A Reversible Mechanochromic AIEgen Based on Triphenylamine for the Selective Detection of Vitamin B2 (Riboflavin) in Aqueous Media and Histotoxicity.

(E)-Ethyl 2-cyano-3-(4'-(diphenyl amino)-[1,1'-biphenyl]-4-yl) acrylate (RSJ) is a novel luminogen based on triphenylamine. It has been fully synthesized and characterized, exhibiting an incredible photophysical phenomenon known as aggregation-induced emission (AIE). This work describes a fluorescent sensor that detects vitamin B2 in mixed aqueous media with high selectivity and a low limit of detection as well as a mechanism for reversible mechanochromic luminescence. Moreover, the molecule was validated for its nontoxicity in water using a histotoxicological study. Fish subjected to two different concentrations of the "novel luminogen" that displayed photophysical phenomena during sensing of vitamin B2 (riboflavin) in mixed aqueous media did not exhibit any significant differences in the structural makeup of their liver, kidney, gills, brain, and muscle tissues when compared with the control group.

Nanomaterials Based Multifunctional Bioactivities of V2O5 and Mesoporous Carbon@V2O5 Composite: Preparation and Characterization.

Nanocarriers have attracted considerable interest due to their prospective applications in the delivery of anticancer medications and their distinct bioactivities. Biogenic nanostructures can be effective nanocarriers for delivering drugs as a consequence of sustainable and biodegradable biomass-derived nanostructures that perform specific functions. In this case, a vanadium oxide (V2O5) and mesoporous carbon@V2O5 (C@V) composite was developed as a possible drug delivery system, and its bioactivities, including antioxidant, antibacterial, and anticancer, were investigated. Doxorubicin (DOX), an anticancer drug, was introduced to the nanoparticles, and the loading and release investigation was conducted. Strong interfacial interactions between mesoporous carbon (MC) and V2O5 nanostructures have been found to improve performance in drug loading and release studies and bioactivities. After incubation, the potent anticancer effectiveness was seen based on C@V nanocomposite. This sample was also utilized to research potential biomedical uses as an antioxidant, antibacterial, and anticancer. The most effective antioxidant, the C@V sample (61.2%), exhibited a higher antioxidant activity than the V-2 sample (44.61%). The C@V sample ultimately attained a high DOX loading efficacy of 88%, in comparison to a pure V2O5 sample (V-2) loading efficacy of 80%. Due to the combination of mesoporous carbon and V2O5, which increases specific surface area and surface sites of action as well as the morphology, it proved that the mesoporous carbon@V2O5 composite (C@V) sample demonstrated greater efficacy.

Vidarabine as a novel antifungal agent against Candida albicans: insights on mechanism of action.

Around 1.5 million mortality cases due to fungal infection are reported annually, posing a massive threat to global health. However, the effectiveness of current antifungal therapies in the treatment of invasive fungal infections is limited. Repurposing existing antifungal drugs is an advisable alternative approach for enhancing their effectiveness. This study evaluated the antifungal efficacy of the antiviral drug vidarabine against Candida albicans ATCC 90028. Antifungal susceptibility testing was performed by microbroth dilution assay and further processed to find the minimum fungicidal concentration. Investigation on probable mode of vidarabine action against C. albicans was assessed by using the ergosterol reduction assay, reactive oxygen species (ROS) accumulation, nuclear condensation, and apoptosis assay. Results revealed that C. albicans was susceptible to vidarabine action and exhibited minimum inhibitory concentration at 150 µg/ml. At a concentration of 300 µg/ml, vidarabine had fungicidal activity against C. albicans. 300 µg/ml vidarabine-treated C. albicans cells demonstrated 91% reduced ergosterol content. Annexin/FITC/PI assay showed that vidarabine (150 µg/ml) had increased late apoptotic cells up to 31%. As per the fractional inhibitory concentration index, vidarabine had synergistic activity with fluconazole and caspofungin against this fungus. The mechanism underlying fungicidal action of vidarabine was evaluated at the intracellular level, and probably because of increased nuclear condensation, enhanced ROS generation, and cell cycle arrest. In conclusion, this data is the first to report that vidarabine has potential to be used as a repurposed antifungal agent alone or in combination with standard antifungal drugs, and could be a quick and safe addition to existing therapies for treating fungal infections.

Furan-Dihydroquinazolinone Based Fluorescent Nanoprobe for Selective Recognition of 4-Nitrophenol: A Spectofluorimetric Approach.

