{"title":"Synthesis, In vitro Antibacterial and Antifungal Activities of Trifluoroalkyl-N, N’-Disubstituted Thioureas","authors":"M. Sanhoury","doi":"10.19080/omcij.2019.09.555770","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555770","url":null,"abstract":"A series of N-(4-trifluoromethylphenyl) thiourea derivatives of biological interest has been prepared by the condensation of various isothiocyanates with primary 4-trifluorophenylamine under uncatalyzed conditions. The chemical structures of all the reported compounds were confirmed by FT-IR, multinuclear NMR (1H, 13C, 19F) and HRMS spectrometry. Some of these compounds were screened for their in vitro antibacterial activity against ten pathogenic strains representing different types of gram-positive and gram-negative bacteria, two pathogenic fungi ( Penicilluim sp, Aspergillus flavus ) and two yeasts ( Candida albicans and Candida glabrata ). More than four of the synthesized compounds showed promising inhibition activities against the tested strains ATCC 19436 with reference to standard vancomycin. Best antimicrobial activity was founded for the 3-pyridylthiourea derivative against Enterococcus faecuim ATCC 25923 with CMI= 3.9 mg/mL. The results indicated also that all the new screened compounds have promising antifungal activity comparable to the activity observed for the reference compounds.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73367219","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":"Chemical Constituents of an Iranian Grown Capsicum annuum and their Cytotoxic Activities Evaluation","authors":"R. Zibaseresht","doi":"10.19080/omcij.2019.09.555769","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555769","url":null,"abstract":"A sample of cayenne pepper ,Capsicum annuum –(Family Solanaceae) was collected from a region in Hamadan, west Iran and extracted from EtOH. GC-MS analysis showed at least 8 compounds out of which 7 compounds were isolated and characterized using 1 H NMR analysis. Cytotoxic effects of the 7 isolated and characterized compounds along with the extract were evaluated against Caco-2 cell lines using MTT assay. The IC 50 values for ethyl palmitate (1), linolelaidic acid ethyl ester (2), ethyl stearate (3), ethyl iso-allocholate (4), 2-(((2-ethylhexyl)oxy)carbonyl) benzoic acid (5), capsaicin (6), dihydrocapsaicin (7) and the extract mixture were determined in μ M (111, 112, 118, 40, 130, 91, 115, and 110, respectively). The data indicated higher cytotoxic effects of (4) and (6) suggested as potential compounds against Caco-2 cell lines.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76198931","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":"Synthesis Condition and Treatment Assisted Tuning of Structural, Magnetic Properties and Bandgap of Ni Nano Ferrite","authors":"Kane S N","doi":"10.19080/omcij.2019.09.555768","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555768","url":null,"abstract":"We report synthesis condition, and thermal treatment assisted tuning of structural, magnetic properties, and bandgap of Ni nano ferrite. Experimental techniques of x-ray diffraction ‘XRD,’ vibration sample magnetometry, Ultraviolet-visible (UV-Vis) diffuse reflectance measurements, Scanning Electron Microscopy ‘SEM,’ Energy Dispersive spectroscopy ‘EDS’ measurements, were used to study the synthesized samples. XRD verify the formation of nano spinel ferrite phase (grain diameter: 38.3-39.2nm), and incorporation of Ni, Fe in spinel lattice, with lattice parameter (0.8345-0.8352nm), which also shows the presence of α -Fe 2 O 3 phase. Results reveal that synthesis condition, and thermal treatment show: a) SEM images with non-homogeneous particle size dispersion, particle agglomeration, while EDS confirms the presence of all elements in studied NiFe 2 O 4 samples, b) non-equilibrium cation distribution, modification of inversion parameter, oxygen parameter, c) strengthening of A-O-B, A-O-A and weakening of B-O-B interaction super-exchange interactions, d) fine-tuning of bandgap (1.39 eV-1.68 eV), and depends on structural properties, e) observed magnetic properties are a collective effect of non-equilibrium cationic distribution; modification of A-O-B, A-O-A, B-O-B super-exchange interactions, and surface spin-canting. Prospective applications based on synthesized nano ferrites are also discussed. Thus, in this work we report, sol-gel auto-combustion synthesis of NiFe 2 O 4 : by varying synthesis conditions (via microwave-assisted sol-gel synthesis, conventional sol-gel synthesis in dry gel form), and post-preparation thermal annealing, to tune structural, magnetic properties and bandgap energy. Prepared samples are studied by x-ray diffraction ‘XRD,’ vibration sample magnetometry, Ultraviolet-visible (UV-Vis) diffuse reflectance measurements, Scanning Electron Microscopy SEM,’ Energy Dispersive spectroscopy ‘EDS’ measurements.