The application of bioisosteres in drug design for novel drug discovery: focusing on acid protease inhibitors

Structure-guided design and synthesis of P1′ position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors

(2011) Harichandra D. Tagad et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design

(2011) Yoshio Hamada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cyclopentane-1,3-dione: A Novel Isostere for the Carboxylic Acid Functional Group. Application to the Design of Potent Thromboxane (A2) Receptor Antagonists

(2011) Carlo Ballatore et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design

(2011) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

BACE1 Inhibitor Peptides: Can an Infinitely Small kcat Value Turn the Substrate of an Enzyme into Its Inhibitor?

(2011) Yoshio Hamada et al.   ACS Medicinal Chemistry Letters

Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1′ and P4 positions

(2010) Harichandra D. Tagad et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Crystal Structures of Inhibitor Complexes of Human T-Cell Leukemia Virus (HTLV-1) Protease

(2010) Tadashi Satoh et al.   JOURNAL OF MOLECULAR BIOLOGY

Significance of interactions of BACE1–Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold

(2009) Yoshio Hamada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Recent progress in the drug discovery of non-peptidic BACE1 inhibitors

(2009) Yoshio Hamada et al.   Expert Opinion on Drug Discovery

Quantum Isostere Database: A Web-Based Tool Using Quantum Chemical Topology To Predict Bioisosteric Replacements for Drug Design

(2009) Mike Devereux et al.   Journal of Chemical Information and Modeling

Triazole Inhibitors ofCryptosporidium parvumInosine 5′-Monophosphate Dehydrogenase

(2009) Sushil K. Maurya et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of selective CXCR4 antagonists containing alkene dipeptide isosteres

(2009) Tetsuo Narumi et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Structure of HIV-1 protease in complex with potent inhibitor KNI-272 determined by high-resolution X-ray and neutron crystallography

(2009) M. Adachi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Design of Potent Aspartic Protease Inhibitors to Treat Various Diseases

(2008) Jeffrey-Tri Nguyen et al.   ARCHIV DER PHARMAZIE

Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties

(2008) Meihui Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme

(2008) Meihui Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

BACE1 inhibitors: Optimization by replacing the residue with non-acidic moiety

(2008) Yoshio Hamada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel non-peptidic and small-sized BACE1 inhibitors

(2008) Yoshio Hamada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Combination of Non-naturald-Amino Acid Derivatives and Allophenylnorstatine−Dimethylthioproline Scaffold in HIV Protease Inhibitors Have High Efficacy in Mutant HIV

(2008) Shingo Nakatani et al.   JOURNAL OF MEDICINAL CHEMISTRY

First Demonstration of Cerebrospinal Fluid and Plasma A  Lowering with Oral Administration of a  -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates

(2008) S. Sankaranarayanan et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Cl-π interactions in protein-ligand complexes

(2008) Yumi N. Imai et al.   PROTEIN SCIENCE

Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors

(2007) Jeffrey-Tri Nguyen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS