Chapter 27. Bioisosterism in Drug Design

Phosphonates as analogues of natural phosphates

1977 • 716 citations

Isosterism and molecular modification in drug design

1979 • 450 citations

Conformational restrictions of biologically active peptides via amino acid side chain groups

1982 • 395 citations

On the concept of linear modified retro-peptide structures

1979 • 255 citations

Pepstatin-derived inhibitors of aspartic proteinases. A close look at an apparent transition-state analog inhibitor

1985 • 218 citations

Quantum-chemistry and catalysis in oxidation of hydrocarbons

1981 • 194 citations

A practitioner's perspective of the role of quantitative structure-activity analysis in medicinal chemistry

1981 • 184 citations

Bicyclic and tricyclic ergoline partial structures. Rigid 3-(2-aminoethyl)pyrroles and 3- and 4-(2-aminoethyl)pyrazoles as dopamine agonists

1980 • 170 citations

Crystal environments and geometries of leucine, isoleucine, valine and phenylalanine provide estimates of minimum nonbonded contact and preferred van der Waals interaction distances

1985 • 162 citations

.gamma.-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects

1981 • 124 citations

Synthesis and hypotensive activity of N-alkyl-N''-cyano-N'-pyridylguanidines

1978 • 124 citations

2,8-Dimethyl-4-(carboxymethyl)-6-(aminomethyl)phenoxathiin S-dioxide: an organic substitute for the .beta.-turn in peptides?

1986 • 88 citations

Acylamido boronic acids and difluoroborane analogs of amino acids: potent inhibitors of chymotrypsin and elastase

1985 • 87 citations

Isopolar<u>vs</u>Isosteric Phosphonate Analogues of Nucleotides

1985 • 82 citations

An arylaminopyridazine derivative of gamma-aminobutyric acid (GABA) is a selective and competitive antagonist at the GABAA receptor site.

1985 • 78 citations

Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles

1985 • 70 citations

Synthesis and blood pressure lowering activity of 3-(substituted-amino)-1,2,4-benzothiadiazine 1-oxide derivatives

1980 • 62 citations

Synthesis of new dipeptide analogs containing novel ketovinyl and hydroxyethylidene isosteres via Grignard addition to chiral .alpha.-amino aldehydes

1985 • 54 citations

Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2 receptor antagonists

1982 • 54 citations

The physicochemical approach to drug design and discovery (QSAR)

1981 • 51 citations

Uridine 5'-diphosphate glucose analogs. Inhibitors of protein glycosylation that show antiviral activity

1985 • 50 citations

Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine

1985 • 48 citations

Receptor binding sites of hypoglycemic sulfonylureas and related [(acylamino)alkyl]benzoic acids

1984 • 48 citations

Interaction of histamine H2-receptor antagonists with GABA and benzodiazepine binding sites in the CNS

1983 • 47 citations

Synthesis of potent heptapeptide analogs of cholecystokinin

1984 • 47 citations

Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives

1981 • 46 citations

Synthesis and biological activity of carboxylic acid replacement analogs of the potent angiotensin converting enzyme inhibitor 5(S)-benzamido-4-oxo-6-phenylhexanoyl-L-proline

1985 • 45 citations

Dipole moment in relation to hydrogen receptor histamine antagonist activity for cimetidine analogs

1986 • 45 citations

An interdisciplinary approach to the design of new structures active at the .beta.-adrenergic receptor. Aliphatic oxime ether derivatives

1985 • 41 citations

Chapter 20. Platelet-Activating Factor: Multifaceted Biochemical and Physiological Mediator

1985 • 41 citations

Conformationally restricted cyclic nonapeptides derived from L-cysteine and LL-3-amino-2-piperidone-6-carboxylic acid (LL-Acp), a potent .beta.-turn-inducing dipeptide analog

1985 • 40 citations

Theoretical conformational studies of some dopamine antagonistic benzamide drugs: 3-pyrrolidyl- and 4-piperidyl derivatives

1983 • 38 citations

A general distance-geometry three-dimensional receptor model for diverse dihydrofolate reductase inhibitors

1984 • 37 citations

Conformationally defined adrenergic agents. 1. Design and synthesis of novel .alpha.2-selective adrenergic agents: electrostatic repulsion based conformational prototypes

1985 • 36 citations

[(3-Aryl-1,2-benzisoxazol-6-yl)oxy]acetic acids. A new diuretic series

1982 • 35 citations

Synthesis and .beta.-adrenergic blocking activity of new aliphatic oxime ethers

1980 • 33 citations

Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists

1983 • 31 citations

N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl)-N-methyl-2-hydroxyethanesulfonamide: a potent and selective .alpha.2-adrenoceptor antagonist

1985 • 30 citations

Structure-activity relationships for 2-substituted imidazoles as .alpha.2-adrenoceptor antagonists

1982 • 28 citations

Isosterism and molecular modification in drug design : Tetrazole analogue of GABA : Effects on enzymes of the γ-aminobutyrate system

