International Journal of Medicinal Chemistry最新文献

Hair Growth Promoting Effect of Dicerocaryum senecioides Phytochemicals. 植物化学物质的促发作用。

International Journal of Medicinal Chemistry Pub Date : 2019-12-12 eCollection Date: 2019-01-01 DOI: 10.1155/2019/7105834

H Rambwawasvika, P Dzomba, L Gwatidzo

{"title":"Hair Growth Promoting Effect of Dicerocaryum senecioides Phytochemicals.","authors":"H Rambwawasvika, P Dzomba, L Gwatidzo","doi":"10.1155/2019/7105834","DOIUrl":"https://doi.org/10.1155/2019/7105834","url":null,"abstract":"Phytochemicals from Dicerocaryum senecioides were studied for hair rejuvenation activity using BalB/c mice. Solvent extractions and thin layer chromatography (TLC) were used to extract and isolate the phytochemicals respectively. Phytochemicals were identified by spraying with target-specific revealing reagents. In vivo hair growth stimulating activity for each extract was tested on denuded dorsal skin of 5-week old BalB/c mice against the controls and the standard drug minoxidil. The parameters used to evaluate hair growth were hair growth completion time, hair length, hair weight, hair follicle length, and relative hair follicle area. The identified phytochemicals from the active ethanol extract were steroidal glycosides, triterpenoid glycosides, and flavonoid glycosides. Flavonoid glycosides treatment had the uppermost hair rejuvenation capacity as measured by the shortest hair growth completion time (19 days) versus control (29 days) and longest hair length (11.04 mm and 11.86 mm for male and female mice respectively while the control group had 5.15 mm for male mice and 5.33 mm for female mice). Hair growth stimulation by flavonoid glycosides was also dependent on dose concentration. It can be concluded from this study that flavonoid glycosides extracted from the leaves of Dicerocaryum senecioides have remarkable hair rejuvenation capacity in BalB/c mice. The present results provides insights on the use of Dicerocaryum senecioides for hair rejuvenation in traditional practices and on the potential of the plant as a source of novel compounds that can be used as hair growth promoters.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2019 ","pages":"7105834"},"PeriodicalIF":0.0,"publicationDate":"2019-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2019/7105834","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37581873","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 13

Caffeates and Caffeamides: Synthetic Methodologies and Their Antioxidant Properties 咖啡酸盐和咖啡酰胺:合成方法及其抗氧化性能

International Journal of Medicinal Chemistry Pub Date : 2019-11-11 DOI: 10.1155/2019/2592609

Merly de Armas-Ricard, Enrique Ruiz-Reyes, O. Ramírez-Rodríguez

{"title":"Caffeates and Caffeamides: Synthetic Methodologies and Their Antioxidant Properties","authors":"Merly de Armas-Ricard, Enrique Ruiz-Reyes, O. Ramírez-Rodríguez","doi":"10.1155/2019/2592609","DOIUrl":"https://doi.org/10.1155/2019/2592609","url":null,"abstract":"Polyphenols are secondary metabolites of plants and include a variety of chemical structures, from simple molecules such as phenolic acids to condensed tannins and highly polymerized compounds. Caffeic acid (3,4-dihydroxycinnamic acid) is one of the hydroxycinnamate metabolites more widely distributed in plant tissues. It is present in many food sources, including coffee drinks, blueberries, apples, and cider, and also in several medications of popular use, mainly those based on propolis. Its derivatives are also known to possess anti-inflammatory, antioxidant, antitumor, and antibacterial activities, and can contribute to the prevention of atherosclerosis and other cardiovascular diseases. This review is an overview of the available information about the chemical synthesis and antioxidant activity of caffeic acid derivatives. Considering the relevance of these compounds in human health, many of them have been the focus of reviews, taking as a center their obtaining from the plants. There are few revisions that compile the chemical synthesis methods, in this way, we consider that this review does an important contribution.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-11-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89569091","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}

引用次数: 12

Evaluation of the Molecular State of Piperine in Cyclodextrin Complexes by Near-Infrared Spectroscopy and Solid-State Fluorescence Measurements. 用近红外光谱和固态荧光测定环糊精配合物中胡椒碱的分子状态。

International Journal of Medicinal Chemistry Pub Date : 2019-02-11 eCollection Date: 2019-01-01 DOI: 10.1155/2019/7530480

