The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Caged luciferin-based probes become a luciferase substrate emitting bioluminescence upon ?-lactamase/esterase activation. The inclusion of a cephalosporin moiety renders the probe capable of being used for the detection of a wide-range of ?-lactamases and ?-lactamase-expressing bacteria. Embodiments of a rapid high-throughput assay for the identification of ?-lactamase-expressing bacteria is made possible by the use of such probes. In some embodiments the cephalosporin is substituted by a carbapenem moiety to generate carbapenem-caged luciferin carbapenem-cleavable probes capable of being used for the detection of a wide-range of carbapenem-expressing bacteria. Accordingly embodiments of a rapid high-throughput assay for the identification of carbapenem-expressing bacteria is made possible by the use of these probes.

Caged luciferin-based probes become a luciferase substrate emitting bioluminescence upon ?-lactamase/esterase activation. The inclusion of a cephalosporin moiety renders the probe capable of being used for the detection of a wide-range of ?-lactamases and ?-lactamase-expressing bacteria. Embodiments of a rapid high-throughput assay for the identification of ?-lactamase-expressing bacteria is made possible by the use of such probes. In some embodiments the cephalosporin is substituted by a carbapenem moiety to generate carbapenem-caged luciferin carbapenem-cleavable probes capable of being used for the detection of a wide-range of carbapenem-expressing bacteria. Accordingly embodiments of a rapid high-throughput assay for the identification of carbapenem-expressing bacteria is made possible by the use of these probes.

This application describes a compound represented by Formula (I):

Y?Z?X.sup.1S(O)(X.sup.2)F).sub.m].sub.n(I)

wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

This application describes modified amino acids and polypeptides comprising a SO.sub.2F or CH.sub.2CH.sub.2SO.sub.2F group bound to the side chain of an amino acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptor sites of receptor proteins are also described herein.

This application describes modified amino acids and polypeptides comprising a SO.sub.2F or CH.sub.2CH.sub.2SO.sub.2F group bound to the side chain of an amino acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptor sites of receptor proteins are also described herein.