Novel 4-Thiazolidinone Derivatives as Anti-Infective Agents: Synthesis, Characterization, and Antimicrobial Evaluation

A series of new 4-thiazolidinone derivatives was synthesized, characterized by spectral techniques, and screened for antimicrobial activity. All the compounds were evaluated against five Gram-positive bacteria, two Gram-negative bacteria, and two fungi, at concentrations of 50, 100, 200, 400, 800, and 1600 µg/mL, respectively. Minimum inhibitory concentrations of all the compounds were also determined and were found to be in the range of 100–400 µg/mL. All the compounds showed moderate-to-good antimicrobial activity. Compounds 4a [2-(4-fluoro-phenyl)-3-(4-methyl-5,6,7,8-tetrahydro-quinazolin-2-yl)-thiazolidin-4-one] and 4e [3-(4,6-dimethyl-pyrimidin-2-yl)-2-(2-methoxy-phenyl)-thiazolidin-4-one] were the most potent compounds of the series, exhibiting marked antimicrobial activity against Pseudomonas fluorescens, Staphylococcus aureus, and the fungal strains. Thus, on the basis of results obtained, it may be concluded that synthesized compounds exhibit a broad spectrum of antimicrobial activity

Syntheses, Characterization and Antimicrobial Evaluation of Some 1, 3, 5-Trisubustituted Pyrazole Derivatives

A series of 1, 3, 5-trisubustituted pyrazole derivatives were synthesized and screened for antimicrobial activity. The compounds (2j-o) were evaluated against two gram-positive and two gram-negative bacteria and one fungus, at concentrations of 10 µg/mL and 50 µg/mL. The compounds were founds to be inactive against P. aeruginosa and A. niger but exhibited moderate activity against B. subtilis, E. coli and S. aureus. It can be concluded that the newly synthesized compounds possess promising antimicrobial activity

Isolation, Characterization and Activity of the Flowers of Rhododendron arboreum (Ericaceae)

The flowers of Rhododendron arboreum have been reported to possess certain polyphenolic compounds. Thus, this study was aimed at the anti-microbial and phytochemical screening of the flowers. Important bioactive agents like steroids, saponins and flavonoids were detected in the flowers. Quercetin (a flavonoid) was isolated from the diethyl ether fraction of alcoholic extract by solvent-solvent extraction method. Isolated quercetin was identified and characterized by chemical tests, M.P., TLC, paper chromatography (with authentic marker) and spectroscopic methods like UV-Visible, FT-IR, 1HNMR, 13CNMR and Mass spectroscopy. The anti-microbial activity of the alcoholic and aqueous extract and isolated quercetin were investigated against five bacterial and two fungal strains by agar well-diffusion method. The activity was found to be concentration dependent. Ethanolic extract was found to be more active in comparison to the aqueous extract. Hence, isolation was done with ethanolic extract. The lowest effective concentration of quercetin was found to be 12.5 mg/ml against S. aureus and P. aeruginosa. Both extracts and isolated quercetin were found ineffective against fungal strains. Quercetin may be one of the components responsible for the observed anti-microbial activity of the plant

Solution‐Processed Ternary Organic Photodetectors with Ambipolar Small‐Bandgap Polymer for Near‐Infrared Sensing

Abstract Organic photodetectors (OPDs) detecting light in the near‐infrared (NIR) range from 900 to 1200 nm offer numerous applications in biomedical imaging and health monitoring. However, an ultra‐low bandgap of the electron donor compound required to achieve NIR detection poses a unique challenge in selecting a complementary acceptor material with a suitable energy‐level offset. To tackle this, a solution‐processed, fullerene‐dominated, ternary device is engineered by adding an ultra‐low bandgap (0.6–0.8 eV) ambipolar polymer, polybenzobisthiadiazole‐dithienocyclopentane (PBBTCD), into the active layer of visible‐light‐responsive OPDs (bandgap of 1.8 eV) to form a ternary blend. The resulting OPD benefits from the extended absorption beyond 1000 nm. The cascaded energy level alignment within the ternary blend and the applied reverse bias both improve the overall NIR photocurrent responsivity by 2 orders of magnitude, reaching 0.4 mA W−1 at 1050 nm and −2 V for ternary devices. Furthermore, a photovoltage responsivity of 0.3 mV m2 W−1 along with significant open‐circuit voltage (Voc) of 0.12 V allow NIR detection in the Voc mode. Prominently, this ability is accomplished with a minimal presence of PBBTCD. Taken together, this work indicates potential strategies for extending the spectral activity of conventional OPDs through introduction of an ambipolar ultra‐low bandgap polymer as a minor element

Low bandgap donor-acceptor-donor-based TPA-azaBODIPY-TPA small molecule for flexible near-infrared organic photodetectors

