药物化学期刊(英文)最新文献

{"title":"Physicochemical Properties and Biological Activities of Novel Hydrazonate Copper Complexes","authors":"Sommai Patitungkho, Kingkaew Patitungkho","doi":"10.4236/ojmc.2023.131001","DOIUrl":"https://doi.org/10.4236/ojmc.2023.131001","url":null,"abstract":"","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88433748","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, SAR, and in Silico ADME Screening Studies of Some 9-Amino-3-Phenylacridone Derivatives as Topoisomerase II Inhibitors","authors":"Abiodun S. Oyedele, Toluwase H. Fatoki, Esha Dalvie, Neil Osheroff, Cosmas O. Okoro","doi":"10.4236/ojmc.2023.132002","DOIUrl":"https://doi.org/10.4236/ojmc.2023.132002","url":null,"abstract":"Cancer is a leading cause of death globally, claiming about 9.6 million lives and approximately 420 million new cases of cancer will be diagnosed in the world by the year 2025. The aim of this study was to synthesize and computationally evaluate pharmacological potential of some derivatives of 9-amino-3-phenylacridone, as topoisomerase II (Topo II) inhibitors. In this study, 10 derivatives of 3-phenyl-9-aminoacridone were chemically synthesized and characterized, and the potential pharmacological indications of these compounds were computationally predicted by methods such as ADMET prediction, molecular target prediction and molecular docking. The results showed that two derivatives (58e and 58j) were non-permeant of blood-brain barrier, and this property was found similar to that of amsacrine and etoposide. The results of molecular docking of the ten derivatives of 3-phenyl-9-aminoacridone that were synthesized in this work showed that the synthetic compounds (58a-j) and the standard drugs have overall best binding affinities for human acetylcholine esterase than butyrylcholinesterase, and overall best binding affinities for human topo IIα than human topo IIβ. Overall, the results of this study suggest that the synthetic compounds 58a, 58c, 58f, 58g, and 58i could probably inhibit topo IIα by catalytic inhibition as seen with amsacrine, but only 58b and 58e possessed DNA non-intercalation properties as seen with etoposide, serving as topo II poison. In conclusion, this study showed that 3-phenyl-9-aminoacridone derivatives are potential inhibitor of topo IIα/β both by catalytic inhibition and poison as non-intercalator of DNA.","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135360664","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 Copper (II), Palladium (II), and Platinum (II) 2-Acetylpyrazine Tert-Butylthiosemicarbazone Complexes: Inhibition of Human Topoisomerase IIα and Activity against Breast Cancer Cells","authors":"E. Lisic, Sarah N. Grossarth, Sarah B. Bowman, Jessica L. Hill, Michael W. Beck, J. Deweese, Xiaohua Jiang","doi":"10.4236/ojmc.2022.121001","DOIUrl":"https://doi.org/10.4236/ojmc.2022.121001","url":null,"abstract":"","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74623744","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, Biological Evaluation, and SAR Studies of Varyingly Substituted 4-Thioflavonols","authors":"Rubina Bibi, A. Sadiq, E. Mughal","doi":"10.4236/ojmc.2022.122002","DOIUrl":"https://doi.org/10.4236/ojmc.2022.122002","url":null,"abstract":"","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84463731","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":"Design, Synthesis and Antibacterial Activity Evaluation of 4,5-Diphenyl-1H-Imidazoles Derivatives","authors":"Coulibaly Bamoro, Fante Bamba, Koffi Téki Dindet Steve-Evanes, A. Vallin, V. Chagnault","doi":"10.4236/ojmc.2021.112002","DOIUrl":"https://doi.org/10.4236/ojmc.2021.112002","url":null,"abstract":"Due to the continuous emergence and rapid spread of drug-resistant strains of bacteria, there is an urgent need for the development of novel antimicrobials. Along this line, the synthesis and antibacterial activity of 4,5-diphenylimidazol-2-thiol derivatives 2a-g and 6a-e are reported. The structures of the synthesized compounds were confirmed by Nuclear Magnetic Resonance (NMR) and High Resolution Mass Spectrometry (HRMS). All compounds were screened in vitro for their antibacterial activity against Pseudomonas aeruginosa and Escherichia coli (Gram-negative bacteria) and also against Staphyloccocus aureus and Enterococcus faecalis (Gram-positive bacteria). The results showed most of the synthesized compounds have no antibacterial activity. However compound 6d was two-fold potent than ciprofloxacin against Staphylococcus aureus with Minimum Inhibitory Concentration (MIC) of 4 μg/mL and 6c showed moderate biological activity against Staphylococcus aureus (16 μg/mL) and Enterococcus faecalis (16 μg/mL).","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75790641","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":"Anti-Melanogenesis Effect of Daniellic Acid Isolated from Daniellia oliveri (Rolfe) Hutch. & Dalziel (Leguminosae) Oleoresin of Burkina Faso","authors":"Aminata P. Nacoulma, M. Compaoré, N. R. Meda, L. Pottier, V. Megalizzi, I. Somé, M. Kiendrebeogo","doi":"10.4236/ojmc.2021.114004","DOIUrl":"https://doi.org/10.4236/ojmc.2021.114004","url":null,"abstract":"Over the past years, natural products have been used as useful candidates for prevention and treatment of skin disorders such as skin darkening. In this current research, Daniellia oliveri which was a potential source of cosmeceut-ical agent was selected to investigate its active components. Daniellic acid isolated from the oleoresin was characterized by using data from 1 H-NMR, 13 C-NMR, HSQC, IR, and online chemo-informatic analysis. The daniellic acid antioxidant, anti-proliferative, and tyrosinase inhibition capabilities were evaluated. This compound possessed an anti-DPPH and iron (III) reducing effect compared to quercetin. It was able to inhibit 9 tumor cells with IC 50 going from 0.03 mM (U373) to 0.14 mM (Malme-3M). Interestingly daniellic acid inhibits tyrosinase activity with 1.20 mM as IC 50 . The tyrosinase inhibition mechanism was noncompetitive mixed-type with un-significant effect on cell melanogenesis. Daniellic acids induced a half-reduction of melanin production in B16F10 cell in IBMX stimulation (p < 0.05). The same observation was effective in Malme-3M melanin production with a significant daniellic acid action than kojic acid (p < 0.05) without reducing cell viabilities. This bioactive daniellic acid could explain the traditional uses of oleoresins from Daniellia oliveri for genitor-urinary tract diseases treatments, wound healing, and skin ailments in Burkina Faso.","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85035492","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":"Critical Evaluation of Melaleuca alternifolia : A Review of the Phytochemical Profile, Pharmacological Attributes and Medicinal Properties in the Botanical, Human and Global Perspectives","authors":"Ibrahim Kasujja","doi":"10.4236/OJMC.2021.111001","DOIUrl":"https://doi.org/10.4236/OJMC.2021.111001","url":null,"abstract":"Melaleuca (tea tree) oil has become increasingly commonly used in recent decades. The essential oil in Australia for the past 120 years is now available globally as an active component in various products. Historically, Melaleuca oil is known for its antiseptic and anti-inflammatory actions. Currently, microwave technology is applied to extract Melaleuca oil, but this extraction technology is not commercially under practice. Traditionally, Melaleuca oil extraction is possible through steam distillation of the Melaleuca alternifolia terminal branches and leaves, and the resultant extract is always either clear or pale yellowish. Melaleuca oil has been promoted as a therapeutic agent because scientific studies indicate that the Rideal-Walker (RW) coefficients of its extract composition include 8 for cymene, 16 for terpineol, 13.5 for tepinen-4-ol and 3.5 for cineole. The mode of action against bacteria is now partially elucidated, and assumptions exist. Hydrocarbons partition into biological membranes to disrupt the vital functions of Melaleuca oil, and also its components behave in the same manner. Therefore, the inhibition of respiration and the