R₁ is selected from the group consisting of M₁-AA₁, M₁-AA₂-AA₁, and M₁-AA₃-AA₂-AA₁;

W is selected from the group consisting of halogen, cyano, and hydrogen;

M₁ is selected from the group consisting of H, NH₂—CO—, NH₂—CS—, NH₂—SO₂—, X—NH—CO—, X₂N—CO—, X—NH—CS—, X₂N—CS—, X—NH—SO₂—, X₂N—SO₂—, X—CO—, X—CS—, X—, Y—SO₂—, Y—O—CO—, Y—O—CS—, morpholine-CO—, and biotinyl;

X is selected from the group consisting of H, C_1-10 alkyl, C_3-15 cyclized alkyl, C_1-10 fluoroalkyl, C_1-10 alkyl substituted with J, C_1-10 fluoroalkyl substituted with J, 1-admantyl, 9-fluorenyl, phenyl, pentafluorophenyl, phenyl monosubstituted with K, phenyl disubstituted with K, phenyl trisubstituted with K, naphthyl, naphthyl monosubstituted with K, naphthyl disubstituted with K, naphthyl trisubstituted with K, C_1-10 fluoroalkyl with an attached phenyl group, C_1-10 alkyl with an attached phenyl group, C_1-10 alkyl with two attached phenyl groups, C_1-10 alkyl with an attached phenyl group substituted with K, C_1-10 alkyl with two attached phenyl groups substituted with K, C_1-10 alkyl with an attached naphthyl group, C_1-10 alkyl with an attached naphthyl group substituted with K, C_1-10 alkyl with an attached phenoxy group, and C_1-10 alkyl with an attached phenoxy group substituted with K on the phenoxy group;

Y is selected from the group consisting of C_1-10 alkyl, C_3-15 cyclized alkyl, C_1-10 fluoroalkyl, C_1-10 alkyl substituted with J, C_1-10 fluoroalkyl substituted with J, 1-admantyl, 9-fluorenyl, phenyl, phenyl monosubstituted with K, phenyl disubstituted with K, phenyl trisubstituted with K, naphthyl, naphthyl monosubstituted with K, naphthyl disubstituted with K, naphthyl trisubstituted with K, C_1-10 fluoroalkyl with an attached phenyl group, C_1-10 alkyl with an attached phenyl group, C_1-10 alkyl with two attached phenyl groups, C_1-10 alkyl with an attached phenyl group substituted with K, C_1-10 alkyl with two attached phenyl groups substituted with K, C_1-10 alkyl with an attached naphthyl group, C_1-10 alkyl with an attached naphthyl group substituted with K, C_1-10 alkyl with an attached phenoxy group, and C_1-10 alkyl with an attached phenoxy group substituted with K on the phenoxy group;

J is selected from the group consisting of halogen, CO₂H, OH, CN, NO₂, amino, C_1-10 alkoxy, C_1-10 alkylamino, C_2-12 dialkylamino, C_1-10 alkyl-O—CO—, C_1-10 alkyl-O—CO—NH—, and C_1-10 alkyl-S—;

K is selected from the group consisting of halogen, C_1-10 alkyl, C_1-10 perfluoroalkyl, C_1-10 alkoxy, phenoxy, NO₂, CN, OH, CO₂H, CONH₂, amino, C_1-10 alkylamino, C_2-12 dialkylamino, C_1-10 acyl, and C_1-10 alkoxy-CO—, and C_1-10 alkyl-S—;

AA₁, AA₂, and AA₃ are side chain blocked or unblocked amino acids with the L configuration, D configuration, or no chirality at the alpha-carbon selected from the group consisting of alanine, valine, leucine, isoleucine, proline, methionine, methionine sulfoxide, phenylalanine, tryptophan, glycine, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine, phenylglycine, beta-alanine, norleucine, norvaline, alpha-aminobutanoic acid, epsilon-aminocaproic acid, citrulline, hydroxyproline, ornithine, homoarginine, sarcosine, indoline 2-carboxylic acid, 2-azetidinecarboxylic acid, pipecolinic acid (2-piperidine carboxylic acid), O-methylserine, O-ethylserine, S-methylcysteine, S-ethylcysteine, S-benzylcysteine, NH₂—CH(CH₂CHEt₂)—CO₂H, alpha-aminoheptanoic acid, NH₂—CH(CH₂-1-naphthyl)-CO₂H, NH₂—CH(CH₂-2-naphthyl)-CO₂H, NH₂—CH(CH₂CH₂CH₂-phenyl)-CO₂H, NH₂—CH(CH₂-cyclohexyl)-CO₂H, NH₂—CH(CH₂-cyclopentyl)-CO₂H, NH₂—CH(CH₂-cyclobutyl)—CO₂H, NH₂—CH(CH₂-cyclopropyl)-CO₂H, trifluoroleucine, 4-fluorophenylalanine, lysine substituted on the epsilon nitrogen with a biotinyl group, hexafluoroleucine,