Toshinari Ezawa, Yutaka Inoue, Isamu Murata, Koichi Takao, Yoshiaki Sugita, Ikuo Kanamoto

{"title":"Evaluation of the Molecular State of Piperine in Cyclodextrin Complexes by Near-Infrared Spectroscopy and Solid-State Fluorescence Measurements.","authors":"Toshinari Ezawa, Yutaka Inoue, Isamu Murata, Koichi Takao, Yoshiaki Sugita, Ikuo Kanamoto","doi":"10.1155/2019/7530480","DOIUrl":"https://doi.org/10.1155/2019/7530480","url":null,"abstract":"The purpose of this study was to evaluate the physicochemical properties of piperine (PP) in ground mixtures (GMs) of PP with α-, β-, or γ-cyclodextrin (CD) under conditions of humidity, heat, and humidity-heat. In solid-state fluorescence measurements, the fluorescence maxima for GM (PP/αCD = 1/2), GM (PP/βCD = 1/1), and GM (PP/γCD = 1/1) were observed at 463, 472, and 469 nm, respectively. On the other hand, the humidified GMs exhibited maxima at 454, 460, and 465 nm, while the humidified-heated samples displayed fluorescence maxima at 455, 455, and 469 nm, respectively. Therefore, the molecular behavior of PP with α, β, and γCD was concluded to vary upon the coordination of water molecules. NIR and solid-state fluorescence measurements revealed that the molecular behavior of PP inside the α, β, and γCD cavity changed by water and heat factors depends on the mobility of the methylenedioxyphenyl group.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2019 ","pages":"7530480"},"PeriodicalIF":0.0,"publicationDate":"2019-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2019/7530480","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37231063","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

Synthesis and Evaluation of Baylis-Hillman Reaction Derived Imidazole and Triazole Cinnamates as Antifungal Agents. Baylis-Hillman反应衍生咪唑和三唑肉桂酸酯的合成与评价。

International Journal of Medicinal Chemistry Pub Date : 2018-10-16 eCollection Date: 2018-01-01 DOI: 10.1155/2018/5758076

Grady L Nelson, Michael J Williams, Shirisha Jonnalagadda, Mohammad A Alam, Gautam Mereddy, Joseph L Johnson, Sravan K Jonnalagadda

引用次数: 1

Crystallography and Its Impact on Carbonic Anhydrase Research. 晶体学及其对碳酸酐酶研究的影响。

International Journal of Medicinal Chemistry Pub Date : 2018-09-13 eCollection Date: 2018-01-01 DOI: 10.1155/2018/9419521

Carrie L Lomelino, Jacob T Andring, Robert McKenna

{"title":"Crystallography and Its Impact on Carbonic Anhydrase Research.","authors":"Carrie L Lomelino, Jacob T Andring, Robert McKenna","doi":"10.1155/2018/9419521","DOIUrl":"10.1155/2018/9419521","url":null,"abstract":"X-ray and neutron crystallography are powerful techniques utilized to study the structures of biomolecules. Visualization of enzymes in complex with substrate/product and the capture of intermediate states can be related to activity to facilitate understanding of the catalytic mechanism. Subsequent analysis of small molecule binding within the enzyme active site provides insight into mechanisms of inhibition, supporting the design of novel inhibitors using a structure-guided approach. The first X-ray crystal structures were determined for small, ubiquitous enzymes such as carbonic anhydrase (CA). CAs are a family of zinc metalloenzymes that catalyze the hydration of CO2, producing HCO3 - and a proton. The CA structure and ping-pong mechanism have been extensively studied and are well understood. Though the function of CA plays an important role in a variety of physiological functions, CA has also been associated with diseases such as glaucoma, edema, epilepsy, obesity, and cancer and is therefore recognized as a drug target. In this review, a brief history of crystallography and its impact on CA research is discussed.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2018 ","pages":"9419521"},"PeriodicalIF":0.0,"publicationDate":"2018-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6158936/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36558522","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Phytochemical Study and Evaluation of the Cytotoxic Properties of Methanolic Extract from Baccharis obtusifolia. 烟酒醇提物细胞毒性的植物化学研究与评价。

International Journal of Medicinal Chemistry Pub Date : 2018-08-01 eCollection Date: 2018-01-01 DOI: 10.1155/2018/8908435

