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Synthesis and biological evaluation of a new series of ortho-carboranyl biphenyloxime derivatives. 一类新的邻碳硼基联苯氧肟衍生物的合成及生物学评价。
Chemistry Central Journal Pub Date : 2018-06-29 DOI: 10.1186/s13065-018-0444-z
Guofan Jin, Fuyan Xiao, Ruijiang Liu
{"title":"Synthesis and biological evaluation of a new series of ortho-carboranyl biphenyloxime derivatives.","authors":"Guofan Jin,&nbsp;Fuyan Xiao,&nbsp;Ruijiang Liu","doi":"10.1186/s13065-018-0444-z","DOIUrl":"https://doi.org/10.1186/s13065-018-0444-z","url":null,"abstract":"<p><p>(Z,Z')-1,1'-(4-ortho-Caboranyldimethyl)-bis(2-methoxyphenylethan-1-oxime) intermediate 3 was synthesized by a three-step reaction with a final treatment with base to give a new series of ortho-carboranyl biphenyloxime derivatives (4-8). Compounds 7 and 8 showed high solubility and the in vitro study results revealed high levels of accumulation in HeLa cells with higher cytotoxicity and boron uptake compared to L-boronphenylalanine.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"76"},"PeriodicalIF":0.0,"publicationDate":"2018-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0444-z","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36271571","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: 2
In vitro antioxidant properties of the biflavonoid agathisflavone. 双类黄酮抗氧化性能的体外研究。
Chemistry Central Journal Pub Date : 2018-06-29 DOI: 10.1186/s13065-018-0443-0
Anderson Wilbur Lopes Andrade, Keylla da Conceição Machado, Katia da Conceição Machado, Daiana Dias Ribeiro Figueiredo, Jorge Mauricio David, Muhammad Torequl Islam, Shaikh Jamal Uddin, Jamil A Shilpi, Jéssica Pereira Costa
{"title":"In vitro antioxidant properties of the biflavonoid agathisflavone.","authors":"Anderson Wilbur Lopes Andrade,&nbsp;Keylla da Conceição Machado,&nbsp;Katia da Conceição Machado,&nbsp;Daiana Dias Ribeiro Figueiredo,&nbsp;Jorge Mauricio David,&nbsp;Muhammad Torequl Islam,&nbsp;Shaikh Jamal Uddin,&nbsp;Jamil A Shilpi,&nbsp;Jéssica Pereira Costa","doi":"10.1186/s13065-018-0443-0","DOIUrl":"https://doi.org/10.1186/s13065-018-0443-0","url":null,"abstract":"<p><strong>Purpose: </strong>Free radicals are considered as the causative agents of a variety of acute and chronic pathologies. Natural antioxidants have drawn attention of the researchers in recent years for their ability to scavenge free radicals with minimal or even no side effects. This study evaluates the antioxidant capacity of agathisflavone, a naturally occurring biflavonoid by a number of in vitro methods.</p><p><strong>Methods: </strong>Agathisflavone was subjected to DPPH, ABTS, OH and NO radical scavenging assay, reducing potential and inhibition of lipid peroxidation (TBARS) test using trolox as a standard.</p><p><strong>Results: </strong>Agathisflavone showed concentration-dependent antioxidant activity against all types of free radicals used in this study. The antioxidant capacity, reducing potential and inhibition of lipid peroxidation showed by agathisflavone were comparable to that of trolox.</p><p><strong>Conclusion: </strong>Agathisflavone exhibited antioxidant capacity, which suggests considering this biflavonoid for the use in the prevention and/or treatment of diseases precipitated by oxidative stress.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"75"},"PeriodicalIF":0.0,"publicationDate":"2018-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0443-0","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36271572","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: 31
Crystal structure, DFT calculations and evaluation of 2-(2-(3,4-dimethoxyphenyl)ethyl)isoindoline-1,3-dione as AChE inhibitor. 2-(2-(3,4-二甲氧基苯基)乙基)异吲哚啉-1,3-二酮作为乙酰胆碱酯酶抑制剂的晶体结构、DFT计算和评价。
Chemistry Central Journal Pub Date : 2018-06-25 DOI: 10.1186/s13065-018-0442-1
Erik Andrade-Jorge, José Bribiesca-Carlos, Francisco J Martínez-Martínez, Marvin A Soriano-Ursúa, Itzia I Padilla-Martínez, José G Trujillo-Ferrara