R₂ is selected from the group consisting of C_1-10 alkyl, C_1-10 perfluoroalkyl, C_1-10 alkyl substituted with Q, C_1-10 alkyl substituted with phenyl, C_1-10 alkyl with an attached phenyl substituted with K, C_1-10 alkyl substituted with naphthyl, C_1-10 alkyl with an attached naphthyl substituted with K, phenyl, phenyl substituted with K, naphthyl, naphthyl substituted with K, C_1-10 alkyl substituted with CONH₂, C_1-10 alkyl substituted with CONHR₅, C_1-10 alkyl substituted with CO₂H, C_1-10 alkyl substituted with SO₂NH₂, C_1-10 alkyl substituted with SO₃H, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-furyl substituted with K, 3-furyl substituted with K, 2-thienyl substituted with K, 3-thienyl substituted with K, 2-furyl substituted with G, 3-furyl substituted with G, 2-thienyl substituted with G, 3-thienyl substituted with G, C_1-10 alkyl substituted with CO₂R₅, CH₂CH₂SCH₃, CH₂-3-indolyl, C_1-2 alkyl with an attached 2-furyl, C_1-2 alkyl with an attached 3-furyl, C_1-2 alkyl with an attached 2-thienyl, C_1-2 alkyl with an attached 3-thienyl, C_1-2 alkyl with an attached 2-furyl substituted with K, C_1-2 alkyl with an attached 3-furyl substituted with K, C_1-2 alkyl with an attached 2-thienyl substituted with K, C_1-2 alkyl with an attached 3-thienyl substituted with K, C_1-2 alkyl with an attached 2-furyl substituted with G, C_1-2 alkyl with an attached 3-furyl substituted with G, C_1-2 alkyl with an attached 2-thienyl substituted with G, C_1-2 alkyl with an attached 3-thienyl substituted with G, CH₂-2-imidazyl, C_1-10 alkyl substituted with G, C_1-10 alkyl with an attached phenyl substituted with G, C_1-10 alkyl with an attached naphthyl substituted with G, phenyl substituted with G, and naphthyl substituted with G;

R₅ is selected from the group consisting of C_1-10 alkyl and C_1-10 alkyl substituted with phenyl;

Q is selected independently from the group consisting of C_1-10 alkoxy, C_1-10 alkyl-S—, C_1-10 alkoxy substituted with phenyl, and C_1-10 alkyl-S-substituted with phenyl;

G is selected from the group consisting of cyano, amidino (—C(═NH)NH₂), guanidino (—NHC(═NH)NH₂), isothiureido (—S—C(═NH)NH₂), amino, C_1-6 alkylamino, C_2-12 dialkylamino, and imidazyl;

R₃ is selected independently from the group consisting of H, R₆, halogen, CN, CO—C₆H₅, benzoyl substituted with K on the phenyl, CO₂H, CO₂R₇, CONHR₈, CONR₈R₉, CO-AA₄-T,

R₄ is selected from the group consisting of R₆, halogen, CN, CO—C₆H₅, benzoyl substituted with K on the phenyl, CO₂H, CO₂R₇, CONHR₈, CONR₈R₉, CO-AA₄-T,

R₆ is selected independently from the group consisting of phenyl, phenyl monosubstituted with K, phenyl disubstituted with K, phenyl trisubstituted with K, naphthyl, naphthyl monosubstituted with K, naphthyl disubstituted with K, naphthyl trisubstituted with K, C_1-10 alkenyl, C_3-15 cyclized alkyl, C_1-10 alkyl with a phenyl group attached to the C_1-10 alkyl, C_3-15 cyclized alkyl with an attached phenyl group, C_1-10 alkyl with an attached phenyl group monosubstituted with K, C_1-10 alkyl with an attached phenyl group disubstituted with K, C_1-10 alkyl with an attached phenyl group trisubstituted with K, C_3-15 cyclized alkyl with an attached phenyl group substituted with K, C_1-10 alkyl with a naphthyl group attached to the C_1-10 alkyl, C_3-15 cyclized alkyl with an attached naphthyl group, C_1-10 alkyl with an attached naphthyl group monosubstituted with K, C_1-10 alkyl with an attached naphthyl group disubstituted with K, C_1-10 alkyl with an attached naphthyl group trisubstituted with K, C_3-15 cyclized alkyl with an attached naphthyl group substituted with K, C_1-10 alkyl with an attached 2-furyl group, C_1-10 alkyl with an attached 3-furyl group, C_1-10 alkyl with an attached 2-pyridyl group, C_1-10 alkyl with an attached 3-pyridyl group, C_1-10 alkyl with an attached 4-pyridyl group, 2-furyl, 3-furyl, 2-pyridyl, 3-pyridyl, and 4-pyridyl;

