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Published: 1 January 2012
Journal: BMC Chemistry
BMC Chemistry, Volume 2, pp 23-23; https://doi.org/10.1186/2191-2858-2-23

Abstract:
Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. IC50 values of the synthesized compounds against the proliferation of human hepatocellular carcinoma and human epithelial carcinoma cell lines were determined through MTT assay. Molecular docking study gave a clear insight into the structural activity relationship of the compounds in comparison with monastrol.
Mandira Banik, , , , Bimal K Banik
Published: 1 January 2012
Journal: BMC Chemistry
BMC Chemistry, Volume 2, pp 11-11; https://doi.org/10.1186/2191-2858-2-11

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Published: 10 October 2013
Journal: BMC Chemistry
BMC Chemistry, Volume 7, pp 166-166; https://doi.org/10.1186/1752-153x-7-166

Abstract:
Background: Over the past decades, the economic development and world population growth has led to increased for food demand. Increasing the fish production is considered one of the alternatives to meet the increased food demand, but the processing of fish leads to by-products such as skin, bones and viscera, a source of environmental contamination. Fish viscera have been reported as an important source of digestive proteases with interesting characteristics for biotechnological processes. Thus, the aim of this study was to purify and to characterize a trypsin from the processing by-products of crevalle jack (Caranx hippos) fish. Results: A 27.5 kDa trypsin with N-terminal amino acid sequence IVGGFECTPHVFAYQ was easily purified from the pyloric caeca of the crevalle jack. Its physicochemical and kinetic properties were evaluated using N-α-benzoyl-DL-arginine-p-nitroanilide (BApNA) as substrate. In addition, the effects of various metal ions and specific protease inhibitors on trypsin activity were determined. Optimum pH and temperature were 8.0 and 50°C, respectively. After incubation at 50°C for 30 min the enzyme lost only 20% of its activity. Km, kcat, and kcat/Km values using BApNA as substrate were 0.689 mM, 6.9 s-1, and 10 s-1 mM-1, respectively. High inhibition of trypsin activity was observed after incubation with Cd2+, Al3+, Zn2+, Cu2+, Pb2+, and Hg2+ at 1 mM, revealing high sensitivity of the enzyme to metal ions. Conclusions: Extraction of a thermostable trypsin from by-products of the fishery industry confirms the potential of these materials as an alternative source of these biomolecules. Furthermore, the results suggest that this trypsin-like enzyme presents interesting biotechnological properties for industrial applications.
Published: 2 December 2014
Journal: BMC Chemistry
BMC Chemistry, Volume 4, pp 1-4; https://doi.org/10.1186/s13588-014-0013-y

Abstract:
Background: Macrotyloma uniflorum Linn (Fabaceae) is a herbaceous plant with annual branches. It is used in kidney stones, inflamed joints, fever, musculoskeletal disorders, sinus wounds and localized abdominal tumors. It is reported as an antioxidant and nutraceutical (forage and food). GC-MS analysis of ethanol extract has led to identification of twenty-eight compounds from M. uniflorum by comparison of their retention indices and mass spectra fragmentation patterns with those stored on the GC-MS computer library. Results: The main constituents identified were mome inositol, ethyl alpha-d-glucopyranoside, n- hexadecanoic acid, linoleic acid (9, 12-octadecadienoic acid), its esters and ethyl derivatives, Vitamin E, stigmasterol and 3-beta-stigmast-5-en-3-ol. Conclusions: The extracts are rich in linoleic acid and its esters, mome inositol and ethyl alpha-d-glucopyranoside; therefore, this plant can be medicinally beneficial as an antioxidant, in diabetes and its related disorders.
Published: 2 December 2014
Journal: BMC Chemistry
BMC Chemistry, Volume 4, pp 1-4; https://doi.org/10.1186/s13588-014-0014-x