Fluorescent organic nanoparticles (FONPs) have attracted much attention as a practicable and effective platform for detection applications. The present article describes the preparation of FONPs derived from the quinazolinone-based 2-(furan-2-yl)-2,3-dihydroquinazolin-4(1H)-one derivative FHDQ. Self-assembly of FHDQ in an aqueous medium resulted in the formation of FONPs through H-type aggregation and showed excellent fluorescence properties. The presence of other coexisting species solutions did not affect the selective fluorescence quenching observed with the addition of 4-nitrophenol (4-NP). The photophysical properties, i.e., UV-Vis absorbance, fluorescence emission, and lifetime measurements together with zeta particle sizer, support excited-state complex formation followed by a dynamic fluorescence quenching phenomenon in the emission of FDHQNPs. In the concentration range of 0 to 36 µg.[Formula: see text], the detection limit of this turn-off sensor FDHQNPs against 4-NP was determined to be 0.01611 µM. Finally, the practicability of the FDHQNPs for the analysis of 4-NP in environmental samples was demonstrated.

Histotoxicity of AIEgen Based on Triphenylamine for the Simultaneous and Discriminatory Sensing of Hg2+ and Ag+ Directly in Aqueous Media for Environmental Applications.

A newly synthesized AIEgen based on triphenylamine is fully characterized and coded as BRA for the simultaneous and discriminatory selective detection of Hg2+ and Ag+ ions directly in mixed aqueous media for the identification and purification of water with a low detection limit. Moreover, we employed BRA in histotoxicity in that when compared to the control group, fish exposed to the "novel synthesized luminogen (BRA)" that demonstrated photophysical phenomena during the "sensing of mercury and silver (heavy metals) in aqueous media" did not show any major distinguishing changes in the architecture of their gills, liver, muscle, brain, kidney, and heart tissues.

Construction of Waste Chalk Powder into mpg-C3N4-CaSO4 as an Efficient Photocatalyst for Dye Degradation under UV-Vis Light and Sunlight.

In this article, we present the synthesis of calcium sulfate nanoparticles (CaSO4 NPs) from waste chalk powder by the calcination method. These CaSO4 NPs were utilized for the construction of a mesoporous graphitic carbon nitride-calcium sulfate (mpg-C3N4-CaSO4) photocatalyst. Synthesized materials were confirmed by several characterization techniques. The photocatalytic performance of the synthesized samples was tested by the degradation of methylene blue (MB) in the presence of both UV-vis light and sunlight. The efficiency of photocatalytic degradation of MB dye using the optimized mpg-C3N4-CaSO4-2 composite reached 91% within 90 min in the presence of UV-vis light with superb photostability and recyclability after five runs compared to individual mpg-C3N4 and CaSO4 NPs and reached 95% within 120 min under sunlight. Histotoxicological studies on fish liver and ovary indicated that the dye containing the solution damaged the structure of the liver and ovary tissues, whereas the photodegraded solution of MB was found to be less toxic and caused negligible alterations in their typical structure similar to the control group.

Bioderived Mesoporous Carbon@Tungsten Oxide Nanocomposite as a Drug Carrier Vehicle of Doxorubicin for Potent Cancer Therapy.

Scientists have investigated the possibility of employing nanomaterials as drug carriers. These nanomaterials can preserve their content and transport it to the target region in the body. In this investigation, we proposed a simple method for developing distinctive, bioderived nanostructures with mesoporous carbon nanoparticles impregnated with tungsten oxide (WO3). Prior to characterizing and encapsulating WO3 with bioderived mesoporous carbon, the anticancer drug doxorubicin (DOX) was added to the nanoparticles and examined loading and release study. The approaches for both nanoparticle production and characterization are discussed in detail. Colloidal qualities of the nanomaterial can be effectively preserved while also allowing transdermal transportation of nanoparticles into the body by forming them into green, reusable, and porous nanostructures. Although the theories of nanoparticles and bioderived carbon each have been studied separately, the combination presents a new route to applications connected to nanomedicine. Furthermore, this sample was used to study exotic biomedical applications, such as antioxidant, antimicrobial, and anticancer activities. The W-3 sample had lower antioxidant activity (44.01%) than the C@W sample (56.34%), which was the most potent. A high DOX entrapment effectiveness of 97% was eventually achieved by the C@W sample, compared to a pure WO3 entrapment efficiency of 91%. It was observed that the Carbon/WO3 composite (C@W) sample showed more efficacy because the mesoporous carbon composition with WO3 increases the average surface area and surface-active locations.