leakage of ions or loss of intracellular material and the inability to maintain homeostasis reflect the loss of membrane integrity and lysis in Melaleuca oil products containing lower than usual terpenes concentrations. Melaleuca oil possesses antifungal properties and is known exclusively for the treatment of Candida albicans. This essential oil strongly changes the permeability of Candida albican cells. C. albicans treatment with 0.25% tea tree oil leads to propidium iodide uptake. However, a significant loss of 260-nmlight-absorbing materials after staining with methylene blue occurs after 6 hours. Melaleuca extracts alter the permeability of Candida glabrata that ocHow to cite this paper: Kasujja, I. (2021) Critical Evaluation of Melaleuca alternifolia: A Review of the Phytochemical Profile, Pharmacological Attributes and Medicinal Properties in the Botanical, Human and Global Perspectives. Open Journal of Medicinal Chemistry, 11, 1-15. https://doi.org/10.4236/ojmc.2021.111001 Received: December 14, 2020 Accepted: March 28, 2021 Published: March 31, 2021 Copyright © 2021 by author(s) and Scientific Research Publishing Inc. This work is licensed under the Creative Commons Attribution International License (CC BY 4.0). http://creativecommons.org/licenses/by/4.0/","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77492245","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 and Antibacterial Activities of New 2-(Benzylthio)pyrimidines and 2-(Benzimidazolylmethylthio)pyrimidines Derivatives","authors":"Achi Patrick-Armand, Coulibali Sioménan, Zon Doumadé, Timotou Adéyolé, B. Eric, Touré Daouda, Sissouma Drissa, A. Ané","doi":"10.4236/ojmc.2021.113003","DOIUrl":"https://doi.org/10.4236/ojmc.2021.113003","url":null,"abstract":"","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79365824","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":"Targeting PPARγ Receptor Using New Phosphazene Derivative Containing Thiazolidinedione: Design, Synthesis, and Glucose Uptake","authors":"S. S. Neyadi, A. Adem, N. Amir, I. Abdou","doi":"10.4236/ojmc.2020.102003","DOIUrl":"https://doi.org/10.4236/ojmc.2020.102003","url":null,"abstract":"The peroxisome proliferator activator receptor-γ (PPAR-γ) remained the most effective target for management of diabetes mellitus. The present work endeavors rational designing new PPAR-γ agonist bearing cyclotriphosphazene and thiazolidine-2,4-dione scaffolds. Thiazolidinedione (TZD) derivatives are the novel class of oral antidiabetic drugs which are selective agonist for the nuclear PPARγ that enhances the transcription of several insulin responsive genes but TZDs are known to cause weight gain, hepatotoxicity and fluid retention. So, cyclotriphosphazene containing thiazolidine-2,4-dione was designed, synthesized as PPARγ agonist. The in-vitro antidiabetic activity showed that compound 8 has similar activity and exhibited higher glucose uptake in comparison to pioglitazone as reference drugs. This research opened new avenues for smart designing of molecules with high efficiency towards the management of hyperglycemia.","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90246643","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 and Characterization of Kalata B2 Cyclotide (GLPVCGETCFGGTCNTPGCSCTWPICTRD) on Wang Resin, as Solid Support","authors":"Verma Deepshikha, P. Rajasekharan","doi":"10.4236/ojmc.2020.102004","DOIUrl":"https://doi.org/10.4236/ojmc.2020.102004","url":null,"abstract":"With the help of the solid phase peptide synthesizing method, we synthesized Kalata B2 cyclotide and the final product was purified by preparative HPLC. The sequence of Kalata B2 is GLPVCGETCFGGTCNTPGCSCTWPICTRD and its m/z M + H mass is 2955.53. It had been first isolated from Oldenlandia affinis plant leaves extract which belongs to Rubiaceae family. The synthesis of Kalata B2 has been characterized through UPLC/MS, LC/MS, CD, 1HNMR, and IR.","PeriodicalId":68630,"journal":{"name":"药物化学期刊(英文)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89164284","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}