Abstract:
Background: Benzimidazoles and triazoles are useful structures for research and development of new pharmaceutical molecules and have received much attention in the last decade because of their highly potent medicinal activities. Findings: A simple and efficient synthesis of triazole was carried out by treatment of 2-(4-azidophenyl)-1H-benzo[d]imidazole (6) with different types of terminal alkynes in t-BuOH/H2O, sodium ascorbate, and Zn(OTf)2, screened for cytotoxicity assay and achieved good results. A series of new benzimidazole-linked 1,2,3-triazole (8a-i) congeners were synthesized through cyclization of terminal alkynes and azide. These synthesized congeners 8a-i were evaluated for their cytotoxicity against five human cancer cell lines. These benzimidazole-linked 1,2,3-triazole derivatives have shown promising activity with IC50 values ranging from 0.1 to 43 μM. Among them, the compounds (8a, 8b, 8c, and 8e) showed comparable cytotoxicity with adriamycin control drug. Conclusions: In conclusion, we have developed a simple, convenient, and an efficient convergent approach for the synthesis of benzimidazole-linked 1,2,3-triazole congeners as agents.
Published: 20 September 2014
Journal: BMC Chemistry
BMC Chemistry, Volume 4, pp 8-8; https://doi.org/10.1186/s13588-014-0008-8

Abstract:
Background: The current investigation sought to explore the nature of the secondary metabolites in the algae, Laurencia pacifica. Results: This report details the first isolation of the sesquiterpenes isoaplysin (1), isolaurenisol (2), debromoisolaurinterol (3), debromoaplysinol (4), laur-11-en-10-ol (5), 10α-hydroxyldebromoepiaplysin (6), and the previously unknown 10-bromo-3,7,11,11-tetramethylspiro[5.5]undeca-1,7-dien-3-ol (7) from the algae, Laurencia pacifica. Isoaplysin (1) and debromoaplysinol (4) showed promising levels of growth inhibition against a panel cancer-derived cell lines of colon (HT29), glioblastoma (U87, SJ-G2), breast (MCF-7), ovarian (A2780), lung (H460), skin (A431), prostate (Du145), neuroblastoma (BE2-C), pancreas (MIA), murine glioblastoma (SMA) origin with average GI50 values of 23 and 14 μM. Conclusions: Isoaplysin (1) and debromoaplysinol (4) were up to fourfold more potent in cancer-derived cell populations than in non-tumor-derived normal cells (MCF10A). These analogues are promising candidates for anticancer drug development.
Published: 27 June 2014
Journal: BMC Chemistry
BMC Chemistry, Volume 4, pp 1-4; https://doi.org/10.1186/s13588-014-0004-z

Abstract:
Background: The aim of this study was to evaluate the effects of nitroxin biofertilizer and chemical fertilizer on the growth, yield, and essential oil composition of dill. The experiment was conducted under field condition in randomized complete block design with three replications and two factors. Results: The first factor was the concentrations of nitroxin biofertilizer (0%, 50%, and 100%) of the recommended amount (1 l of biological fertilizer for 30 kg of seed). The second factor was the following chemical fertilizer treatments: no fertilizer (control) and 50 and 100 kg ha−1 urea along with 300 kg ha−1 ammonium phosphate. Different characteristics such as plant height, number of umbel per plant, number of umbellet per umbel, number of grain per umbellet, 1,000 seed weight, grain yield, biological yield, and oil percentage were recorded. According to the results, the highest height, biological yield, and grain yield components (except harvest index) were obtained on biological fertilizer. The results showed the highest essential oil content detected in biological fertilizer and chemical fertilizer. Identification of essential oil composition showed that the content of carvone increased with the application of biofertilizers and chemical fertilizers. The results indicated that the application of biofertilizers enhanced yield and other plant criteria in this plant. Conclusions: Generally, it seems that the use of biofertilizers or combinations of biofertilizer and chemical fertilizer could improve dill performance in addition to reduction of environmental pollution.
, Maha O. A. Omar, Magda E. Mahmoud
Published: 1 February 2023
Journal: BMC Chemistry
BMC Chemistry, Volume 17, pp 1-14; https://doi.org/10.1186/s13065-023-00911-8

