The invention provides a 3-sulfydryl-N-benzyl propanamide compound. The structural formula of the 3-sulfydryl-N-benzyl propanamide compound is as shown in the specification, wherein R is C1-C4 alkyl containing a straight chain structure, or C1-C4 alkyl containing a cyclic structure. The compound has a good effect in restraining the activity of NDM-1.

Use of 3-sulfydryl-N-benzyl propanamide compound in restraint of NDM-1

The invention provides a preparation method of a gamma-lactam bridging dipeptide compound The preparation method comprises the following steps: performing reaction on dibasic acid ester as shown in aformula I and tert-butyl oxycarbonyl ethylamine as shown in a formula II to obtain 2-[4-(alkoxy carbonyl)-2-oxypyrrole alkyl acetate as shown in a formula III; hydrolyzing the 2-[4-(alkoxy carbonyl)-2-oxypyrrole alkyl acetate under the existence of an alkaline substance to obtain 2-(4-carboxyl-2-oxo-pyrrolidine)acetic acid ester; performing reaction on the 2-(4-carboxyl-2-oxo-pyrrolidine)acetic acid ester and tertiary butanol under the existence of diphenyl azide phosphate to obtain Boc-protected pyrrolityl acetate as shown in a formula V; and performing hydrolysis to obtain 20{4-[(tert-butoxy)carboyl amino]-2-oxo-pyrrolidine}acetic acid as shown in a formula VI The preparation method provided by the invention does not use sulfide, and is favorable for environmental protection, simple insynthesis route and high in yield

Preparation method of gamma-lactam bridging dipeptide compound

The invention belongs to the field of biomedicine, particularly relates to mercaptopropionamide compounds shown in a formula (I) and medicinal salts thereof, and a preparation method and medicinal application thereof, and in particular relates to application in preparation of drugs against gram-negative drug-resistant bacteria. Some compounds are tested for NDM-1 enzyme activity, and are combinedwith meropenem to carry out in vitro antibacterial activity tests. Experimental results show that some compounds have better NDM-1 enzyme inhibitory activity and can obviously reduce the minimum inhibitory concentration (MIC value) of the meropenem. The compound and salts thereof can be used for preparing NDM-1 enzyme inhibitors, and can be combined with the meropenem to prepare a compound preparation for resisting the gram-negative drug-resistant bacteria.

Mercaptopropionamide compounds and preparation method and medicinal application thereof

The present invention relates to cysteine derivatives for use in the treatment or prevention of a bacterial infection by inhibiting bacterial quorum sensing. Bacterial infections of particular interest are bacterial infections caused by Gram-positive bacteria that employ thiolactone containing auto-inducing peptides (AIPs).

Cysteine derivatives for treatment and prevention of bacterial infections

The invention relates to application of mercapto-propanol compounds in preparation of medicaments for inhibiting the activity of drug-resistant bacteria. According to the application, the structural formulae of the mercapto-propanol compounds are shown in the specification, wherein R represents C1-C4 alkyl containing a linear chain structure and C1-C4 alkyl or sulfydryl containing a cyclic structure. The compounds have the well effect of inhibiting the activity of NDM-1.

Application of mercapto-propanol compounds in inhibition of NDM-1

The invention provides purpose of L-cysteine compound with a following general formula for restraining new delhi metallo (NDM)-1 activity in medicine. R is C1-C4 carbalkoxy or aromatic oxygen carbonyl or C1-C4 alkyl acyl. The compound has the function on restraining NDM-1 activity.

Purpose of L-cysteine compound for restraining new delhi metallo (NDM)-1 activity

The invention provides an application of 3-mercaptopropionic acid compounds preparing drugs for inhibiting activity of drug-resistant bacteria, wherein the structural formula of the 3-mercaptopropionic acid compounds is as follows, wherein R represents a C1-C3 alkane or a C1-C4 alkyl group with a cyclic structure. The compound provided by the invention has very good effect for inhibiting the activity of NDM-1. An IC50 value for inhibiting the activity of the NDM-1 of the compound 2-methyl-3-mercaptopropionic acid is 56.3 +/- 10.9 [mu]M.

Application of 3-mercaptopropionic acid compounds in inhibiting NDM-1

The invention provides application of 3-mercaptopropionic acid amide compounds with the following general formula (I) in medicine which restrains the activity of multidrug-resistant bacteria through restraining the activity of NDM-1, wherein R1 is selected from a formula and R2 is selected from a C1-C4 alkyl group.

Application of 3-mercaptopropionic acid amide compounds

The invention relates to uses of D-homocysteine-L-phenylalanine dipeptide derivatives in the preparation of new Delhi metallo-beta-lactamase 1 (NDM-1) inhibitors, and concretely relates to uses of compounds of general formula I in the preparation of medicines for preventing and/or treating infectious diseases and the preparation of NDM-1 inhibitors.

Uses of D-homocysteine-L-phenylalanine dipeptide derivatives in preparation of new Delhi metallo-beta-lactamase 1 inhibitors

The invention provides an application of (R)-2-methyl-3-mercaptopropionic acid in preparing drugs for inhibiting activity of drug-resistant bacteria, wherein the structural formula of the (R)-2-methyl-3-mercaptopropionic acid is as follows. The compound can effectively inhibit the activity of NDM-1.

Application of (R)-2-methyl-3-mercaptopropionic acid in inhibiting NDM-1

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