Madridge journal of pharmaceutical research最新文献

{"title":"Sitagliptin Attenuates the Pharmacokinetics and Biodistribution of Hydrochlorothiazide in Rats","authors":"Mbah J. Chika","doi":"10.18689/mjpr-1000110","DOIUrl":"https://doi.org/10.18689/mjpr-1000110","url":null,"abstract":"","PeriodicalId":92935,"journal":{"name":"Madridge journal of pharmaceutical research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48613846","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 Evaluation of Novel N-Substituted-[Benzoylamino]-5-Ethyl-1,2,3,6-Tetrahydropyridines as Potential Anti-Cancer Agents.","authors":"Elizabeth D Henderson,&nbsp;Madhavi Gangapuram,&nbsp;Suresh Kumar Vk Eyunni,&nbsp;Kinfe K Redda,&nbsp;Tiffany Wilson-Ardley","doi":"10.18689/mjpr-1000109","DOIUrl":"https://doi.org/10.18689/mjpr-1000109","url":null,"abstract":"<p><strong>Background and objective: </strong>Inflammation is believed to incite carcinogenesis by causing cell and genome damage. Tetrahydropyridines have gained significant synthetic interest because they constitute biologically active features of pharmaceutical agents. Previous tetrahydropyridines developed by our research group were effective in inhibiting inflammation. Since there is a relationship between inflammation and cancer, the objective of this manuscript is to expand our prior study to determine the anti-cancer activity of novel tetrahydropyridine analogs.</p><p><strong>Materials and methods: </strong>3-Ethylpyridine reacted with O-mesitylenesulfonylhydroxylamine to furnish N-amino-3-ethylpyridinium mesitylenesulfonate. The reaction of N-amino-3-ethylpyridinium mesitylenesulfonate with substituted acid chlorides gives the stable crystalline pyridinium ylides. A sodium borohydride reduction of ylides furnishes the target compounds, N-substituted [benzoylamino]-5-ethyl-1,2,3,6-tetrahydropyridines. The evaluation of these analogs cytotoxicity against Ishikawa, MCF-7, and MDA-MB-231 cell lines were determined after 72 hours of drug exposure employing CellTiter-Glo assay. To explore the interaction between the tetrahydropyridine derivatives and estrogen receptor alpha, SYBYL-X 2.1 was used to determine the best bioactive conformations of the tetrahydropyridine derivatives for the active site of the receptor.</p><p><strong>Results: </strong>Four novel N-substituted [benzoylamino]-5-ethyl-1,2,3,6-tetrahydropyridines were synthesized, purified, and characterized. The four tetrahydropyridine analogs exhibited some anti-cancer activity. Based on the molecular modeling studies, EH3 was expected to have the best antiproliferative activity due to having the highest docking score for ERα. However, EH2 had the best antiproliferative activity. Nevertheless, the biological screening and molecular modeling can provide insight to help with the design of more biologically active compounds as potential anti-cancer agents.</p>","PeriodicalId":92935,"journal":{"name":"Madridge journal of pharmaceutical research","volume":"3 1","pages":"52-59"},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6922087/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37475535","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}

{"title":"Qualitative Study on the Phytochemical Constituents of the Flower Buds of Bauhinia variegata","authors":"Ks Kew, M. Neivashini, Xc Ooi, P. Nabila, N. Khan","doi":"10.18689/mjpr-1000108","DOIUrl":"https://doi.org/10.18689/mjpr-1000108","url":null,"abstract":"The objective of the present study was to do qualitative evaluation of phytochemicals present in the flower buds of Bauhinia variegata that belongs to a family “Fabaceae’ which is well known for its scented flowers. The young premature flower buds of the plant were subjected to analysis for its phytochemical constituents as fresh material. The fresh raw flower buds of the plant were macerated and subjected to hot percolation separately. The maceration was carried out for 72 hours with absolute alcohol. The hot percolation (Soxhelt extraction) was carried out in intervals, approximately for 40 hours). The shade dried flower buds were also underwent for maceration and hot percolation separately with absolute alcohol. The extracts were dried over rotary evaporated. After evaporation, the greenish pinkish colour gummy mass was obtained from the fresh flower bud extractions. The evaporated extracts of shade dried flower buds were of greenish gummy mass. Some of the extracts were of greenish yellow and greenish in colour. All evaporated extracts were dissolved and diluted in respective solvents for phytochemical analysis. The qualitative screening of analytical results showed the presence of alkaloids, reducing sugars, terpenoids, glycosides, tannins, flavonoids and carbohydrates in all the extractions. The tests for saponins revealed that this group was not present in any of the solvent extracts. Anthraquinones showed the presence in Flower A and Bud SA only while this group was not present in Flower B, Bud A and Bud B samples.","PeriodicalId":92935,"journal":{"name":"Madridge journal of pharmaceutical research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44150518","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}