{"title":"Crystal structure, DFT calculations and evaluation of 2-(2-(3,4-dimethoxyphenyl)ethyl)isoindoline-1,3-dione as AChE inhibitor.","authors":"Erik Andrade-Jorge,&nbsp;José Bribiesca-Carlos,&nbsp;Francisco J Martínez-Martínez,&nbsp;Marvin A Soriano-Ursúa,&nbsp;Itzia I Padilla-Martínez,&nbsp;José G Trujillo-Ferrara","doi":"10.1186/s13065-018-0442-1","DOIUrl":"10.1186/s13065-018-0442-1","url":null,"abstract":"<p><p>Dioxoisoindolines have been included as a pharmacophore group in diverse drug-like molecules with a wide range of biological activity. Various reports have shown that phthalimide derivatives are potent inhibitors of AChE, a key enzyme involved in the deterioration of the cholinergic system during the development of Alzheimer's disease. In the present study, 2-(2-(3,4-dimethoxyphenyl)ethyl)isoindoline-1,3-dione was synthesized, crystallized and evaluated as an AChE inhibitor. The geometric structure of the crystal and the theoretical compound (from molecular modeling) were analyzed and compared, finding a close correlation. The formation of the C6-H6···O19 interaction could be responsible for the non-negligible out of phenyl plane deviation of the C19 methoxy group, the O3 from the carbonyl group lead to C16-H16···O3<sup>i</sup> intermolecular interactions to furnish C(9) and C(14) infinite chains within the (- 4 0 9) and (- 3 1 1) families of planes. Finally, the biological experiments reveal that the isoindoline-1,3-dione exerts a good competitive inhibition on AChE (Ki = 0.33-0.93 mM; 95% confidence interval) and has very low acute toxicity (LD<sub>50</sub> > 1600 mg/kg) compared to the AChE inhibitors currently approved for clinical use.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"74"},"PeriodicalIF":0.0,"publicationDate":"2018-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0442-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36253900","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: 11
Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives. 新型4,4′-(1,4-苯基)双(嘧啶-2-胺)衍生物的设计、合成、抑菌及对人大肠癌细胞系的细胞毒性研究
Chemistry Central Journal Pub Date : 2018-06-25 DOI: 10.1186/s13065-018-0440-3
Sanjiv Kumar, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah, Balasubramanian Narasimhan
{"title":"Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives.","authors":"Sanjiv Kumar,&nbsp;Siong Meng Lim,&nbsp;Kalavathy Ramasamy,&nbsp;Vasudevan Mani,&nbsp;Syed Adnan Ali Shah,&nbsp;Balasubramanian Narasimhan","doi":"10.1186/s13065-018-0440-3","DOIUrl":"https://doi.org/10.1186/s13065-018-0440-3","url":null,"abstract":"<p><strong>Background: </strong>Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies.</p><p><strong>Results: </strong>The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity using tube dilution method and anticancer activity against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B assay.</p><p><strong>Conclusions: </strong>The biological study demonstrated that compounds s7, s8, s11, s14, s16, s17 and s18 have shown more promising antimicrobial activity with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compound s3 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"73"},"PeriodicalIF":0.0,"publicationDate":"2018-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0440-3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36252307","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: 11
Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1): challenging target for antitubercular drug discovery. 十戊烯基磷酸基核糖2'-外甲酰基酶(DprE1):抗结核药物发现的挑战性靶点。
Chemistry Central Journal Pub Date : 2018-06-23 DOI: 10.1186/s13065-018-0441-2
Jineetkumar Gawad, Chandrakant Bonde
