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21.
Membrane Disruption and Enhanced Inhibition of Cell‐Wall Biosynthesis: A Synergistic Approach to Tackle Vancomycin‐Resistant Bacteria
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Venkateswarlu Yarlagadda Dr. Sandip Samaddar Dr. Krishnamoorthy Paramanandham Dr. Bibek R. Shome Dr. Jayanta Haldar 《Angewandte Chemie (International ed. in English)》2015,54(46):13644-13649
Resistance to glycopeptide antibiotics, the drugs of choice for life‐threatening bacterial infections, is on the rise. In order to counter the threat of glycopeptide‐resistant bacteria, we report development of a new class of semi‐synthetic glycopeptide antibiotics, which not only target the bacterial membrane but also display enhanced inhibition of cell‐wall biosynthesis through increased binding affinity to their target peptides. The combined effect of these two mechanisms resulted in improved in vitro activity of two to three orders of magnitude over vancomycin and no propensity to trigger drug resistance in bacteria. In murine model of kidney infection, the optimized compound was able to bring bacterial burden down by about 6 logs at 12 mg kg?1 with no observed toxicity. The results furnished in this report emphasize the potential of this class of compounds as future antibiotics for drug‐resistant Gram‐positive infections. 相似文献
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Adhikari B Nanda J Banerjee A 《Chemistry (Weinheim an der Bergstrasse, Germany)》2011,17(41):11488-11496
The N-terminally pyrene-conjugated oligopeptide, Py-Phe-Phe-Ala-OMe, (Py=pyrene 1-butyryl acyl) forms transparent, stable, supramolecular fluorescent organogels in various organic solvents. One of these organogels was thoroughly studied using various techniques including transmission electron microscopy (TEM), field-emission scanning electron microscopy (FESEM), atomic force microscopy (AFM), Fourier-transform infrared (FTIR) spectroscopy, photoluminescence (PL) spectroscopy, and rheology. Unfunctionalized and non-oxidized graphene was successfully incorporated into this fluorescent organogel in o-dichlorobenzene (ODCB) to form a stable hybrid organogel. Graphene is well dispersed into the gel medium by using non-covalent π-π stacking interactions with the pyrene-conjugated gelator peptide. In the presence of graphene, the minimum gelation concentration (mgc) of the hybrid organogel was lowered significantly. This suggests that there is a favorable interaction between the graphene and the gelator peptide within the hybrid organogel system. This hybrid organogel was characterized using TEM, AFM, FTIR, PL, and rheological studies. The TEM study of graphene-containing hybrid organogel revealed the presence of both graphene sheets and entangled gel nanofibers. The AFM study indicated the presence of 3 to 4 layers in exfoliated graphene in ODCB and the presence of both graphene nanosheets and the network of gel nanofibers in the hybrid gel system. The rheological investigation suggested that the flow of the hybrid organogel had become more resistant towards the applied angular frequency upon the incorporation of graphene into the organogel. The hybrid gel is about seven times more rigid than that of the native gel. 相似文献
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Nagarwal RC Singh PN Kant S Maiti P Pandit JK 《Chemical & pharmaceutical bulletin》2011,59(2):272-278
The aim of this investigation was to develop 5-fluorouracil (5-FU) loaded chitosan nanoparticles (CH-DNPs) for ophthalmic delivery. CH-DNPs were fabricated by ionotropic gelation mechanism using chitosan (CH) and a polyanion (TPP). The nanoparticles were smooth and spherical, confirmed by scanning electron microscopy (SEM) and atomic force microscope (AFM). CH/TPP mass ratio and TPP significantly changed the particles size morphology and encapsulation efficiency. The nanoparticles size ranged from approximately 114 to 192 nm and had a positive zeta potential (30±4 mV). The encapsulation efficiency, loading capacity and recovery of DNPs were 8.12-34.32%, 3.14-15.24% and 24.22 to 67% respectively. Physical characterization was done by Fourier transform infrared (FT-IR) and X-ray diffraction (XRD). No interaction was observed in between drug and polymer and crystallinity of drug was not changed in drug loaded nanoparticles. In-vitro release study of DNPs showed diffusion controlled release. Bioavailability study of batch CS9 was studied in rabbit eye and compare to 5-FU solution. 5-FU level was significantly higher in aqueous humor of rabbit eye. Ocular tolerance was studied in the eye of New Zealand rabbits and tested formulation was non-irritant with no sign of inflammation. 相似文献
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Summary Cobaloxime complexes containing the biologically active ligand imidazole and poorly coordinating anions, such as ClO
4
–
or BF
4
–
, have been synthesised. The perchlorate anion is not involved in coordination and there is evidence that [Co(DH)2(L)2]ClO4 complexes are formed, whereas the tetrafluoroborate anion is involved in weak coordination giving complexes of the type [Co(DH)2(L)(BF4)] in the solid state. However, solvolysis of these latter complexes in solution yields 11 electrolytic species. The i.r. and electronic spectra, magnetic and conductivity measurements in nonaqueous media have been employed to characterise the complexes.Ligand abbreviations Py
pyridine
- Im
imidazole
- Me
methyl
- Al
allyl
- Vi
vinyl 相似文献
26.
Because of the critical slowing down of the order parameter fluctuations, they do not follow the temperature oscillations produced adiabatically by a pressure wave. The resulting hysteresis leads to the observed dispersion and attenuation of ultrasound. The effect depends entirely upon the frequency dependent specific heat. We discuss here the mathematical features of this function, including it dynamic scaling properties. 相似文献
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[reaction: see text] We report highly efficient two-step procedures for the synthesis of 1,3-oxazole-, thiazole-, and imidazole-containing peptides on solid phase from dipeptides composed of C-terminal threonine, serine, cysteine, or diaminopropionic acid by using different cyclodehydration procedures followed or preceded by oxidation. The methods are compatible with Fmoc solid-phase peptide synthesis conditions and with N-Fmoc, N-Boc, N-Cbz, and N-Alloc protecting groups. 相似文献
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Dr. Sourav Maiti Dr. Jayanta Dana Prof. Dr. Hirendra N. Ghosh 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(3):692-702
The photovoltaic performance of quantum-dot solar cells strongly depends on the charge-carrier relaxation and recombination processes, which need to be modulated in a favorable way to obtain maximum efficiency. Recently, significant efforts have been devoted to investigate the carrier dynamics of nanocrystal sensitizers, both in solution and deposited on TiO2 photoanodes, with the aim to correlate the excitonics with solar-energy conversion efficiency. This Minireview summarizes some proof of the concepts that efficiency can be directly correlated to the exciton dynamics of quantum-dot solar cells. The presented findings are based on CdSeS alloy, CdSe/CdS core/shell, Au/CdSe nanohybrids, and Mn-doped CdZnSSe nanocrystals, where the favourable excitonic processes are optimized to enhance the efficiency. Future prospects and limitations are addressed as well. 相似文献