Juan Carlos Romero-Benavides, Gina C Ortega-Torres, Javier Villacis, Sara L Vivanco-Jaramillo, Karla I Galarza-Urgilés, Natalia Bailon-Moscoso

引用次数: 9

Applications of Click Chemistry in the Development of HIV Protease Inhibitors. 点击化学在HIV蛋白酶抑制剂开发中的应用。

International Journal of Medicinal Chemistry Pub Date : 2018-07-19 eCollection Date: 2018-01-01 DOI: 10.1155/2018/2946730

Mukesh M Mudgal, Nagaraju Birudukota, Mayur A Doke

{"title":"Applications of Click Chemistry in the Development of HIV Protease Inhibitors.","authors":"Mukesh M Mudgal, Nagaraju Birudukota, Mayur A Doke","doi":"10.1155/2018/2946730","DOIUrl":"https://doi.org/10.1155/2018/2946730","url":null,"abstract":"Acquired Immunodeficiency Syndrome (AIDS) has been devastating for millions of people around the world. Inhibition of the human immunodeficiency virus (HIV) protease is among the most important approaches for the therapeutic intervention in HIV infection. Since the discovery of the HIV-1 protease, this enzyme has been considered as a key target for the inhibition of viral replication. A large body of research has been done to develop an effective HIV-1 protease inhibitor. There are to date 10 HIV-1 protease inhibitor drugs approved by the Food and Drug Administration (FDA) that have improved the survival and quality of life of HIV infected people. These drugs are prescribed in combination with the reverse transcriptase inhibitors, which is referred to as highly active antiretroviral therapy (HAART). The HIV-1 protease inhibitors play a vital role in HAART. The applications of click chemistry are dispersing in the field of drug discovery. Recently, click chemistry has captured a lot of attention and has become a powerful tool for the synthesis of medicinal skeletons in the discovery of anti-HIV drugs. Click reaction is a well-known method for making carbon-heteroatom-carbon bonds. Click reactions are popular because they are wide in scope, of high yielding, quick to perform, and easy to purify. In this review, we outlined current approaches towards the development of HIV-1 protease inhibitors employing click chemistry.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2018 ","pages":"2946730"},"PeriodicalIF":0.0,"publicationDate":"2018-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2018/2946730","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36401375","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Biophysical, Biochemical, and Cell Based Approaches Used to Decipher the Role of Carbonic Anhydrases in Cancer and to Evaluate the Potency of Targeted Inhibitors. 生物物理，生化和基于细胞的方法用于破译碳酸酐酶在癌症中的作用，并评估靶向抑制剂的效力。

International Journal of Medicinal Chemistry Pub Date : 2018-07-16 eCollection Date: 2018-01-01 DOI: 10.1155/2018/2906519

Mam Y Mboge, Anusha Kota, Robert McKenna, Susan C Frost

{"title":"Biophysical, Biochemical, and Cell Based Approaches Used to Decipher the Role of Carbonic Anhydrases in Cancer and to Evaluate the Potency of Targeted Inhibitors.","authors":"Mam Y Mboge, Anusha Kota, Robert McKenna, Susan C Frost","doi":"10.1155/2018/2906519","DOIUrl":"https://doi.org/10.1155/2018/2906519","url":null,"abstract":"Carbonic anhydrases (CAs) are thought to be important for regulating pH in the tumor microenvironment. A few of the CA isoforms are upregulated in cancer cells, with only limited expression in normal cells. For these reasons, there is interest in developing inhibitors that target these tumor-associated CA isoforms, with increased efficacy but limited nonspecific cytotoxicity. Here we present some of the biophysical, biochemical, and cell based techniques and approaches that can be used to evaluate the potency of CA targeted inhibitors and decipher the role of CAs in tumorigenesis, cancer progression, and metastatic processes. These techniques include esterase activity assays, stop flow kinetics, and mass inlet mass spectroscopy (MIMS), all of which measure enzymatic activity of purified protein, in the presence or absence of inhibitors. Also discussed is the application of X-ray crystallography and Cryo-EM as well as other structure-based techniques and thermal shift assays to the studies of CA structure and function. Further, large-scale genomic and proteomic analytical methods, as well as cell based techniques like those that measure cell growth, apoptosis, clonogenicity, and cell migration and invasion, are discussed. We conclude by reviewing approaches that test the metastatic potential of CAs and how the aforementioned techniques have contributed to the field of CA cancer research.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2018 ","pages":"2906519"},"PeriodicalIF":0.0,"publicationDate":"2018-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2018/2906519","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36399787","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Synthesis, Anti-Inflammatory Activity, and In Silico Study of Novel Diclofenac and Isatin Conjugates. 新型双氯芬酸和依沙汀缀合物的合成、抗炎活性和硅研究。