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73063303","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":"Synthesis, Characterization, Biological and Antitumor Activity of Co(II) , Ni (II) , Cu(II) and Zn (II) Complexes of N-(2-Chlorophenyl)-N’-Benzoyl Thiourea","authors":"Khalid M Wahdan","doi":"10.19080/omcij.2019.09.555767","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555767","url":null,"abstract":"A derivative of thiourea ligand N-(2-chlorophenyl)-N’-Benzoyl thiourea (CBT) in equimolar ratio 1:1and its transition metal complexes Co II , Ni II , Cu II and Zn II were synthesized by microwave (green chemistry). The structure of ligand and its complexes have been characterized by using elemental analysis, mass Spectroscopy, FT-IR, UV-Vis,1HNMR and 13CNMR. The geometry of the proposed structures of the chelates based on their electronic spectra, electron spin resonance (ESR) and magnetic susceptibility. The stability of complexes was studied by TGA analysis (Thermal studies). The free derivative thiourea ligand (CBT) and its complexes were Studied for antibacterial and antifungal activity. Also the anticancer activity of ligand and its complexes were studied against breast cell cancer (MCF-7). It was noticed that the Ni II complex showed the highest cytotoxic activity (IC 50 =122) more than the free CBT ligand.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73244046","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":"An Assessment of the Anti-Inflammatory, Antimicrobial, and Antioxidant Activities of Ficus sur Stem-Bark","authors":"Clement Osei Akoto","doi":"10.19080/omcij.2019.09.555766","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555766","url":null,"abstract":"Ficus sur (Moraceae), is a plant that has found use in traditional African medicine in the treatment of sickle cell disease, epilepsy, pain and inflammations. The present study was aimed at investigating hexane and methanol stem-bark extracts of Ficus sur for their phytoconstituents, anti-inflammatory, antimicrobial and antioxidant activities. Phytochemical screenings were performed using standard protocols. In-vitro anti-inflammatory activities were assessed using egg albumin denaturation method. In-vitro antimicrobial (agar and broth dilution method) and antioxidant [total antioxidant capacity (TAC), DPPH and H 2 O 2 scavenging] assays were carried out on the extracts. Thin layer chromatography was employed in the separation of the components of both extracts. The phytochemical investigation revealed the presence of secondary metabolites such as anthraquinones, terpenoids, flavonoids, steroids, saponins, phenols and tannins. The extracts showed anti-inflammatory activity comparable to that of diclofenac sodium. The extracts showed antimicrobial activity against test organisms with MICs ranging from 2.5- 40 mg/ mL. The IC 50 values for methanol and hexane extracts in the DPPH and H 2 O 2 assays were 89.95 ± 0.30 and 350.70 ± 0.72 μg/mL and 708.51 ± 0.28 and 682.76 ± 0.20 μg/mL, respectively. The TAC (gAAE/100 g) for methanol and hexane extracts were 23.560 ± 0.014 and 17.863 ± 0.037 g, respectively. The results suggest that the stem bark of Ficus sur could be exploited as potential therapeutic candidate for the treatment of bacterial infections, inflammations and diseases associated with oxidative-stress.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"113 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79387606","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":"Synthesis of a Novel Sensor Electrode Based on Bromothymol Blue as an Indicator Electrode in Potentiometric Acid-Base Titration in Aqueous Solution","authors":"Nasser M Abu Ghalwa","doi":"10.19080/omcij.2019.09.555764","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555764","url":null,"abstract":"A modified bromothymol blue BTB electrode was prepared by spin coating of the BTB indicator on conducting glass substrate, and its use as indicator electrode to potentiometric acid-base titration in aqueous solution at 298 K was developed. The change of the open circuit potential with pH (E-pH) curve is linear with slope of 0.052 V/Dec at 298 K. The standard potential of this electrode, E0, was determined with respect to the SCE as reference electrode. The recovery percentage for potentiometric acid-base titration using G/BTB as indicator electrode was calculated","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"22 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76344027","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":"LCA-AZT Conjugate Anti-Cancer invitro Activity","authors":"Hengguang Li","doi":"10.19080/omcij.2019.09.555760","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555760","url":null,"abstract":"Pseudo nucleoside or short pseudo aptamer and telomerase have been selected as novel ligands and receptors in our effort to discover new anti-cancer reagents. We proposed that lithocholic acid (LCA) could be able to play the role of a vehicle to transport major therapeutic moiety into cell membrane through oral administration, like cholic acid delivering fatty acids, peptides in gastrointestinal track, but it’s more hydrophobic. Zidovudine or azidothymidine (AZT) was used as targeting head or/and therapeutic reagent aiming reverse transcriptase that plays central role of cancer cell telomere repairing. Telomerase is a reverse transcriptase, the major TERT, or hTERT in humans is a catalytic subunit of the entire enzyme. Even though both LCA and AZT have anticancer activities respectively, the conjugate of LCA-AZT was designed as our initial pseudo short aptamer inhibitor of cancer telomerase to verify our hypothetic concept that pseudo short aptamers targeting cancer telomerase are able to shut down the cancer cell growth, and cause the cells eventually senescence and mortality. As a consequence, two lung cancer cell lines and two colorectal cancer cell lines were treated by the conjugate, except lung cancer cell H1299, the efficacy of the conjugate was better than the parent compounds apparently. It conformed and proofed also the docking predictions via the molecular computational simulation. The all cancer cells used by a CCK-8 assay appeared apoptosis in the range of 56 μM – 90 μM IC50 after exposure to the LCA-AZT conjugate. The effectiveness of the conjugate was also time dependent, because the telomerase is a kind of reverse transcriptase, the mechanism would be like the inhibition of reverse transcriptase in HIV virus, the inhibition of telomere repairing toward cell death would be time consumable.