{"title":"Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1): challenging target for antitubercular drug discovery.","authors":"Jineetkumar Gawad,&nbsp;Chandrakant Bonde","doi":"10.1186/s13065-018-0441-2","DOIUrl":"https://doi.org/10.1186/s13065-018-0441-2","url":null,"abstract":"<p><p>Tuberculosis has proved harmful to the entire history of mankind from past several decades. Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1) is a recent target which was identified in 2009 but unfortunately it is neither explored nor crossed phase II. In past several decades few targets were identified for effective antitubercular drug discovery. Resistance is the major problem for effective antitubercular drug discovery. Arabinose is constituent of mycobacterium cell wall. Biosynthesis of arabinose is FAD dependant two step epimerisation reaction which is catalysed by DprE1 and DprE2 flavoprotein enzymes. The current review is mainly emphases on DprE1 as a perspective challenge for further research.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"72"},"PeriodicalIF":0.0,"publicationDate":"2018-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0441-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36252179","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: 20
Tissue-specific chemical profiling and quantitative analysis of bioactive components of Cinnamomum cassia by combining laser-microdissection with UPLC-Q/TOF-MS. 激光显微解剖与UPLC-Q/TOF-MS相结合的肉桂组织特异性化学图谱及生物活性成分定量分析
Chemistry Central Journal Pub Date : 2018-06-21 DOI: 10.1186/s13065-018-0438-x
Wenwen Zhou, Zhitao Liang, Ping Li, Zhongzhen Zhao, Jun Chen
{"title":"Tissue-specific chemical profiling and quantitative analysis of bioactive components of Cinnamomum cassia by combining laser-microdissection with UPLC-Q/TOF-MS.","authors":"Wenwen Zhou,&nbsp;Zhitao Liang,&nbsp;Ping Li,&nbsp;Zhongzhen Zhao,&nbsp;Jun Chen","doi":"10.1186/s13065-018-0438-x","DOIUrl":"https://doi.org/10.1186/s13065-018-0438-x","url":null,"abstract":"<p><strong>Background: </strong>Cinnamomi Cortex, the dried stem bark of Cinnamomum cassia Presl (Rougui in Chinese) has been widely used in traditional Chinese medicine, cooking and perfumery for thousands of years. Traditionally, the Cinnamomi Cortex of thick size is considered to be of good quality; however, there is no scientific data to support this point. Considering that essential oils are the main bioactive components, Cinnamomi Cortex of greater variety and amount essential oils is thought to be of better quality. In this study, laser microdissection coupled with ultra-high performance liquid chromatography-quadrupole/time-of-flight-mass spectrometry (UPLC-Q/TOF-MS) was applied to profile the essential oils in different tissues of Cinnamomi Cortex and to determine if there is a correlation between the essential oil content and the stem bark thickness.</p><p><strong>Results: </strong>We report the tissue-specific metabolic profiles of different grades of Cinnamomi Cortex. Nineteen chemical components were unequivocally or tentatively identified in the chromatogram of the test samples. The results indicate that the bioactive components, the essential oils, were mainly present in the phloem.</p><p><strong>Conclusion: </strong>Phloem thickness is the key character for evaluating the quality of Cinnamomi Cortex. Our results can be of great importance in improving the cultivation, harvesting, and processing of Cinnamomi Cortex, as well as enhancing its effects in clinical applications.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"71"},"PeriodicalIF":0.0,"publicationDate":"2018-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0438-x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36247964","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: 12
A facile synthesis, and antimicrobial and anticancer activities of some pyridines, thioamides, thiazole, urea, quinazoline, β-naphthyl carbamate, and pyrano[2,3-d]thiazole derivatives. 吡啶类、硫酰胺类、噻唑类、尿素类、喹唑啉类、β-氨基甲酸萘酯类和吡[2,3-d]噻唑类衍生物的简单合成及其抑菌和抗癌活性。
Chemistry Central Journal Pub Date : 2018-06-20 DOI: 10.1186/s13065-018-0439-9
Yasser H Zaki, Marwa S Al-Gendey, Abdou O Abdelhamid