SDS-capped 1-pyrenecarboxaldehyde nanoprobe for selective detection of Cu2+ ion from water samples: Spectroscopic approach.

Sodium dodecyl sulfate (SDS)-capped 1-pyrenecarboxaldehyde nanoparticles (PyalNPs) were prepared using a reprecipitation method in an aqueous medium and exhibited red-shifted aggregation-induced enhanced emission (AIEE). The dynamic light scattering (DLS) examination showed narrower particle size distribution with an average particle size of 41 nm, whereas -34.5 mV zeta potential value indicate the negative surface charge and good stability of nanoparticles (NPs) in an aqueous medium. The AIEE was seen at λmax = 473 nm in a fluorescence spectrum of a PyalNP suspension. In the presence of Cu2+ ions, the fluorescence of PyalNPs quenches very significantly, even in the presence of other metal ions like Ba2+ , Ca2+ , Cd2+ , Co2+ , Al3+ , Fe2+ , Hg2+ , Ni2+ and Mg2+ . The changes in the fluorescence lifetime of PyalNPs in the presence of Cu2+ ions suggested that the type of quenching was dynamic. The fluorescence quenching data for the NPs suspension fitted well into a typical Stern-Volmer relationship in the concentration range 1.0-25 µg/ml of Cu2+ ions. The estimated value of the correlation coefficient R2 = 0.9877 was close to 1 and showed the linear relationship between quenching data and Cu2+ ion concentration. The limit of detection (LOD) was found to be 0.94 ng/ml and is far below the tolerable intake limit value of 1.3 µg/ml accepted by the World Health Organization for Cu2+ ions in drinking water. The fluorescence quenching approach for a SDS-capped Pyal nanosuspension for copper ion quantification is of high specificity and coexisting ions were found to interfere very negligibly. The developed method was successfully applied for the estimation of copper ions in river water samples.

Valorization of Waste Tungsten Filament into mpg-C3N4-WO3 Photocatalyst: A Sustainable e-Waste Management and Wastewater Treatment.

The waste of tungsten filament materials in the environment is one of the reasons for environmental pollution, and it is very dangerous to animals and plants. To date, not much attention has been given to its utility or recyclability. Herein, the present work reported the synthesis of tungsten trioxide nanoparticles (WO3 NPs) by the utilization of cost-free waste tungsten filament by a simple calcination method. A mesoporous graphitic carbon nitride-tungsten trioxide (mpg-C3N4-WO3) composite designed from the WO3 NPs produced from tungsten filament waste and thiourea as a carbon and nitrogen precursor by a one-step calcination method. The synthesized samples were characterized and confirmed by different characterization techniques. The photocatalytic behavior of the synthesized mpg-C3N4-WO3 composite was assessed, with respect to the effect of initial pH, amount of photocatalyst, dye concentration, and reaction time, as well for the degradation of Methylene Blue (MB) dye under sunlight. The best photocatalytic performance (92%) was achieved using mpg-C3N4-WO3 with experimental condition ([photocatalyst] = 100 mg/L, [MB]0 = 10 mg/L, pH 8, and time = 120 min) under sunlight irradiation with excellent photostability than that of isolated mpg-C3N4 and WO3 NPs. The histotoxicological studies also showed that the photodegraded products of MB were found to be nontoxic and did not structurally changes in the gill architecture as well as brain tissues of freshwater fish Labeo rohita.

Effect of various aqueous extracting agents on fluorescence properties of waste tea residue derived carbon dots (WTR-CDs): Comparative spectroscopic analysis.

Fluorescent carbon dots (CDs) are one of the important carbonaceous nanomaterials in the area of nanoscience and nanotechnology because of their interesting physical as well as chemical properties. Herein we studied the effect of various aqueous extracting agents on fluorescence properties of waste tea residue-based carbon dots (WTR-CDs). WTR-CDs are firstly synthesized by utilizing kitchen waste-based carbonaceous biomass. To check the role of various aqueous media during the course of WTR-CDs synthesis from carbonized carbon powder, extraction of WTR-CDs was carried out in various kinds of aqueous media viz., only aqueous (100% water, WT), aqueous-alcoholic (10% ethanol, ET), aqueous-acidic (10% acetic acid, AA), and aqueous-basic (10% ammonia, AM). The consequences of extracting agents on the photophysical properties of final WTR-CDs-WT, WTR-CDs-ET, WTR-CDs-AA and WTR-CDs-AM were also discussed in detail. We have observed interesting blue shift fluorescence spectra in acidic medium for WTR-CDs-AA and polar protic solvents compared to polar aprotic medium. The solvatochromic behaviour of WTR-CDs-WT in model polar and non-polar solvent was also studied. The effect of cationic, anionic and non-anionic surfactants on the fluorescence of WTR-CDs-WT was also evaluated. The proposed findings may help researchers in the near future to obtain fast, easy and direct synthesize CDs from a variety of biomass-based precursors under different aqueous conditions.