Abstract:
Converting seed coat peas (hulls) (SCP) into beneficial products provides a solution for waste treatment. This study aimed to investigate the phytoconstituents and biological activities of SCP extract. Phytochemical screening, total bioactive compounds, and GC–MS analysis were evaluated. Then, the antioxidant, antibacterial, anticancer, and antiviral activities of SCP extract were determined. The results demonstrate that SCP extract has bioactive compounds such as carbohydrates (29.53 ± 4.23 mg/mL), protein (0.24 ± 0.02 mg/mL), phenolics (27.04 ± 0.94 mg GAE/g extract), and flavonoids (17.19 ± 0.48 mg QE/g extract). The existence of more than 16 substances was determined using GC–MS analysis. The extract showed potential antioxidant activities, with the maximum activity seen for extract (IC50 µg/mL) = 79.16 ± 1.77 for DPPH, 67.40 ± 5.20 for ORAC, and 61.22 ± 4.81 for ABTS assays. The SCP extract showed potent antimicrobial activity against four gram-positive bacteria (Bacillus cereus, Streptomyces sp., Staphylococcus aureus, and Salmonella sp.) and two gram-negative bacteria (Escherichia coli and Pseudomonas sp.). SCP extract exhibited potential anticancer activity against lymphoma U937 and leukemic cells (THP1). The extract exhibited potential antiviral activity, with a selectivity index (SI) equal to 11.30 and 18.40 against herpes simplex-II (HSV-2) and adenovirus (Ad7), respectively. The results demonstrate more accurate information about peas by-products' chemical and antioxidant activities in various applications. The chemical components of peas by-products were found to have an in vitro antioxidant, antibacterial, and antiviral activity against leukemia and lymphoma.
, Ahmed M. Wafaa Nassar, Gamal A. Omran, Samir Morshedy,
Published: 18 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-10; https://doi.org/10.1186/s13065-022-00906-x

Abstract:
Desmopressin acetate (DPA) is a synthetic analogue of vasopressin used in the treatment of diabetes insipidus, bedwetting, hemophilia A, and elevated levels of urea in the blood. Sensitive and selective stability-indicating methods are needed to be developed and validated for its assay pure and pharmaceutical dosage forms in the presence of its degradation products as no method has been reported for its determination in the presence of its degradants. This work describes a comparative study of five simple stability-indicating spectrophotometric techniques for determination of DPA in presence of its acid-degradation products (acid-degradants) without prior separation. The proposed spectrophotometric techniques (First derivative, Derivative ratio, Ratio difference, Mean centering and Dual wavelength) were developed and validated according to ICH guidelines. Acid degradation was carried out with 0.1 N HCl; the acid-degradants were separated on TLC plates and the acidic degradation pathway was established by IR, H-NMR and MS techniques. The TLC method was based on the separation of DPA and its acid-induced degradation products on silica gel plates using methanol: water (80:20, v/v) as a developing system and UV detection at 254 nm. All assay suggested methods were successfully applied for quantitation of DPA in pure and tablet forms. They are specific, sensitive, precise and accurate. They showed good linearity in the concentration range of 1–14 µg/mL with good correlation coefficients, and limit of detection (LOD) of 0.304, 0.274, 0.167, 0.248 and 0.199 and limit of quantitation (LOQ) of 0.920, 0.829, 0.506, 0.751 and 0.604) for each method, respectively. These methods were successfully applied for the simultaneous determination of DPA in its pure and tablet dosage form in the presence of its acid-degradants. The results obtained were statistically comparable with those of reported HPLC assay method; no significant differences were observed with relevance to accuracy and precision. All the methods are sensitive, selective and can be used for the routine analysis of DPA in its pure and dosage forms.
Published: 15 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-7; https://doi.org/10.1186/s13065-022-00910-1