International Journal of Medicinal Chemistry Pub Date : 2018-06-12 eCollection Date: 2018-01-01 DOI: 10.1155/2018/9139786

Musab Mohamed Ibrahim, Tilal Elsaman, Mosab Yahya Al-Nour

{"title":"Synthesis, Anti-Inflammatory Activity, and In Silico Study of Novel Diclofenac and Isatin Conjugates.","authors":"Musab Mohamed Ibrahim, Tilal Elsaman, Mosab Yahya Al-Nour","doi":"10.1155/2018/9139786","DOIUrl":"https://doi.org/10.1155/2018/9139786","url":null,"abstract":"The design, synthesis, and development of novel non-steroidal anti-inflammatory drugs (NSAIDs) with better activity and lower side effects are respectable area of research. Novel Diclofenac Schiff's bases (M1, M2, M4, M7, and M8) were designed and synthesized, and their respective chemical structures were deduced using various spectral tools (IR, 1H NMR, 13C NMR, and MS). The compounds were synthesized via Schiff's condensation reaction and their anti-inflammatory activity was investigated applying the Carrageenan-induced paw edema model against Diclofenac as positive control. Percentage inhibition of edema indicated that all compounds were exhibiting a comparable anti-inflammatory activity as Diclofenac. Moreover, the anti-inflammatory activity was supported via virtual screening using molecular docking study. Interestingly compound M2 showed the highest in vivo activity (61.32% inhibition) when compared to standard Diclofenac (51.36% inhibition) as well as the best binding energy score (-10.765) and the virtual screening docking score (-12.142).","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2018 ","pages":"9139786"},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2018/9139786","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36312303","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 15

Synthesis, Characterization, and Antimicrobial Activity of a Novel Trisazo Dye from 3-Amino-4H-thieno[3,4-c][1]benzopyran-4-one. 新型3-氨基- 4h -噻吩[3,4-c][1]苯并吡喃-4-酮三氮杂染料的合成、表征及抗菌活性

International Journal of Medicinal Chemistry Pub Date : 2018-02-01 eCollection Date: 2018-01-01 DOI: 10.1155/2018/9197821

Joseph Tsemeugne, Emmanuel Sopbué Fondjo, Jean-de-Dieu Tamokou, Taoufik Rohand, Arnaud Djintchui Ngongang, Jules Roger Kuiate, Beibam Luc Sondengam

{"title":"Synthesis, Characterization, and Antimicrobial Activity of a Novel Trisazo Dye from 3-Amino-4H-thieno[3,4-c][1]benzopyran-4-one.","authors":"Joseph Tsemeugne, Emmanuel Sopbué Fondjo, Jean-de-Dieu Tamokou, Taoufik Rohand, Arnaud Djintchui Ngongang, Jules Roger Kuiate, Beibam Luc Sondengam","doi":"10.1155/2018/9197821","DOIUrl":"https://doi.org/10.1155/2018/9197821","url":null,"abstract":"A new trisazo dye has been synthesized by coupling the diazonium ion of 3-amino-4H thieno[3,4-c][1]benzopyran-4-one with 2-tert-butyl-4-methoxyphenol. The newly prepared trisazo dye was characterized by its physical, elemental, and spectroscopic data. 2D-NMR (COSY, HSQC, and HMBC) techniques were used to secure the structural assignments. The new trisazo dye (compound 7) along with precursors 3, 4, and 6 was screened by microdilution susceptibility assay for antibacterial and antifungal activities towards eight bacterial strains and three yeasts selected on the basis of their relevance as human pathogens. The results showed that compound 7 (MIC = 2-128 μg/mL) was the most active as compared with its precursors. The most resistant microorganisms were V. cholerae NB2 and V. cholerae SG24, whereas the most sensitive microorganism was C. neoformans. The overall results of this study indicated that compound 7 had the greatest potential value against both yeasts and multidrug-resistant bacteria, so further investigation is warranted.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2018 ","pages":"9197821"},"PeriodicalIF":0.0,"publicationDate":"2018-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2018/9197821","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"35864947","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 10