Identification of Micrococcin P2-Derivatives as Antibiotic Candidates against Two Gram-Positive Pathogens.

Thiopeptides exhibit potent antimicrobial activity against Gram-positive pathogens by inhibiting bacterial protein synthesis. Micrococcins are among the structurally simpler thiopeptides, but they have not been exploited in detail. This research involved a computational simulation of micrococcin P2 (MP2) docking in parallel with the structure-activity relationship (SAR) studied.

Micrococcin P2 Targets .

infection is a global public health threat. Extensive assays using clinical isolates have identified micrococcin P2 (MP2, ) as a particularly effective anti- agent. MP2 possesses a mode of action that differs from other antibiotics and pharmacokinetic properties that render it especially promising.

Nitro-Group-Containing Thiopeptide Derivatives as Promising Agents to Target .

The US Centers for Disease Control and Prevention (CDC) lists as an urgent bacterial threat. Yet, only two drugs, vancomycin and fidaxomicin, are approved by the FDA for the treatment of infections as of this writing, while the global pipeline of new drugs is sparse at best. Thus, there is a clear and urgent need for new antibiotics against that organism.

Verification of De-Identification Techniques for Personal Information Using Tree-Based Methods with Shapley Values.

With the development of big data and cloud computing technologies, the importance of pseudonym information has grown. However, the tools for verifying whether the de-identification methodology is correctly applied to ensure data confidentiality and usability are insufficient. This paper proposes a verification of de-identification techniques for personal healthcare information by considering data confidentiality and usability.

Synthesis and antimicrobial activity of imidazole and pyridine appended cholestane-based conjugates.

A series of 3α-amino-5α-cholestane and 3α,7α-diamino-5α-cholestane derivatives containing imidazole and pyridine rings were synthesized by simple and effective reductive amination, and their in vitro activities against a range of Gram-positive and Gram-negative strains were evaluated. Most of the compound exhibited enhanced activity against MRSA pathogen. 3α,7α-Di(pyridylmethyl)amino-5α-cholestane 10 showed the highest potency in these series toward the Gram-positive bacteria, Staphylococcus epidermidis 887E, with the lowest MIC value of 1 μg/mL.

Antibacterial activity of LCB01-0062, a novel oxazolidinone.

LCB01-0062, a novel oxazolidinone, has potent antibacterial activity against clinical isolates of Gram-positive bacteria. The in vitro activity of LCB01-0062 was compared with that of linezolid, oxacillin, erythromycin, ciprofloxacin, vancomycin and quinupristin/dalfopristin. Among the tested agents, LCB01-0062 showed the most potent antibacterial activity against meticillin-resistant Staphylococcus aureus, meticillin-resistant coagulase-negative staphylococci and vancomycin-resistant enterococci.

In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.

LCB01-0371 is a new oxazolidinone with cyclic amidrazone. In vitro activity of LCB01-0371 against 624 clinical isolates was evaluated and compared with those of linezolid, vancomycin, and other antibiotics. LCB01-0371 showed good activity against Gram-positive pathogens.