Fabrication and Characterization of Anthracene Doped P-terphenyl Thin Films By Spin Coating Technique; Investigation of Fluorescence Properties.

Thin films of p-terphenyl luminophors doped by varying amounts of anthracene were prepared by using spin coating technique. The morphological, structural, and photophysical investigation of thin films of p-terphenyl as a function of anthracene concentration is studied by using scanning electron microscopy (SEM), X-ray diffraction (XRD), fluorescence spectroscopy and fluorescence microscopy. The results of XRD and SEM studies indicated that the doped p-terphenyl thin film is homogeneous as compared with a bare p-terphenyl thin film. The fluorescence spectroscopy results indicate complete quenching of p-terphenyl fluorescence and simultaneous sensitization of blue anthracene like emission towards the red side of the spectrum with maximum intensity at 410 nm. The blue intense emission of anthracene seen in fluorescence microscopy images is in agreement with observed fluorescence spectral results. A suitable mechanism of excitation energy transfer (EET) from p-terphenyl to anthracene molecules is proposed and discussed on the basis of energy level diagram. The efficient EET is believed to occur by the orientation of phenyl rings of p-terphenyl in excited state. As the concentration of doped anthracene increases, the fluorescence intensity of doped p-terphenyl and Full Width at Half Maximum (FWHM) found to be increased. The p-terphenyl film containing 0.65 moles of anthracene is of FWHM as low as 28.51 nm. Such narrow band blue emitting doped luminophors are of demand in light emitting diodes (OLED) and scintillation applications.

Nitrogen-doped carbon dot threads as a "turn-off" fluorescent probe for permanganate ions and its hydrogel hybrid as a naked eye sensor for gold(III) ions.

Highly fluorescent nitrogen-doped carbon dot (NCD) threads were synthesized via simple pyrolysis of citric acid, p-hydroxybenzoic acid, and ammonia. The NCDs show excitation-independent behavior with maximum excitation and emission wavelengths of 350 nm and 435 nm, respectively. The developed probe was used as a turn-off fluorescent sensor for the selective and sensitive determination of permanganate ions in aqueous media. The probe's hydrogel hybrid displayed a beautiful purple color demonstrating its potential as a naked eye sensor for gold detection. The ratiometric sensor exhibited excellent selectivity towards permanganate ions over 27 other ions with a linear range of 510 nM to 2 µM, a detection limit of 170 nM, and a linear regression value (R2) of 0.9944. Similarly, the linear range and limit of detection for gold ions was 3.89-20 µM and 1.285 µM, respectively. The synthesized NCDs were also used as a fluorescent ink as well as a naked eye marker in association with a gold solution demonstrating its potential forensic and anti-counterfeiting applications. Graphical abstract.

A Phenazine based colorimetric and fluorescent chemosensor for sequential detection of Ag+ and I- in aqueous media.

A new colorimetric and fluorescent probe MNTPZ based on 1H-imidazo[4,5-b]phenazine derivative has been designed and synthesized for successive detection of Ag+ and I- . The probe MNTPZ shows selective colorimetric response by a change in color from yellow to orange and "turn-off" fluorometric response upon binding with Ag+ in DMSO: Water (pH = 7, 1:1, v/v) over other cations. The binding mode of probe MNTPZ to Ag+ was studied by Job's plot, 1 H NMR studies, FT-IR spectroscopy and DFT calculations. Moreover, the situ generated probe MNTPZ+ Ag+ complex acted as an efficient fluorometric "turn-on" probe for I- via Ag+ displacement approach. The detection limit of probe MNTPZ for Ag+ and the resultant complex probe MNTPZ+ Ag+ for I- were determined to be 1.36 µmol/L and 1.03 µmol/L respectively. Notably, the developed probe was successfully used for quantitative determination of I- in real samples with satisfactory results.

