Fluorinated azoles as effective weapons in fight against methicillin-resistance staphylococcus aureus (MRSA) and its SAR studies.

The rapid spread of Methicillin-resistant Staphylococcus aureus (MRSA) and its difficult-to-treat skin and filmsy diseases are making MRSA a threat to human life. The most dangerous feature is the fast emergence of MRSA resistance to all recognized antibiotics, including vancomycin. The creation of novel, effective, and non-toxic drug candidates to combat MRSA isolates is urgently required. Fluorine containing small molecules have taken a centre stage in the field of drug development. Over the last 50 years, there have been a growing number of fluorinated compounds that have been approved since the clinical usage of fluorinated corticosteroids in the 1950 s and fluoroquinolones in the 1980 s. Due to its advantages in terms of potency and ADME (absorption, distribution, metabolism, and excretion), fluoro-pharmaceuticals have been regarded as a potent and useful tool in the rational drug design method. The flexible bioactive fluorinated azoles are ideal candidates for the development of new antibiotics. This review summarizes the decade developments of fluorinated azole derivatives with a wide antibacterial activity against diverged MRSA strains. In specific, we correlated the efficacy of structurally varied fluorinated azole analogues including thiazole, benzimidazole, oxadiazole and pyrazole against MRSA and discussed different angles of structure-activity relationship (SAR).

Recent developments of P-glycoprotein inhibitors and its structure-activity relationship (SAR) studies.

P-glycoprotein (P-gp) over-expression is a key factor in multi-drug resistance (MDR), which is a major factor in the failure of cancer treatment. P-gp inhibitors have been demonstrated to have powerful pharmacological properties and may be used as a therapeutic approach to overcome the MDR in cancer cells. Combining clinical investigations with biochemical and computational research may potentially lead to a clearer understanding of the pharmacological properties and the mechanisms of action of these P-gp inhibitors. The task of turning these discoveries into effective therapeutic candidates for a variety of malignancies, including resistant and metastatic kinds, falls on medicinal chemists. A variety of P-gp inhibitors with great potency, high selectivity, and minimal toxicity have been identified in recent years. The latest advances in drug design, characterization, structure-activity relationship (SAR) research, and modes of action of newly synthesized, powerful small molecules P-gp inhibitors over the previous ten years are highlighted in this review. P-gp transporter over-expression has been linked to MDR, therefore the development of P-gp inhibitors will expand our understanding of the processes and functions of P-gp-mediated drug efflux, which will be helpful for drug discovery and clinical cancer therapies.

A Direct Epitaxial Approach To Achieving Ultrasmall and Ultrabright InGaN Micro Light-Emitting Diodes (µLEDs).

A direct epitaxial approach to achieving ultrasmall and ultrabright InGaN micro light-emitting diodes (µLEDs) has been developed, leading to the demonstration of ultrasmall, ultraefficient, and ultracompact green µLEDs with a dimension of 3.6 µm and an interpitch of 2 µm. The approach does not involve any dry-etching processes which are exclusively used by any current µLED fabrication approaches. As a result, our approach has entirely eliminated any damage induced during the dry-etching processes. Our green µLED array chips exhibit a record external quantum efficiency (EQE) of 6% at ∼515 nm in the green spectral region, although our measurements have been performed on bare chips which do not have any coating, passivation, epoxy, or reflector, which are generally used for standard LED packaging in order to enhance extraction efficiency. A high luminance of >107 cd/m2 has been obtained on the µLED array bare chips. Temperature-dependent measurements show that our µLED array structure exhibits an internal quantum efficiency (IQE) of 28%. It is worth highlighting that our epitaxial approach is fully compatible with any existing microdisplay fabrication techniques.

Nonpolar (112Ì 0) GaN Metal-Semiconductor-Metal Photodetectors with Superior Performance on Silicon.

This article reports a nonpolar GaN metal-semiconductor-metal (MSM) photodetector (PD) with an ultrahigh responsivity and an ultrafast response speed in the ultraviolet spectral region, which was fabricated on nonpolar (112̅0) GaN stripe arrays with a major improvement in crystal quality grown on patterned (110) silicon substrates by means of using our two-step processes. Our nonpolar GaN MSM-PD exhibits a responsivity of 695.3 A/W at 1 V bias and 12628.3 A/W at 5 V bias, both under 360 nm ultraviolet illumination, which are more than 20 times higher and 4 orders of magnitude higher compared to the current state-of-the-art photodetector, respectively. The nonpolar GaN MSM-PD displays a rise time and a fall time of 66 and 43 µs, respectively, which are 3 orders of magnitude faster compared to the current state-of-the-art photodetector.

Exploring an Approach toward the Intrinsic Limits of GaN Electronics.

To fully exploit the advantages of GaN for electronic devices, a critical electric field that approaches its theoretical value (3 MV/cm) is desirable but has not yet been achieved. It is necessary to explore a new approach toward the intrinsic limits of GaN electronics from the perspective of epitaxial growth. By using a novel two-dimensional growth mode benefiting from our high-temperature AlN buffer technology, which is different from the classic two-step growth approach, our high-electron-mobility transistors (HEMTs) demonstrate an extremely high breakdown field of 2.5 MV/cm approaching the theoretical limit of GaN and an extremely low off-state buffer leakage of 1 nA/mm at a bias of up to 1000 V. Furthermore, our HEMTs also exhibit an excellent figure-of-merit (Vbr2/Ron,sp) of 5.13 × 108 V2/Ω·cm2.