{"title":"A facile synthesis, and antimicrobial and anticancer activities of some pyridines, thioamides, thiazole, urea, quinazoline, β-naphthyl carbamate, and pyrano[2,3-d]thiazole derivatives.","authors":"Yasser H Zaki,&nbsp;Marwa S Al-Gendey,&nbsp;Abdou O Abdelhamid","doi":"10.1186/s13065-018-0439-9","DOIUrl":"https://doi.org/10.1186/s13065-018-0439-9","url":null,"abstract":"<p><strong>Background: </strong>Chalcones have a place with the flavonoid family and show a few very important pharmacological activities. They can used as initial compounds for synthesis of several heterocyclic compounds. The compounds with the backbone of chalcones have been reported to possess various biological activities.</p><p><strong>Results: </strong>Pyridine and thioamide derivatives were obtained from the reaction of 3-(furan-2-yl)-1-(p-tolyl)prop-2-en-1-one with the appropriate amount of malononitrile, benzoylacetonitrile, ethyl cyanoacetate and thiosemicarbazide in the presence of ammonium acetate. The reaction of 3,5-di(furan-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide with ethyl 2-chloro-3-oxobutanoate, 3-chloropentane-2,4-dione or ethyl chloroacetate produced thiazole derivatives. Pyrano[2,3-d]thiazole derivatives were obtained as well from thiazolone to arylidene malononitrile. The structures of the title compounds were clarified by elemental analyses, and FTIR, MS and NMR spectra. Some compounds were screened against various microorganisms (i.e., bacteria +ve, bacteria -ve and fungi). We observed that compounds (3a), (4a), (4d), (5), (7) and compound (8) exhibited high cytotoxicity against the MCF-7 cell line, with IC<sub>50</sub> values of 23.6, 13.5, 15.1, 9.56, 14.2 and 23.5 μmol mL<sup>-1</sup>, respectively, while compound (9) was displayed the lowest values against MCF-7 cell lines.</p><p><strong>Conclusions: </strong>Efficient synthetic routes for some prepared pyridines, pyrazoline, thioamide, thiazoles and pyrano[2,3-d]thiazole were created. Moreover, selected newly-synthesized products were evaluated for their antitumor activity against two carcinoma cell lines: breast MCF-7 and colon HCT-116 human cancer cell lines.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"70"},"PeriodicalIF":0.0,"publicationDate":"2018-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0439-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36243432","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: 25
4-Thiazolidinone coumarin derivatives as two-component NS2B/NS3 DENV flavivirus serine protease inhibitors: synthesis, molecular docking, biological evaluation and structure-activity relationship studies. 作为双组分 NS2B/NS3 DENV 黄病毒丝氨酸蛋白酶抑制剂的 4-噻唑烷酮香豆素衍生物:合成、分子对接、生物学评价和结构-活性关系研究。
Chemistry Central Journal Pub Date : 2018-06-12 DOI: 10.1186/s13065-018-0435-0
Samina Khan Yusufzai, Hasnah Osman, Mohammad Shaheen Khan, Basma M Abd Razik, Mohammed Oday Ezzat, Suriyati Mohamad, Othman Sulaiman, Jualang Azlan Gansau, Thaigarajan Parumasivam
{"title":"4-Thiazolidinone coumarin derivatives as two-component NS2B/NS3 DENV flavivirus serine protease inhibitors: synthesis, molecular docking, biological evaluation and structure-activity relationship studies.","authors":"Samina Khan Yusufzai, Hasnah Osman, Mohammad Shaheen Khan, Basma M Abd Razik, Mohammed Oday Ezzat, Suriyati Mohamad, Othman Sulaiman, Jualang Azlan Gansau, Thaigarajan Parumasivam","doi":"10.1186/s13065-018-0435-0","DOIUrl":"10.1186/s13065-018-0435-0","url":null,"abstract":"<p><p>A series of novel 4-thiazolidinone inhibitors SKYa-SKYg, containing coumarin as a core structure were synthesized via facile and efficient method. The structures of the synthesized compounds were established by extensive spectroscopic studies (FT IR, 1D NMR, 2D NMR, LC-MS) and elemental analysis. All the synthesized hybrids were further evaluated for their potential as anti-tubercular agents against Mycobacterium tuberculosis H37Rv ATCC 25618, and anti-bacterial agents against Escherichia coli, Enterobacter aerogenes, Salmonella typhi, Streptococcus pneumoniae and Staphylococcus aureus. Interestingly, the hybrids displayed potent bioactivity. However, compounds SKYc, SKYd, and SKYe appeared to be more effective against the tested bacterial strains, among which compound SKYb showed the highest inhibition against all the bacterial strains ranging from 41 to 165 μg/mL, as compared to the standards, streptomycin, kanamycin and