Strategy and Tactics in Combinatorial Organic Synthesis. Applications to Drug Discovery

Design of Specific Inhibitors of Angiotensin-Converting Enzyme: New Class of Orally Active Antihypertensive Agents

1977 • 1,851 citations

Calcium antagonism and calcium entry blockade.

1986 • 1,201 citations

Applications of Combinatorial Technologies to Drug Discovery. 1. Background and Peptide Combinatorial Libraries

1994 • 1,130 citations

Applications of Combinatorial Technologies to Drug Discovery. 2. Combinatorial Organic Synthesis, Library Screening Strategies, and Future Directions

1994 • 1,126 citations

General method for rapid synthesis of multicomponent peptide mixtures

1991 • 1,122 citations

Cycloaddition Reactions in Organic Synthesis

1990 • 1,062 citations

A general and expedient method for the solid-phase synthesis of 1,4-benzodiazepine derivatives

1992 • 441 citations

Chemistry and biological activity of thiazolidinones

1981 • 390 citations

Discovery of Nanomolar Ligands for 7-Transmembrane G-Protein-Coupled Receptors from a Diverse N-(Substituted)glycine Peptoid Library

1994 • 356 citations

"Diversomers": an approach to nonpeptide, nonoligomeric chemical diversity.

1993 • 337 citations

Synthesis of 1,4-Dihydropyridines by Cyclocondensation Reactions

1988 • 278 citations

The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library.

1994 • 265 citations

Tetrahedron report number 103

1981 • 239 citations

Medicinal Chemistry in the Golden Age of Biology: Lessons from Steroid and Peptide Research

1991 • 224 citations

Peptidomimetics derived from natural products

1993 • 214 citations

Recent Advances in Azomethine Ylide Chemistry

1989 • 214 citations

High-Resolution 1H NMR in Solid-Phase Organic Synthesis

1994 • 213 citations

Carbon-Carbon Bond-Forming Methods on Solid Support. Utilization of Kenner's "Safety-Catch" Linker

1994 • 207 citations

The asymmetric synthesis of β-lactam antibiotics - I. application of chiral oxazolidones in the staudinger reaction.

1985 • 204 citations

Angiotensin‐converting enzyme inhibitors: Medicinal chemistry and biological actions

1982 • 193 citations

Straightforward and general method for coupling alcohols to solid supports

1994 • 191 citations

Differential binding energy: a detailed evaluation of the influence of hydrogen-bonding and hydrophobic groups on the inhibition of thermolysin by phosphorus-containing inhibitors

1991 • 181 citations

Calcium- and calmodulin-antagonism of elnadipine derivatives: comparative SAR

1992 • 177 citations

Solid-Phase Synthesis of Structurally Diverse 1,4-Benzodiazepine Derivatives Using the Stille Coupling Reaction

1995 • 162 citations

Combinatorial Organic Synthesis of Highly Functionalized Pyrrolidines: Identification of a Potent Angiotensin Converting Enzyme Inhibitor from a Mercaptoacyl Proline Library

1995 • 161 citations

Solid-Supported Combinatorial Synthesis of Structurally Diverse β-Lactams

1996 • 158 citations

Trimethylorthoformate: A mild and effective dehydrating reagent for solution and solid phase imine formation

1995 • 153 citations

Solid phase synthesis of peptides containing the CH2NH peptide bond isostere

1987 • 149 citations

Methods for Combinatorial Organic Synthesis: The Use of Fast 13C NMR Analysis for Gel Phase Reaction Monitoring

1994 • 137 citations

Simultaneous Solid-Phase Synthesis of .beta.-Turn Mimetics Incorporating Side-Chain Functionality

1994 • 133 citations

Expedient Method for the Solid-Phase Synthesis of Aspartic Acid Protease Inhibitors Directed toward the Generation of Libraries

1995 • 131 citations

Strategies for Combinatorial Organic Synthesis: Solution and Polymer-Supported Synthesis of 4-Thiazolidinones and 4-Metathiazanones Derived from Amino Acids

1995 • 127 citations

Possible role for water dissociation in the slow binding of phosphorus-containing transition-state-analog inhibitors of thermolysin

1987 • 114 citations

(Phosphinyloxy)acyl amino acid inhibitors of angiotensin converting enzyme (ACE). 1. Discovery of (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L-proline, a novel orally active inhibitor of ACE

1988 • 105 citations

Solid-phase synthesis and biological properties of .psi.[CH2NH] pseudopeptide analogs of a highly potent somatostatin octapeptide

1987 • 84 citations

1,3-Dipolar cycloaddition reactions of imines of α-amino-acid esters: X-ray crystal and molecular structure of methyl 4-(2-furyl)-2,7-diphenyl-6,8-dioxo-3,7-diazabicyclo[3.3.0]octane-2-carboxylate

1978 • 79 citations

A Transition State Analog Inhibitor Combinatorial Library

1995 • 67 citations

Phosphonate Ester Synthesis Using a Modified Mitsunobu Condensation

1994 • 64 citations

Recent advances in the generation of chemical diversity libraries

1994 • 60 citations

The synthesis of phosphonate esters; an extension of the Mitsunobu reaction

1992 • 59 citations

Carbon-13 NMR relaxation times of a tripeptide methyl ester and its polymer-bound analogs

1990 • 57 citations

Excursions in drug discovery

1993 • 55 citations

Solid-Phase Synthesis of Peptidylphosphonates

1994 • 47 citations

Libraries of non-polymeric organic molecules

1995 • 32 citations

Nuclear magnetic resonance spectral analysis of polymer-supported reagents and catalysts

1984 • 21 citations