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77112956","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":"Insight into Interactions of l-Arginine/l-Histidine with Drug Betaine Hydrochloride in Aqueous Medium at Different Temperatures by using Physicochemical Methods","authors":"Anil Kumar Nain","doi":"10.19080/omcij.2019.09.555763","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555763","url":null,"abstract":"Studies on physicochemical properties of l -arginine/ l -histidine in aqueous solutions of betaine hydrochloride are beneficial in understanding solute-solvent interactions. The densities, ρ , ultrasonic speeds, u and viscosities, η of l -arginine and l -histidine in water and in aqueous-betaine hydrochloride (1 % and 2 % betaine hydrochloride in water, w/w) solvents have been experimentally measured at six temperatures (293.15, 298.15, 303.15, 308.15, 313.15 and 318.15) K and at atmospheric pressure in nine different concentrations. Related molecular and thermodynamic properties like the apparent molar volume, V φ , limiting apparent molar volume, and transfer volume, , were also evaluated in this study using density data. Likewise from the ultrasonic data, different thermo-acoustical parameters, such as apparent molar compressibility, , s K φ , limiting apparent molar compressibility, , s K οφ and transfer compressibility, , , s tr K οφ have been evaluated. The trends in transfer properties have been interpreted in terms of cosphere overlap model. In addition, the rheological data have been used to determine Falkenhagen Coefficient, A , Jones-Dole coefficient, B , free energy of activation of viscous flow per mole of solvent, and solute, #2 , entropies, # S ο ∆ and enthalpies, # H ο ∆ of activation of viscous flow. Hydration number, H n has also been calculated. Different parameters such as nature of solute, solute-solvent interactions, etc., were categorized by using different analytical and physical loom. The results show that the studied drug is a structure maker compound in all systems of this work. The free energy parameters indicate the formation of transition state in the presence of amino acids. The solute co-solute interactions are strongest in the system containing l -arginine.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84907011","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":"New MCl3 (M = Y, Dy, Pr) Salicylato, Maleato, Phtalato, Phenylsufonato and Phosphato Complexes and Adducts: Synthesis and Infrared Study","authors":"Dame Seye","doi":"10.19080/omcij.2019.09.555761","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555761","url":null,"abstract":"Nine rare earth complexes have been synthesized from reaction carried in common organic solvent between salicylate, maleate, phtalate, phenylsulfonate or phosphate ammonium salt and MCl3 (M = Y, Dy, Pr). All compounds have been structurally characterized by infrared. Structures involving the complex anions have been proposed. The suggested structures are discrete or of double metallic components type. The oxyanions behave towards metallic centres as monodentate, monochelating or monochelating and monodentate ligands. The coordination number at rare earth metal atoms vary from five (5) for Pr and Dy to twelve (12) for Dy. For compounds containing a protonated amine, when the possible hydrogen bonding interactions are considered supramolecular architectures may be","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77738056","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":"Essential Oil Activity Against Methicillin-Resistant Staphylococcus aureus and Multidrug-Resistant Mycobacterium tuberculosis: A Mini-Review","authors":"A. Intisar","doi":"10.19080/omcij.2019.09.555759","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555759","url":null,"abstract":"Drug resistance among pathogenic bacteria has been a major concern for decades. Diseases caused by them have been the main cause of death in developing countries where this factor contributes around one third of the total number of deaths. With the gradual increase in microbial resistance and the side effects that synthetic medicines may cause, there has always been a need of finding natural medicines that can effectively treat such diseases. Among such potent resources are plant essential oils that have been reported in literature and is a recent topic of extraordinary interest. In this study, antimicrobial potential of essential oils of various plants against two resistant strains: methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Mycobacterium tuberculosis (MDRTB), has been discussed.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"116 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79223164","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}