Abstract:
The discoveries recommend that the photoinduced conditions of fluorescein-determined go about as impetus for photochemically combining polysubstituted quinolines in ethanol at room temperature under air environment by means of revolutionary Friedländer hetero-annulation of 2-aminoaryl ketone and α-methylene carbonyl compound. This study lays out an original capability for photochemically orchestrating fluorescein. This non-metallic organic dye is economically accessible and modest, producing great outcomes, accelerating the cycle, and achieving a high compound economy. The turnover number (TON) and turnover recurrence (TOF) of polysubstituted quinolines have been determined. This cycle will likewise run on a gram scale, demonstrating the chance of modern applications.
Ebrahim Nabatian, Mahdi Mousavi, Mostafa Pournamdari, ,
Published: 12 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-12; https://doi.org/10.1186/s13065-022-00905-y

Abstract:
A simple and precise analytical approach developed for single and simultaneous determination of resorcinol (RC) and hydroquinone (HQ) in pharmaceutical samples using carbon paste electrode (CPE) modified with 1-Ethyl-3-methylimidazolium tetrafluoroborate as ionic liquid and ZnFe2O4 nanoparticle. A significant enhancement in the peak current and sensitivity of the proposed sensor observed by using modifiers in the composition of working electrode compared to bare CPE which is in accordance with the results obtained from electrochemical impedance spectroscopy investigations. Electrochemical investigations revealed a well-defined irreversible oxidation peak for RC over a wide concentration range from 3.0 µM to 500 µM in 0.1 M phosphate buffer solution (pH 6.0) with the linear regression equations of Ip (µA) = 0.0276 CRC (µM) + 0.5508 (R2 = 0.997). The limit of detection and quantification for RC analysis were found to be 1.46 µM and 4.88 µM, respectively. However, the obtained SW voltammograms for simultaneous determination of RC and HQ exhibited a desirable peak separation of about 360 mV potential difference and a satisfactory linear response over the range of 50–700 µM and 5-350 µM with the favorable correlation coefficient of 0.991 and 0.995, respectively. The diffusion coefficient (D) of RC and the electron transfer coefficient (α) at the surface of ZnFe2O4/NPs/IL/CPE estimated to be 2.83 × 10− 4 cm s− 1 and 0.76. The proposed sensor as a promising and low-cost method successfully applied for determination of RC in commercial pharmaceutical formulations such as the resorcinol cream of 2% O/W emulsion available on the market with the recovery of 98.47 ± 0.04.
Hebat-Allah S. Tohamy, , Hossam M. El-Masry, Ibrahim A. Saleh, Mona M. AbdelMohsen
Published: 12 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-7; https://doi.org/10.1186/s13065-022-00907-w

Abstract:
In this study, we have used hydroxyethyl cellulose (HEC) to prepare antimicrobial films for multipurpose applications. Using HEC gives mangiferin powder (M) mechanical properties, while mangiferin powder gives HEC antimicrobial activities. Various concentrations of M (2.5, 5 and 10% wt/vol) were added to HEC to enhance the antimicrobial ability of HEC/M films. The results showed that 10% (wt/vol) was the optimum concentration to accomplish the antimicrobial activity. Various analyses were performed to study the prepared films’ physical, chemical, mechanical, and antimicrobial properties.
Ehab F. Elkady, , Ayoub N. Mozayad
Published: 12 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-15; https://doi.org/10.1186/s13065-022-00908-9