vancomycin. Moreover, derivative SKYa was found to be the strongest against M. tuberculosis (83 μg/mL). Additionally, the anti-dengue potential of the coumarin hybrids as two-component NS2B/NS3 DENV flavivirus serine protease inhibitors was calculated using computational molecular docking approach, with reference to the standards 4-hydroxypanduratin, panduratin and ethyl 3-(4-(hydroxymethyl)-2-methoxy-5-nitrophenoxy)propanoate with DS of - 3.379, - 3.189 and - 3.381, respectively. The docking results revealed that the synthesized hybrids exhibited potent anti-dengue activity among which compounds SKYf, SKYd, SKYc and SKYe were found to be the best ones with docking scores of - 4.014, - 3.964, - 3.905 and - 3.889. In summary, we discovered 4-thiazolidinone coumarin derivatives as a new scaffold that may eventually yield useful compounds in the treatment of bacterial and viral infections.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"69"},"PeriodicalIF":0.0,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5997609/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36217908","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
Heterocyclization of polarized system: synthesis, antioxidant and anti-inflammatory 4-(pyridin-3-yl)-6-(thiophen-2-yl) pyrimidine-2-thiol derivatives. 极化体系的杂环化:4-(吡啶-3-基)-6-(噻吩-2-基)嘧啶-2-硫醇衍生物的合成、抗氧化和抗炎。
Chemistry Central Journal Pub Date : 2018-06-08 DOI: 10.1186/s13065-018-0437-y
Wesam S Shehab, Magda H Abdellattif, Samar M Mouneir
{"title":"Heterocyclization of polarized system: synthesis, antioxidant and anti-inflammatory 4-(pyridin-3-yl)-6-(thiophen-2-yl) pyrimidine-2-thiol derivatives.","authors":"Wesam S Shehab,&nbsp;Magda H Abdellattif,&nbsp;Samar M Mouneir","doi":"10.1186/s13065-018-0437-y","DOIUrl":"https://doi.org/10.1186/s13065-018-0437-y","url":null,"abstract":"<p><strong>Background: </strong>Chalcones are intent in the daily diet as a favorable chemotherapeutic compound; on the other hand thiophene moiety is present in a large number of bioactive molecules having diverse biological efficiency.</p><p><strong>Results: </strong>Our current goal is the synthesis of (E)-1-(pyridin-3-yl)-3-(thiophen-2-yl) prop-2-en-1-one 3 that<sup>'</sup>s used as a starting compound to synthesize the novel pyrimidine-2-thiol, pyrazole, pyran derivatives. Chalcones 3 was prepared by condensation of 3-acetylpyridine with thiophene 2-carboxaldehyde which reacted with thiourea to obtain pyrimidinthiol derivative 4. Compound 4 was allowed to react with hydrazine hydrate to afford 2-hydrazinylpyrimidine derivative 5. Compound 5 was used as a key intermediate for a facile synthesis of the targets 6 and 7. In contrast, pyranone 8 was obtained by transformation of compound 5. Using as a precursor for the synthesis of new pyrazolo pyrimidine derivatives 9-10. The major incentive behind the preparation of these compounds was the immense biological activities associated to these heterocyclic derivatives.</p><p><strong>Conclusions: </strong>The newly synthesized compounds (1-4) showed potent anti-inflammatory activities both in vitro and in vivo. They also exhibited promising antioxidant vitalities against α, α-diphenyl-β-picrylhydrazyl scavenging activity and lipid peroxidation. In conclusion, compound 1 showed a hopefully anti-inflammatory and antioxidant activities.</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"68"},"PeriodicalIF":0.0,"publicationDate":"2018-06-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0437-y","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36204414","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: 21
Analysis of paracetamol, pseudoephedrine and cetirizine in Allercet Cold® capsules using spectrophotometric techniques. 用分光光度法分析Allercet Cold®胶囊中对乙酰氨基酚、伪麻黄碱和西替利嗪的含量。
Chemistry Central Journal Pub Date : 2018-06-01 DOI: 10.1186/s13065-018-0436-z
Souha H Youssef, Maha Abdel-Monem Hegazy, Dalia Mohamed, Amr Mohamed Badawey
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引用次数: 13
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