Organic photodetectors (OPDs) hold great promise for use in flexible electronics as they can be designed on substrates featuring various shapes and using cost-effective solution-processed methods. Organic conjugated materials offering two or more distinct optoelectronic functions are especially appealing here as they provide multifunctionality while also retaining the ease of fabrication and low-cost advantage. One such material is TPA-azaBODIPY-TPA that has been shown to feature ideal charge transfer properties and excitation energy levels. In our recent work, we demonstrated the versatile nature of this material acting as either a charge transport interlayer in perovskite solar cells, or as a light-absorbing layer in OPDs. TPA-azaBODIPY-TPA-based solar cells showed a 60 % increase in power conversion efficiency when compared to a control device using a conventional interlayer PEDOT:PSS. Having also demonstrated the successful utilization of TPA-azaBODIPY-TPA in OPDs manufactured on glass substrates, we further explore its applications in the design and fabrication of flexible OPDs for near-infrared sensing. Fabricated devices on flexible substrates show a near-infrared spectral responsivity of 49 mA W-1 at 730 nm, a high linear dynamic range of 110 dB and fast temporal responses below 100 μs. With robust thermal stability as well as excellent solubility and processability, TPA-azaBODIPY-TPA is found to be perfect candidate for the next-generation of smart optoelectronic flexible devices.</p

Schizonticidal antimalarial sesquiterpene lactones from <i>Magnolia champaca</i> (L.) Baill. ex Pierre: microwave-assisted extraction, HPTLC fingerprinting and computational studies

<p>The present study explored the schizonticidal potential of traditionally used <i>Magnolia champaca</i> (L.) Baill. ex. Pierre flowers, identifying constituents of interest. The extraction of phytoconstituents was carried out by microwave-assisted technique, isolated via column chromatography, and characterised by various physicochemical, spectral (IR, 1H-NMR and Mass) and chromatographic (HPTLC) techniques. Both the isolated compounds (parthenolide and costunolide diepoxide) exhibited potent schizonticidal antimalarial activity during primary screening in rodent models, with maximum parasitaemia suppression (85.18% and 83.65%, respectively) at a dose of 20 mg/kg body weight when compared to the standard drugs chloroquine and artesunate. <i>In silico</i> techniques were employed to identify the probable biological target and mechanism of action of these isolated compounds. Molecular docking studies also predicted the binding orientations and multi-targeted action of these compounds, in particular costunolide diepoxide with maximum affinity towards SERCA and DHFR proteins. Additionally, favourable <i>in silico</i> ADMET parameters were envisaged through various computational programmes.</p

Energy-Level Manipulation in Novel Indacenodithiophene-Based Donor–Acceptor Polymers for Near-Infrared Organic Photodetectors

Organic photodetectors (OPDs) are promising candidates for next-generation digital imaging and wearable sensors due to their low cost, tuneable optoelectrical properties combined with high-level performance, and solution-processed fabrication techniques. However, OPD detection is often limited to shorter wavelengths, whereas photodetection in the near-infrared (NIR) region is increasingly being required for wearable electronics and medical device applications. NIR sensing suffers from low responsivity and high dark currents. A common approach to enhance NIR photon detection is lowering the optical band gap via donor–acceptor (D–A) molecular engineering. Herein, we present the synthesis of two novel indacenodithiophene (IDT)-based D–A conjugated polymers, namely, PDPPy-IT and PSNT-IT via palladium-catalyzed Stille coupling reactions. These novel polymers exhibit optical band gaps of 1.81 and 1.27 eV for PDPPy-IT and PSNT-IT, respectively, with highly desirable visible and NIR light detection through energy-level manipulation. Moreover, excellent materials’ solubility and thin-film processability allow easy incorporation of these polymers as an active layer into OPDs for light detection. In the case of PSNT-IT devices, a photodetection up to 1000 nm is demonstrated with a peak sensitivity centered at 875 nm, whereas PDPPy-IT devices are efficient in detecting the visible spectrum with the highest sensitivity at 660 nm. Overall, both OPDs exhibit spectral responsivities up to 0.11 A W–1 and dark currents in the nA cm–2 range. With linear dynamic ranges exceeding 140 dB and fast response times recorded below 100 μs, the use of novel IDT-based polymers in OPDs shows great potential for wearable optoelectronics

Versatile aza-BODIPY-based low-bandgap conjugated small molecule for light harvesting and near-infrared photodetection

The versatile nature of organic conjugated materials renders their flawless integration into a diverse family of optoelectronic devices with light-harvesting, photodetection, or light-emitting capabilities. Classes of materials that offer the possibilities of two or more distinct optoelectronic functions are particularly attractive as they enable smart applications while providing the benefits of the ease of fabrication using low-cost processes. Here, we develop a novel, multi-purpose conjugated small molecule by combining boron-azadipyrromethene (aza-BODIPY) as electron acceptor with triphenylamine (TPA) as end-capping donor units. The implemented donor–acceptor–donor (D–A–D) configuration, in the form of TPA-azaBODIPY-TPA, preserves ideal charge transfer characteristics with appropriate excitation energy levels, with the additional ability to be used as either a charge transporting interlayer or light-sensing semiconducting layer in optoelectronic devices. To demonstrate its versatility, we first show that TPA-azaBODIPY-TPA can act as an excellent hole transport layer in methylammonium lead triiodide (MAPbI3)-based perovskite solar cells with measured power conversion efficiencies exceeding 17%, outperforming control solar cells with PEDOT:PSS by nearly 60%. Furthermore, the optical bandgap of 1.49 eV is shown to provide significant photodetection in the wavelength range of up to 800 nm where TPA-azaBODIPY-TPA functions as donor in near-infrared organic photodetectors (OPDs) composed of fullerene derivatives. Overall, the established versatility of TPA-azaBODIPY-TPA, combined with its robust thermal stability as well as excellent solubility and processability, provides a new guide for developing highly efficient multi-purpose electronic materials for the next-generation of smart optoelectronic devices. (Figure presented.).</p