Abstract:
An isocratic RP-HPLC method has been developed for the separation and determination of methocarbamol (MTL), indomethacin (IND), and betamethasone (BET) in combined dosage form using an Inertsil ODS-3v C18 (250 × 4.6 mm, 5 μm) column with UV- detection at 235 nm. Experimental design using Box-Behnken design (BBD) was applied to study the response surface during method optimization and to achieve a good separation with a minimum number of experimental runs. The three independent parameters were pH of buffer, % of acetonitrile and flow rate of the mobile phase while the peak resolution of IND from MTL and the peak resolution of BET from IND (R2) were taken as responses to obtain mathematical models. The composite desirability was employed to optimize a set of responses overall (peak resolutions). The predicted optimum assay conditions include a mobile phase composition of acetonitrile and phosphate buffer (pH 5.95) in a ratio of 79:21, v/v, pumped at a flow rate of 1.4 mL min−1. With this ideal condition, the optimized method was able to achieve baseline separation of the three drugs with good resolution and a total run time of less than 7 min. The linearity of MTL, IND, and BET was determined in the concentration ranges of 5–600 µg mL− 1, 5–300 µg mL− 1, and 5–300 µg mL− 1 and the regression coefficients were 0.9994, 0.9998, and 0.9998, respectively. The average percent recoveries for the accuracy were determined to be 100.41 ± 0.60%, 100.86 ± 0.86%, and 100.99 ± 0.65% for MTL, IND, and BET, respectively. The R.S.D.% of the intra-day precision was found to be less than 1%, while the R.S.D.% of the inter-day precision was found to be less than 2%. The RP-HPLC method was fully validated with regard to linearity, accuracy, precision, specificity, and robustness as per ICH recommendations. The proposed method has various applications in quality control and routine analysis of the investigated drugs in their pharmaceutical dosage forms and laboratory-prepared mixtures with the goal of reducing laboratory waste, analysis time, and effort.
, Mohamed R. Elgindi, Enas M. Shawky, Haitham A. Ibrahim
Published: 10 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-9; https://doi.org/10.1186/s13065-022-00909-8

Abstract:
Ludwigia adscendens subsp. diffusa (Onagraceae), an important aquatic herb widely distributed in the Nile River and canals in Egypt. The goal of the current study is to investigate the phytochemical composition of L. adscendens aerial parts n-butanol and ethyl acetate fractions and screening of its biological activities. Phytochemical investigation of L. adscendens resulted in the isolation and purification of eleven compounds belonging to flavonoids, saponins, triterpenoids, and oligosaccharides, of which one compound was identified as new using different spectroscopic techniques. Compound 2 was identified as a new compound namely, 3-O-[β-D-glucopyranoside (1 → 4) α-L-rhamnopyranoside]-23-O-feruloyl-hederagenin-28-O-[α-L-rhamnopyranoside (1 → 2) β-D-glucopyranoside], along with other 10 well know compounds. Furthermore, antidiabetic, hepatoprotective and cytotoxic activities of n-butanol and ethyl acetate fractions were investigated in vitro, revealing that ethyl acetate fraction was the most active as antidiabetic (IC50 = 62.3 µg/mL), hepatoprotective (IC50 = 80.75 µg/mL), and cytotoxic against human prostate cancer cell line (IC50 = 52.2 µg/mL). Collectively, L. adscendens aerial part is rich with a myriad of phytochemicals with potential health benefits.
Muhammad Shoaib Ali Gill, Nursyuhada Azzman, Sharifah Syed Hassan, Syed Adnan Ali Shah,
Published: 8 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-9; https://doi.org/10.1186/s13065-022-00902-1

Abstract:
Quinolone is a privileged scaffold in medicinal chemistry and 4-Quinolone-3-Carboxamides have been reported to harbor vast therapeutic potential. However, conversion of N-1 substituted 4-Quinolone 3-Carboxylate to its corresponding carbamates is highly restrictive. This motivated us to adopt a much simpler, scalable and efficient methodology for the synthesis of highly pure N-1 substituted 4- Quinolone-3-Carboxamides with excellent yields. Our adopted methodology not only provides a robust pathway for the convenient synthesis of N-1 substituted 4- Quinolone-3-Carboxamides which can then be explored for their therapeutic potential, this may also be adaptable for the derivatization of other such less reactive carboxylate species.
Maryam Asariha, , Sepideh Izadi, Faezeh H. Pirhayati, Mehdi Fouladi, Maryam Gholamhosseinpour
Published: 6 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-10; https://doi.org/10.1186/s13065-022-00895-x

Abstract:
In the present study, a green surface modification of gold nanoparticles (GNPs) using chondroitin sulfate (CHS) and chitosan (CS) to deliver an extended-release of doxorubicin (DOX) was proposed. Following synthesis of each step of unconjugated counterpart, including CHS-GNPs, DOX–CHS–GNP, and conjugated construct DOX–CHS–GNP-CS, physicochemical properties of the nanoparticles (NPs) were characterized by FT-IR, DLS, and TEM analyses, and the release of DOX was determined by using UV–Vis spectrometry. Then, NPs were effectively taken up by MDA-MB-468, βTC-3, and human fibroblast (HFb) cell lines with high release percent and without significant cytotoxicity. The DOX–CHS–GNPs and DOX–CHS–GNP-CS NPs showed a mean size of 175.8 ± 1.94 and 208.9 ± 2.08 nm; furthermore, a zeta potential of − 34 ± 5.6 and − 25.7 ± 5.9 mV, respectively. The highest release of DOX was 73.37% after 45 h, while in the absence of CS, the release of DOX was 76.05% for 24 h. Compared to CHS-GNPs, the presence of CS decreased the rate of sustained release of DOX and improved the drug release efficiency. The results demonstrated an excellent release and negligible cytotoxicity at high concentrations of CHS-GNP-CS. Consequently, in ovo assessment corroborated the efficacy of the green fabricated NPs proposed effective targeted delivery of DOX for anti-tumor therapy in vitro. Graphical Abstract
Mona A. Abdel Rahman, Mohamed R. Elghobashy, Hala E. Zaazaa, Shimaa A. Atty,
Published: 2 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-11; https://doi.org/10.1186/s13065-022-00904-z

Abstract:
Etoricoxib (ETO), Paracetamol (PCM), and two toxic impurities for Paracetamol impurity K (4-aminophenol (PAP)) and impurity E (para-hydroxy acetophenone (PHA)) were separated using a simple and selective HPLC method that was tested for the first time. PCM is a commonly used analgesic and antipyretic medication that has recently been incorporated into COVID-19 supportive treatment. Pharmaceuticals containing PCM in combination with other analgesic-antipyretic drugs like ETO help to improve patient compliance. The studied drugs and impurities were separated on a GL Sciences Inertsil ODS-3 (250 × 4.6) mm, 5.0 µm column, and linear gradient elution was performed using 50 mM potassium dihydrogen phosphate adjusted to pH 4.0 with ortho-phosphoric acid and acetonitrile as mobile phase at 2.0 mL/min flow rate at 25 °C and UV detection at 220 nm. The linearity range was 1.5–30.0 µg/mL for ETO and PCM while 0.5–10.0 µg/mL for PAP and PHA, with correlation coefficients (r) for ETO, PCM, PAP, and PHA of 0.9999, 0.9993, 0.9996, and 0.9998, respectively. The proposed method could be used well for routine analysis in quality control laboratory.
Mbang I. Ofem, , , , Gloria C. Apebende, Terkumbur E. Gber, Joseph O. Odey, Neksumi Musa,
Published: 3 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-15; https://doi.org/10.1186/s13065-022-00896-w

Abstract:
This research work focuses on the synthesis, characterization through spectra (FT-IR, UV–vis, and 1H-NMR) investigations, and the use of density functional theory (DFT) along with time-dependent density functional theory (TD-DFT) to investigate the electronic, structural, reactivity, photophysical properties, and the photovoltaic properties of a novel (E)-6-(4-(dimethylamino)phenyl)diazenyl)-2-octyl-benzoisoquinoline-1,3-dione. The structure of the synthesized compound was modeled using the Gaussian09W and GaussView6.0.16 softwares employing B3LYP and 6–31 + G(d) basis set. The DFT studies was performed in order to investigate the Frontier Molecular Orbital (FMO), Natural Bond Orbital (NBO), charge distribution, Nonlinear Optics (NLO), and stability of the titled molecule. The HOMO–LUMO energy gap which corresponds to the difference between HOMO and LUMO energies of the studied compound was found to be 2.806 eV indicating stiff and smooth nature of the titled molecule. This accounts for the less stability and high chemical reactivity of the compound. The photovoltaic properties were conducted to evaluate the light harvesting efficiency (LHE), short circuit current density (JSC), Gibbs free energy of injection ( $$\Delta {G}_{inj}$$ΔGinj ), open cycled voltage (VOC) and Gibbs free energy regeneration ( $$\Delta {G}_{reg}$$ΔGreg ) and solar cell conversion efficiency. Interestingly, the results obtained were found to be in good agreement with other experimental and computational findings.
Girma Worku Seifu, , Botros Youssef Beshay, Ariaya Hymete,
Published: 2 December 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-12; https://doi.org/10.1186/s13065-022-00903-0

Abstract:
Quinazolinones are a diverse group of nitrogen-containing heterocyclic compounds with promising antimalarial and antileishmanial activities. Herein, some 3-aryl-2-styryl substituted-4(3H)-quinazolinones were synthesized via cyclization, condensation, and hydrolysis reactions. 1H NMR, FTIR and elemental microanalysis was used to verify the structures of the synthesized compounds. The in vivo antimalarial and in vitro antileishmanial activities of the target compounds were investigated using mice infected with Plasmodium berghi ANKA and Leishmania donovani strain, respectively. Among the test compounds, 8 and 10 showed better antimalarial activities with percent suppression of 70.01 and 74.18, respectively. In addition, (E)-2-(4-nitrostyryl)-3-phenylquinazolin-4(3H)-one (6) showed promising antileishmanial activity (IC50 = 0.0212 µg/mL). It is two and 150 times more active than the standard drugs amphotericin B deoxycholate (IC50 = 0.0460 µg/mL) and miltefosine (IC 50 = 3.1911 µg/mL), respectively. Its superior in vitro antileishmanial activity was supported by a molecular docking study conducted in the active site of Lm-PTR1. Overall, the synthesized 3-aryl-2-styryl substituted-4(3H)-quinazolinones showed promising antileishmanial and antimalarial activities and are desirable scaffolds for the synthesis of different antileishmanial and antimalarial agents.
Arezoo Rastegari, Azadeh Manayi, Mahdi Rezakazemi, Mahdieh Eftekhari, Mahnaz Khanavi, Tahmineh Akbarzadeh,
Published: 28 November 2022
Journal: BMC Chemistry
BMC Chemistry, Volume 16, pp 1-9; https://doi.org/10.1186/s13065-022-00897-9

Abstract:
In this study, the ethyl acetate fraction of Myristica fragrans Houtt. was investigated for its in vitro anticholinesterase activity as well as neuroprotectivity against H2O2-induced cell death in PC12 neuronal cells and the ability to chelate bio-metals (Zn2+, Fe2+, and Cu2+). The fraction was inactive toward acetylcholinesterase (AChE); however, it inhibited the butyrylcholinesterase (BChE) with IC50 value of 68.16 µg/mL, compared with donepezil as the reference drug (IC50 = 1.97 µg/mL) via Ellman’s method. It also showed good percentage of neuroprotection (86.28% at 100 µg/mL) against H2O2-induced neurotoxicity and moderate metal chelating ability toward Zn2+, Fe2+, and Cu2+. The phytochemical study led to isolation and identification of malabaricone A (1), malabaricone C (2), 4-(4-(3,4-dimethoxyphenyl)-2,3-dimethylbutyl)benzene-1,2-diol (3), nectandrin B (4), macelignan (5), and 4-(4-(benzo[d][1,3]dioxol-5-yl)-1-methoxy-2,3-dimethylbutyl)-2-methoxyphenol (6) which were assayed for their cholinesterase (ChE) inhibitory activity. Compounds 1 and 3 were not previously reported for M. fragrans. Among isolated compounds, compound 2 showed the best activity toward both AChE and BChE with IC50 values of 25.02 and 22.36 μM, respectively, compared with donepezil (0.07 and 4.73 μM, respectively).
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