R₇ is selected independently from the group consisting of phenyl, phenyl monosubstituted with K, phenyl disubstituted with K, phenyl trisubstituted with K, naphthyl, naphthyl monosubstituted with K, naphthyl disubstituted with K, naphthyl trisubstituted with K, C_1-10 alkyl, C_1-10 alkenyl, C_3-15 cyclized alkyl, C_1-10 alkyl with a phenyl group attached to the C_1-10 alkyl, C_3-15 cyclized alkyl with an attached phenyl group, C_1-10 alkyl with an attached phenyl group substituted with K, C_1-10 alkyl with an attached phenyl group disubstituted with K, C_1-10 alkyl with an attached phenyl group trisubstituted with K, C_3-15 cyclized alkyl with an attached phenyl group monosubstituted with K, C_3-15 cyclized alkyl with an attached phenyl group disubstituted with K, C_3-15 cyclized alkyl with an attached phenyl group trisubstituted with K, C_1-10 alkyl with a naphthyl group attached to the C_1-10 alkyl, C_3-15 cyclized alkyl with an attached naphthyl group, C_1-10 alkyl with an attached naphthyl group monosubstituted with K, C_1-10 alkyl with an attached naphthyl group disubstituted with K, C_1-10 alkyl with an attached naphthyl group trisubstituted with K, C_3-15 cyclized alkyl with an attached naphthyl group monosubstituted with K, C_3-15 cyclized alkyl with an attached naphthyl group disubstituted with K, C_3-15 cyclized alkyl with an attached naphthyl group trisubstituted with K, C_1-10 alkyl with an attached 2-furyl group, C_1-10 alkyl with an attached 3-furyl group, C_1-10 alkyl with an attached 2-pyridyl group, C_1-10 alkyl with an attached 3-pyridyl group, and C_1-10 alkyl with an attached 4-pyridyl group;

T is selected independently from the group consisting of OH, OR₁₀, NHR₁₁, and NR₁₀R₁₁;

AA₄ is a side chain blocked or unblocked amino acid with the L configuration, D configuration, or no chirality at the alpha-carbon selected from the group consisting of alanine, valine, leucine, isoleucine, proline, methionine, methionine sulfoxide, phenylalanine, tryptophan, glycine, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine, phenylglycine, beta-alanine, norleucine, norvaline, alpha-aminobutanoic acid, epsilon-aminocaproic acid, citrulline, hydroxyproline, ornithine, homoarginine, sarcosine, indoline 2-carboxylic acid, 2-azetidinecarboxylic acid, pipecolinic acid (2-piperidine carboxylic acid), O-methylserine, O-ethylserine, S-methylcysteine, S-ethylcysteine, S-benzylcysteine, NH₂—CH(CH₂CHEt₂)-CO₂H, alpha-aminoheptanoic acid, NH₂—CH(CH₂-1-naphthyl)-CO₂H, NH₂—CH(CH₂-2-naphthyl)-CO₂H, NH₂—CH(CH₂CH₂CH₂-phenyl)-CO₂H, NH₂—CH(CH₂-cyclohexyl)-CO₂H, NH₂—CH(CH₂-cyclopentyl)-CO₂H, NH₂—CH(CH₂-cyclobutyl)-CO₂H, NH₂—CH(CH₂-cyclopropyl)-CO₂H, trifluoroleucine, 4-fluorophenylalanine, lysine substituted on the epsilon nitrogen with a biotinyl group, hexafluoroleucine, and

R₈ and R₉ are selected independently from the group consisting of H, C_1-10 alkyl, C_1-10 alkenyl, C_3-20 cyclized alkyl, C_1-10 alkyl with a phenyl group attached to the C_1-10 alkyl, C_1-10 alkyl with two phenyl groups attached to the C_1-10 alkyl, C_3-20 cyclized alkyl with an attached phenyl group, phenyl, phenyl substituted with K, C_1-10 alkyl with an attached phenyl group substituted with K, C_1-10 alkyl with an attached phenyl group disubstituted with K, C_1-10 alkyl with an attached phenyl group trisubstituted with K, C_1-10 alkyl with two phenyl groups attached to the C_1-10 alkyl and substituted with K on the phenyl group, C_1-10 alkyl with two phenyl groups attached to the C_1-10 alkyl and disubstituted with K on the phenyl groups, C_3-20 cyclized alkyl with an attached phenyl group substituted with K, C_1-10 alkyl with a morpholine [—N(CH₂CH₂)O] ring attached through nitrogen to the alkyl, C_1-10 alkyl with a piperidine ring attached through nitrogen to the alkyl, C_1-10 alkyl with a pyrrolidine ring attached through nitrogen to the alkyl, C_1-20 alkyl with an OH group attached to the alkyl, —CH₂CH₂CH₂OCH₃, C_1-10 alkyl substituted by 1-naphthyl, C_1-10 alkyl substituted by 2-naphthyl, C_1-10 alkyl with an attached cyclohexyl group, —NH—CH₂CH₂-(4-hydroxyphenyl), —NH—CH₂CH₂-(3-indolyl), C_1-10 alkyl with an attached 2-furyl group, C_1-10 alkyl with an attached 3-furyl group, C_1-10 alkyl with an attached 2-pyridyl group, C_1-10 alkyl with an attached 3-pyridyl group, C_1-10 alkyl with an attached 4-pyridyl group, and C_1-5 alkyl with an attached phenyl and a hydroxyl attached to the C_1-5 alkyl;

R₁₀ and R₁₁ are selected independently from the group consisting of H, C_1-10 alkyl, phenyl, nitrophenyl, and C_1-10 alkyl substituted with phenyl;