1983 • 28 citations

Synthesis and diuretic profile of 3-(3-amino-1,2,4-oxadiazol-5-yl)-5-chloro-2,6-pyrazinediamine, an amiloride-type diuretic

1980 • 28 citations

Histamine H2 receptor antagonists. 1. Synthesis of N-cyano and N-carbamoyl amidine derivatives and their biological activities

1984 • 27 citations

The Arenology Principle

1971 • 26 citations

4-(Aminoalkyl)-7-hydroxy-2(3H)-indolones, a novel class of potent presynaptic dopamine receptor agonists

1983 • 25 citations

Inhibitors of glycolic acid oxidase. 4-Substituted-2,4-dioxobutanoic acid derivatives

1983 • 25 citations

Pyridazinones. 2. Synthesis and antisecretory and antiulcer activities of thiourea and 2-cyanoguanidine derivatives

1983 • 25 citations

Dipeptide glycols: A new class of renin inhibitors

1985 • 25 citations

Synthesis of aminomethyl-substituted cyclic imide derivatives for evaluation as anticonvulsants

1983 • 22 citations

Potential antiatherosclerotic agents. 3. Substituted benzoic and nonbenzoic acid analogs of cetaben

1983 • 21 citations

In search of new anticancer drugs. 13. Phosphonic and phosphinic analogs of ornithine

1985 • 20 citations

Mesoionic pyridazine ribonucleosides. A novel biologically active nucleoside metabolite

1984 • 20 citations

Potential inhibitors of nucleotide biosynthesis. 1. Nitrosoureidonucleosides. 2

1981 • 19 citations

Quaternary heterocyclylamino .beta.-lactams: a generic alternative to the classical acylamino side chain

1982 • 19 citations

Chapter 30. Recent Progress in the Rational Design of Peptide Hormones and Neurotransmitters

1984 • 19 citations

Synthesis and crystal structure of 17-deaza-17-methyl thionium isomorphinan (isosulforphanol) perchlorate, an isostere of the opiate isolevorphanol

1985 • 18 citations

Dopaminergic agonists: comparative actions of amine and sulfonium analogs of dopamine

1984 • 18 citations

Prostaglandins and congeners. 25. Inhibition of gastric acid secretion. Replacement of the carboxylate moiety of a prostaglandin with a hydroxymethylketo functional group

1980 • 17 citations

Dopamine receptor agonist activity of some 5-(2-aminoethyl)carbostyril derivatives

1985 • 17 citations

Phosphorus analogs of .gamma.-aminobutyric acid, a new class of anticonvulsants

1984 • 16 citations

Apparent bioisosteric replacement of -S- by NCN: synthesis of N-cyano-2-aza-A-nor-5.alpha.-androstan-17.beta.-ol acetate, an aza steroid androgen

1979 • 16 citations

Analogs of platelet activating factor. 3. Replacement of the phosphate moiety with a sulfonylbismethylene group

1985 • 16 citations

5-Sulfamoylorthanilic acids, a sulfonamide series with salidiuretic activity

1983 • 16 citations

The dipole moments of 1,3-dimethylthiourea, 1,3-dimethyl-2-cyanoguanidine and 1,1-bis-methylamino-2-nitroethene in a aqueous solution

1982 • 14 citations

Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3.alpha.,4a.alpha.,10a.beta.)-1,2,3,4,4a,5,10,10a-octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide

1985 • 14 citations

Synthesis of some phosphonates with antiherpetic activity

1984 • 13 citations

Bulky amine analogs of ketoprofen: potent antiinflammatory agents

1984 • 11 citations

Chapter 19. Peptides of the Hypothalamus

1981 • 10 citations

The preclinical antipsychotic evaluation of HRP 913, a novel benzisoxazole derivative

1983 • 9 citations

Antihypertensive (2-aminoethyl)thiourea derivatives. 2

1980 • 9 citations

Vitamin K dependent carboxylation: synthesis and biological properties of tetrazolyl analogs of pentapeptidic substrates

1984 • 8 citations

β,γ-Peroxy Analogs of Adenosine and Guanosine Triphosphate: Synthesis and Biological Activity

1982 • 8 citations

Isoterism and molecular modification in drug design: New n-dipropylacetate analogs as inhibitors of succinic semi aldehyde dehydrogenase

1983 • 8 citations

Vitamin K‐dependent carboxylase: Synthesis of an inhibitor of the glutamyl binding site

1983 • 7 citations

New Methods for the Synthesis of Base Sensitive Cyanopyrimidine and Cyanopyridine Nucleosides

1984 • 7 citations

The dielectric properties of seven polar amidine-containing compounds of biological interest

1985 • 6 citations

Sulfonyliminoimidazolidines. A new class of oral hypoglycemia agents. 2. Mode of action and x-ray structure of 1-[[p-[2-(crotonylamine)ethyl]phenyl]sulfonyl]-3-cyclohexyl-2-iminoimidazolidine

1983 • 4 citations

[Antifibrinolytic properties of 5(4'-aminobutyl)-2,4-diketothiazolidine hydrochloride].

1984 • 1 citations