant Mutants

(2009) Marco Radi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Subnanomolar Inhibitor of Cytochromebc1Complex Designed by Optimizing Interaction with Conformationally Flexible Residues

(2009) Pei-Liang Zhao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Donepezil treatment of patients with MCI: A 48-week randomized, placebo-controlled trial

(2009) R. S. Doody et al.   NEUROLOGY

Synthesis and anti-HIV activity of conformationally restricted bicyclic hexahydroisobenzofuran nucleoside analogs

(2009) Alba Díaz-Rodríguez et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

The Practice of Ring Constraint in Peptidomimetics Using Bicyclic and Polycyclic Amino Acids

(2008) Stephen Hanessian et al.   ACCOUNTS OF CHEMICAL RESEARCH

Recent Approaches in the Synthesis of Conformationally Restricted Nucleoside Analogues

(2008) Christophe Mathé et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY