S. Mor, S. Sindhu, M. Khatri, Ravi Punia, K. Jakhar
{"title":"Synthesis, Type II diabetes inhibitory activity, antimicrobial evaluation, and docking studies of N'-arylidene-2-((7-methylbenzo[4,5]thiazolo[2,3-c] [1,2,4]triazol-3-yl)thio)acetohydrazides","authors":"S. Mor, S. Sindhu, M. Khatri, Ravi Punia, K. Jakhar","doi":"10.5155/eurjchem.13.4.426-434.2315","DOIUrl":"https://doi.org/10.5155/eurjchem.13.4.426-434.2315","url":null,"abstract":"N'-Arylidene-2-((7-methylbenzo[4, 5]thiazolo[2,3-c][1, 2, 4]triazol-3-yl)thio)acetohydrazides (6a-j) were prepared by condensation of 2-((7-methylbenzo[4,5]thiazolo[2,3-c][1,2,4] triazol-3-yl)thio)acetohydrazide with appropriately substituted benzaldehydes in dry methanol and a catalytic amount of glacial acetic acid. The prepared compounds tested for in vitro Type II diabetes inhibition and antimicrobial (antibacterial and antifungal) activities employing α-amylase inhibition assay and the serial dilution method, respectively. Type II diabetes inhibitory assay results of all the tested derivatives revealed that precursor 3 (IC50 = 0.16 μM) and acetohydrazide 6i (IC50 = 0.38 μM) showed comparable activity with standard drug acarbose (IC50 = 0.15 μM). The derivatives 6i against B. subtilis and E. coli with MIC values of 0.0300 μmol/mL, compound 6c against S. aureus (MIC = 0.0312 μmol/mL) and compound 6e against P. aeruginosa (MIC = 0.0316 μmol/mL) exhibited remarkable antibacterial activity, however, compound 6b was found to be more active against the fungal strain C. albicans with MIC value of 0.0135 μmol/mL. All acetohydrazides (6a-j) showed greater potency against all strains tested than their precursors 1-4, which is also supported by the results of molecular docking analysis. Furthermore, no general trend for structure activity relationships was established for Type II diabetes inhibitory activity, nor antimicrobial activities of the tested hydrazones (6a-j).","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49254506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The effect of different molecular weight chitosan on the physical and mechanical properties of plasticized films","authors":"S. Mutasher, H. Al-Lami","doi":"10.5155/eurjchem.13.4.460-467.2341","DOIUrl":"https://doi.org/10.5155/eurjchem.13.4.460-467.2341","url":null,"abstract":"Packaging materials based on biodegradable polymers are a viable alternative to replacing conventional plastic packaging of fossil origin. The main two factors affecting functionality and performance are the molecular weight and the type of plasticizer used in these materials. The goal of this research was to modify unfractionated plasticized chitosan films to improve the physical and mechanical characteristics of the original unfractionated chitosan films. Chitosan extracted from local shrimp shells was zone-refined to produce five distinct chitosan fractions with molecular weights ranging from 1.089×105 to 5.605×105 g/mole. The unfractionated and fractionated chitosan films plasticized with 1:3 poly(vinyl alcohol) and 2:1 maleic acid were prepared by casting from their 2% acetic acid solutions. They were examined by FT-IR and were found to be comparable to the native chitosan spectrum, indicating that the primary backbone of the chitosan structure was unaltered. Therefore, the effects of molecular weight fractions and the type of plasticizer on the physical and mechanical properties were investigated. Examining the films’ surface topography by atomic force microscopy revealed that increasing the molecular weight of chitosan fractions from 2.702×105 to 5.605×105 g/mole affects the surface morphology of the chitosan: poly(vinyl alcohol) (1:3) film. This was accompanied by an increase in the surface roughness of the resulting film from 0.953 to 2.82, and for chitosan: maleic acid from 0.509 to 1.62. It was found that the tensile strength and Young’s modulus of the cast films decreased and the percent elongation at break of the plasticized fractionated chitosan films was increased, implying that less stiff films were obtained with fractionated chitosan. The outcome of this work suggests that the biodegradable fractionated chitosan blend film is a promising packaging material and that poly(vinyl alcohol) is the most suitable plasticizer for this formulation.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47569235","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S. Pathak, S. Shukla, Bharat Patel, S. Tripathi, A. Pandey
{"title":"Alendronate functionalized PLGA based nanoparticles for the effective treatment of osteoporosis-Formulation to in-vitro release kinetic studies","authors":"S. Pathak, S. Shukla, Bharat Patel, S. Tripathi, A. Pandey","doi":"10.5155/eurjchem.13.4.407-414.2246","DOIUrl":"https://doi.org/10.5155/eurjchem.13.4.407-414.2246","url":null,"abstract":"Osteoporosis is a bone disease caused due to the reducing bone mineral density. Porous and more fragile bones increase the risk of fractures. Hip, spine, shoulder, and wrist bones are commonly affected by osteoporosis. Low bone density is a leading cause of osteoporosis. The most efficient prescribed drugs for the treatment of osteoporosis are bisphosphonates drugs. Alendronate was the first FDA approved bisphosphonate drug for the treatment of osteoporosis. Osteoclast cells are the primary targeting site for alendronate, responsible for bone resorption. A biopharmaceutical classification system class III bisphosphonate acts as a potent, efficient, and bone resorption inhibitor drug. In the present study, alendronate functionalized PLGA based nanoparticles were developed by a solvent diffusion method and optimized for different process variables. The formulated nanoparticles were characterized for surface morphology, particle size distribution, surface charge and drug-polymer compatibility. The scanning electron microscopy and transmission electron microscopy results showed nanoparticle size in the range below 200 nm. The average particle size and zeta potential of the formulated nanoparticles were found to be 175.3 nm and -13.98 mV, respectively. The highest encapsulation efficiency was 65.23%. The release profile was dissolution medium dependent and followed by the Higuchi model of release kinetics.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49396185","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"The crystal magnification, characterization, X-ray single crystal structure, thermal behavior, and computational studies of the 2,4,6-trimethylpyridinium picrate","authors":"N. B. Arslan, F. Aydın","doi":"10.5155/eurjchem.13.4.468-477.2349","DOIUrl":"https://doi.org/10.5155/eurjchem.13.4.468-477.2349","url":null,"abstract":"A crystal of organic salt, 2,4,6-trimethylpyridinium picrate (TMPPc), was synthesized and magnified by slow evaporation in a polar aprotic solvent and characterized by 1H NMR, 13C NMR, and FT-IR spectroscopic methods. X-ray diffraction analysis of the crystal structure of the compound TMPPc showed the presence of a monoclinic space group with a = 4.0174(4) Å, b = 27.863(3) Å, c = 13.9247(17) Å, β = 95.741(4)°, V = 1550.9(3) Å3, Z = 4, T = 296 K, μ(MoKα) = 0.123 mm-1, Dcalc = 1.500 g/cm3, 62749 reflections measured (5.88° ≤ 2Θ ≤ 57.058°), 3911 unique (Rint = 0.0536, Rsigma = 0.0226) which were used in all calculations. The final R1 was 0.0569 (I > 2σ(I)) and wR2 was 0.1710 (all data). Detailed investigation of molecular packing of the TMPPc molecule indicated the presence of intermolecular hydrogen bond between N4-H44···O1 and C13-H13B···O4 that generates C22(14) chain running parallel to the [001] direction. The infrared and Raman spectra of the prepared TMPPc compound were recorded and discussed. The thermal stability of the obtained TMPPc crystal was analysed by TGA/DTG technique and revealed that the crystal was stable up to 162 °C. Density functional theory calculations such as the value of the HOMO and LUMO energy gap, the parameters of the molecular electrostatic potential, the global reactivity and thermodynamic properties of the compound TMPPc were also performed using the DFT/B3LYP method with the level of the 6-311G (d, p) basis set.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42530119","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sylla Tahiri, M’bra Kouassi Fulgence, Dongui Bini Kouame
{"title":"Phytochemical analysis, investigation of antioxidant and anti-inflammatory activities of ethanolic and aqueous extracts of roots of Combretum glutinosum Perr. ex DC from Cote d'Ivoire","authors":"Sylla Tahiri, M’bra Kouassi Fulgence, Dongui Bini Kouame","doi":"10.5155/eurjchem.13.4.478-482.2352","DOIUrl":"https://doi.org/10.5155/eurjchem.13.4.478-482.2352","url":null,"abstract":"The phytochemical, antioxidant, and anti-inflammatory potential of root (ethanol and aqueous) extracts of Combretum glutinosum was investigated in this study. Their antioxidant activity was determined using an in vitro DPPH radical scavenging activity assay. The ethanol extract had the lowest IC50 (0.055 mg/mL), which is comparable to vitamin C. Phytochemical screening of extracts revealed the presence of sterols and polyterpenes, polyphenols, alkaloids, flavonoids, catechin tannins, gallic tannins, saponosides, terpenoids, mucilages, anthocyanins, volatile oils, and cardiac glycosides. The extracts significantly inhibit the development of paw edema induced by carrageenan. Anti-inflammatory studies showed that the inflammation inhibition potential of 200 mg/kg body weight of all extracts was significantly lower than the standard diclofenac (20 mg/kg) in the first hours. At the third hour, the inflammation inhibition potential of ethanolic and aqueous extracts was significantly higher than that of the standard. This study revealed that Combretum glutinosum extracts have anti-inflammatory effects and can act as an effective antioxidant.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47077967","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Crystal and molecular structure of Michler’s ketone as a pure phase","authors":"I. O. Shotonwa, R. Boere","doi":"10.5155/eurjchem.13.4.435-439.2327","DOIUrl":"https://doi.org/10.5155/eurjchem.13.4.435-439.2327","url":null,"abstract":"The pure phase crystals of Michler’s ketone, [4-(CH3)2NC6H4]2CO, are reported herein as monoclinic in the space group P21/c with Z’ = 2 by single-crystal X-ray diffraction. The data collection of the title compound proved quite difficult, which could explain why the structure has not been reported previously. The crystallographically independent molecules in the asymmetric unit differ by dihedral angles of 24.60/30.34° and 25.25/27.20° between the essentially planar 4-dimethylaminophenyl (DMAP) rings and the central C2C=O plane of the ketone and dihedral angles of 52.14 and 47.41°, respectively, between the DMAP planes. A DMAP ring of each molecule overlaps in the lattice with a methyl ring that overlays the ring centroid of the opposite number (CMe-Cg distances of 3.452 and 3.505 Å), describing sets of trifurcated CAr-acceptor hydrogen bond interactions (HBIs). The trifurcated HBIs possess H∙∙∙CAr distances of 2.90, 2.75, and 2.86 Å; CMe∙∙∙Car distances of 3.554(5), 3.798(5) and 3.881(5) Å; and ÐCMe-H∙∙∙CAr of 115.0, 121.3 and 167.7°, respectively. Stabilization of the asymmetric unit in the title compound is further achieved by supramolecular synthons such as CMe-H∙∙∙CAr (2.831 Å), CAr-H∙∙∙O (2.561 Å) and CAr-H∙∙∙H-CAr (2.290 Å) and coulombic CMe-Ocontact (3.209 Å). The structures of the two independent molecules in the asymmetric unit of the title compound were compared with the same molecule as found in the following co-crystals, adducts or salts: a halogen-bonded adduct with 1,4-diiodotetrafluorobenzene; a hydrogen-bonded adduct with a fluorinated phenol; a coordination complex between the ketone and a trimeric mercury acceptor; and two salts from protonation or methylation at one of the amino nitrogen atoms.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47774274","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Hiba Hashim Mahgoub Mohamed, A. B. W. E. M. Hussien, A. Saeed
{"title":"QSAR and docking studies of pyrazole analogs as antiproliferative against human colorectal adenocarcinoma cell line HT-29","authors":"Hiba Hashim Mahgoub Mohamed, A. B. W. E. M. Hussien, A. Saeed","doi":"10.5155/eurjchem.13.3.319-326.2259","DOIUrl":"https://doi.org/10.5155/eurjchem.13.3.319-326.2259","url":null,"abstract":"In-silico quantitative structure-activity relationship (QSAR) study was performed to develop a model on a series of novel pyrazole derivatives containing acetamide moiety which exhibited considerable antiproliferative activity against human colorectal adenocarcinoma cell line HT-29. The model obtained has a correlation coefficient (r) of 0.9693, squared correlation coefficient (r2) of 0.9395 and a leave-one-out (LOO) cross-validation coefficient (Q2) value of 0.8744. The predictive power of the developed model was confirmed by the external validation which has an r2 value of 0.9488. These parameters confirm the stability and robustness of the model to predict the activity of a new designed set of 3,5-dimethyl-pyrazole derivatives (22-36), results indicated that the compounds 26, 31, 35, and 36 showed the strongest antiproliferative activity with (IC50 = 0.182, 0.172, 0.166 and 0.024 μM, respectively) against human colorectal adenocarcinoma cell line HT-29 compared to the reference vemurafenib with (IC50 = 1.52 μM). Molecular docking was performed on the new designed compounds with the human colorectal adenocarcinoma cell line 5JRQ protein. The docking results showed that compounds 26, 31, 35, and 36 have docking affinity of -8.528, -5.932, 23.017 and 18.432 kcal/mol, respectively.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44021899","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Munisaa Younus, Marium Ahsan, Noor-ul Huda, M. Khan, S. Rasheed, Rabia Sadiq, F. Z. Basha
{"title":"Exploring the diastereoselectivity for Fischer indolization of L-menthone under different conditions, spectral characterization, and biological activities of new (2R,4aS)-2,3,4,4a-tetrahydro-1H-carbazole analogs","authors":"Munisaa Younus, Marium Ahsan, Noor-ul Huda, M. Khan, S. Rasheed, Rabia Sadiq, F. Z. Basha","doi":"10.5155/eurjchem.13.3.293-298.2266","DOIUrl":"https://doi.org/10.5155/eurjchem.13.3.293-298.2266","url":null,"abstract":"Tetrahydrocarbazoles are important class of heterocycles that exhibit numerous biological properties. They are also found in several natural products. In the present study, Fischer indolization of L-menthone was investigated for diastereoselectivity using different reaction conditions. No appreciable diastereoselectivity was observed for the acids used except CuBr and boric acid at varying temperatures, where satisfactory results were obtained. In addition, a small library of new (2R,4aS)-2,3,4,4a-tetrahydro-1H-carbazole analogs was reported and structurally characterized using spectroscopic techniques herein. Additionally, the compounds were evaluated against different biological activities, such as carbonic anhydrase inhibitory, immunomodulatory, and anticancer activities and did not show any activity. As the synthesized library was found safe when tested against cytotoxicity in normal cell line, it will be explored for other biological activities in near future to identify its biological outcome.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46651388","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Nichodimus Hokonya, C. Mahamadi, N. Muchanyereyi, Timothy Gutu
{"title":"Evaluation of the effects of significant factors and interactions on the enrichment of arsenic and chromium by pipette tip solid phase extraction using novel P-ZrO2CeO2ZnO nanoparticles/alginate beads","authors":"Nichodimus Hokonya, C. Mahamadi, N. Muchanyereyi, Timothy Gutu","doi":"10.5155/eurjchem.13.3.327-336.2295","DOIUrl":"https://doi.org/10.5155/eurjchem.13.3.327-336.2295","url":null,"abstract":"The study seeks to determine the most significant factors affecting arsenic and chromium enrichment using novel P-ZrO2CeO2ZnO nanoparticles/alginate beads in order to minimize the total number of runs needed to successfully run the experiment. The effects of interactions between factors were also evaluated so that the optimum conditions which are not affected by the other factors are chosen for the experiments. The most significant factors on arsenic and chromium enrichment were screened for by using a half-factorial design, followed by the optimization of significant factors using the full-factorial design, and the interaction between factors was determined using ANOVA and interaction plots. The most significant factors for chromium recovery were sample volume, eluent flow rate, and sorbent dosage. For both chromium and arsenic recovery, interactions occurred between sample volume, dosage, and pH. The optimum conditions chosen for the experiment that gave favourable results for both metal ions were sample volume 5 mL, dosage 40 mg, pH = 7 and eluent flow rate 1 mL/min. This study showed that a preliminary screening step for the most significant factors for arsenic and chromium enrichment helps to reduce the number of total runs, and for the same experiment interactions between factors were present; hence, it is necessary to take this into account during the experimental design.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42210951","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Study of some alcohol amounts in commercial alcoholic disinfectant solutions using gas chromatography with flame ionization detection","authors":"Masoumeh Darbanian, A. Nezhadali, V. Rahimi","doi":"10.5155/eurjchem.13.3.279-283.2240","DOIUrl":"https://doi.org/10.5155/eurjchem.13.3.279-283.2240","url":null,"abstract":"A simple solvent extraction method was used to analyze alcohol-based hand rubs (ABHRs) using gas chromatography with a flame ionization detector. 79 samples including 68 liquid and 11-gelled ABHRs were analyzed in the Food and Drug Laboratories Research Center of Mashhad, Iran. 17 samples had methanol, 50 samples had the correct percentage of alcohol (60-80%), and 12 samples had the incorrect percentage of alcohol (<60%). The RSD% of methanol, ethanol, and isopropanol were as 2.28, 2.18, and 1.52, respectively. The relative recoveries for methanol, ethanol, and isopropanol were 102.5, 97.8, and 114, respectively. All experiments were repeated three times. The limit of detection and the limit of quantification for methanol, ethanol, and isopropanol were obtained as 0.22, 0.24, 0.10 (%) and 0.71, 0.82, 0.68 (%), respectively.","PeriodicalId":89364,"journal":{"name":"European journal of chemistry (Print)","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48917432","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}