Enhanced Exciplex Emission of Pyrene Thin Films Doped by Perylene: Structural, Photophysical and Morphological Investigation.

The present work reports on the preparation of thin films of pyrene luminophors doped by varying amounts of perylene by spin coating technique. The structural, morphological, and photophysical properties of pyrene thin films have been investigated as a function of perylene contents. X-ray diffraction studies of doped thin films show well-defined peaks, and estimated crystallite size decreases with increasing perylene content, due to the formation of closed packed crystal structure. SEM images of pure pyrene revealed smooth, and compact and separated crystals with amounts of perylene. The result of absorption spectra showed decrease in intensity with perylene content. However, the fluorescence spectra of pyrene containing higher amounts of perylene showed broad and structureless exciplex emission at 510 nm. The emission colour of pyrene luminophors tuned from blue to green by controlling the concentration of perylene. The phenomenon of change in colour was seen due to efficient excitation energy transfer from pyrene to perylene in thin films. It also found that the intensity of exciplex emission increases with increasing concentration of perylene is of high demand in fluorescent lamp as well as green organic light emitting diodes.

Studies on Structural, Optical, Thermal and Electrical Properties of Perylene-Doped p-terphenyl Luminophors.

A simple solid state reaction technique was employed for the preparation of polycrystalline luminophors of p-terphenyl containing different amounts of perylene followed by spectral characterization techniques viz. XRD, SEM, TGA-DSC, UV-Visible spectroscopy, thermo-electrical conductivity, fluorescence spectroscopy, fluorescence life time spectroscopy and temperature dependent fluorescence. X-ray diffraction profiles of the doped p-terphenyl reveal well-defined and sharp peaks indicate homogeneity and crystallinity. The SEM micrograph of pure p-terphenyl exhibit flakes like grains and then compact and finally gets separately with perylene amounts. The observed results indicate that closed packed crystal structures of doped p-terphenyl during crystal formation. The band gaps estimated from UV-visible spectroscopy decreased from 5.20 to 4.10 eV, while thermo-electrical conductivity increases with perylene content. The fluorescence spectra showed partial quenching of p-terphenyl fluorescence and simultaneously sensitization of perylene fluorescence at the excitation wavelength of p-terphenyl (290 nm) due to excitation energy transfer from p-terphenyl to perylene. The observed sensitization results are in harmony with intense blue color seen in fluorescence microscopy images and has high demand in scintillation process.

FRET Between Riboflavin and 9-Anthraldehyde Based Fluorescent Organic Nanoparticles Possessing Antibacterial Activity.

The aqueous suspension of fluorescent nanoparticles were prepared by using 9-anthradehdye derivative (AH). The nanoparticles (AHNPs) were characterized using DLS-zeta sizer and SEM techniques. The photo physical properties of nanoparticles and precursor were measured and compared using UV-absorption spectroscopy, fluorescence spectroscopy and fluorescence lifetime studies. The significant overlap between fluorescence spectrum of AHNPs and excitation spectrum of Riboflavin (RF) led us to explore Fluorescence Resonance Energy Transfer (FRET) studies between AHNPs and RF in aqueous medium. The mechanism of FRET from AHNPs to RF discussed on spectral observations, thermodynamic parameters and changes produces in fluorescence lifetime in absence and presence of different concentrations of RF to AHNPs. The limit of detection for RF (0.071 µM) is considerably low compared with reported methods. Thus, we explore AHNPs as novel nano probe for quantitative determination of RF in pharmaceutical samples based on FRET study. In addition with this, AHNPs has excellent antibacterial activity than the bulk material for two different bacteria culture viz. E. coli and Bacillus sps. Graphical Abstract 9-anthradehdye based fluorescent nanoparticles (AHNPs) explores as nano probe to detect Riboflavin (RF) in aqueous medium based on Fluorescence Resonance Energy Transfer (FRET) studies. The proposed analytical method successfully applied for quantitative determination of RF in pharmaceutical samples. In addition, with this, AHNPs has excellent antibacterial activity than the bulk material for two different bacteria culture suspension viz. E. coli and Bacillus sps.

Stereoselective HPLC separation of alvimopan on cellulose-based immobilized polysaccharide as a chiral stationary phase.

Chiral separation by normal phase high performance liquid chromatography is one of the most powerful technique to quantify the chiral purity of the compounds. In this study, a novel, simple, and specific analytical method was proposed to ascertain the chiral purity of alvimopan (ALV). The normal phase HPLC method was developed based on cellulose tris (3,5-dichlorophenylcarbamate) stationary phase. The separation of ALV isomers achieved by using column CHIRALPAK IC (250 × 4.6 mm, 5 µm), mobile phase n-hexane: isopropyl alcohol: ethanol: diethylamine (650:200:150:5 v/v), column oven temperature 30°C, flow rate 1.0 mL min-1 , injection volume was 10 µL, chromatographic response monitored at 273 nm. The developed method was validated as per the ICH guidelines and found precise, accurate, and linear. The advantage of the method is a good separation of ALV isomers within 35 minutes of the analysis time. Therefore, this method is suitable for routine determination of chiral purity of ALV active pharmaceutical ingredient.

Recognition of D-Penicillamine Using Schiff Base Centered Fluorescent Organic Nanoparticles and Application to Medicine Analysis.

Schiff base centered fluorescent organic compound 1,1'-[(1E,2E)-hydrazine-1,2-diylidenedi(E)methylylidene]- dinaphthalen-2-ol (HN) was synthesized followed by spectral characterization viz., NMR, IR and Mass spectroscopy. The fluorescent nanoparticles of HN prepared using reprecipitation method shows red shifted aggregation induced enhanced emission (AIEE) with respect to HN solution in acetone. The average particle size of nanoparticles (HNNPs) is of 67.2 nm shows sphere shape morphology. The surfactant cetyltrimethyl ammonium bromide (CTAB) used to stabilize HNNPs induces positive charge surface with zeta potential of 11.6 mV. The positive charge of HNNPs responsible to adsorb oppositely charged analyte on its surface with binding interactions. The fluorescence experiments performed with and without addition of different analytes to the aqueous suspension of HNNPs shows selective fluorescence quenching of HNNPs by D-Penicillamine (D-PA). The effect of other coexisting analytes does not affect the selective sensing behavior of D-PA. The mechanism of binding between HNNPs and D-PA was discussed on the basis of electrostatic interaction and adsorption phenomenon. The results interpreted by using DLS-Zeta sizer, Fluorescence lifetime measurements, conductometric titration supports the electrostatic adsorption between HNNPs and D-PA. The method has extremely low limit of detection (LOD) value 0.021 ppm is of significant as compared to reported methods. The proposed fluorescence quenching method was effectively used for quantitative estimation of D-PA from pharmaceutical medicine. Graphical Abstract The fluorescence quenching based selective recognition of D-Penicillamine (D-PA) by using Schiff base centered fluorescent organic nanoparticles was developed and successfully applied to quantitative determination of D-PA from pharmaceutical samples viz. capsule and tablet.

Fluorescence-based sensor for selective and sensitive detection of amoxicillin (Amox) in aqueous medium: Application to pharmaceutical and biomedical analysis.

We here for the first time demonstrate an analytical approach for the highly selective and sensitive detection of amoxicillin (Amox) in aqueous medium based on the fluorescence quenching of quantum dots (QDs). The change in fluorescence intensity of mercaptopropionic acid-capped cadmium sulphide (MPA-CdS) QDs is attributed to the increasing concentration of Amox. The results show that the fluorescence quenching of QDs by Amox takes place through both static and dynamic types of quenching mechanism. The fluorescence quenching of QDs with increase in concentration of Amox shows the linear range between 5 µg ml-1 and 30 µg ml-1 and the limit of detection (LOD) is 5.19 µg ml-1 . There is no interference of excipients, which are commonly present in pharmaceutical formulation and urine samples. For the practical application approach, the developed method has been successfully applied for the determination of Amox in pharmaceutical formulations and urine samples with acceptable results.

Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives.

Objective of the present work was to evaluate the anti-inflammatory, ulcerogenicity and cyclooxygenase activity of indenopyrimidine derivatives. Anti-inflammatory activity of the tested compounds is investigated by carrageenan-induced rat paw edema assay. Compounds A1, A6, A7 and A12 exhibit the comparable anti-inflammatory activity (79.33-81.33%) to the standard drug diclofenac sodium (85.33%), while A6, A7, A9, A12 and A14 show better ulcer index than the reference standard diclofenac sodium. To rationalize the anti-inflammatory activity, docking experiments are performed to study the ability of these compounds to bind into the active site of COX-2 enzyme.