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ONE-POT THREE-COMPONENT MICROWAVE-ASSISTED SYNTHESIS OF NOVEL THIAZOLIDINONE DERIVATIVES CONTAINING THIENO[d]PYRIMIDINE-4-ONE MOIETY AS POTENTIAL ANTIMICROBIAL AGENTS. 一锅三组分微波辅助合成新型噻唑烷酮衍生物含噻诺嘧啶-4- 1片段作为潜在抗菌剂。
Bioorganicheskaia khimiia Pub Date : 2015-05-01
I H El Azab, Sh H Abdel-Hafez
{"title":"ONE-POT THREE-COMPONENT MICROWAVE-ASSISTED SYNTHESIS OF NOVEL THIAZOLIDINONE DERIVATIVES CONTAINING THIENO[d]PYRIMIDINE-4-ONE MOIETY AS POTENTIAL ANTIMICROBIAL AGENTS.","authors":"I H El Azab,&nbsp;Sh H Abdel-Hafez","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]soxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCI M-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and.three fungal strains (Candida albicans NCIM-3471, Aspergillusfiavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 3","pages":"357-65"},"PeriodicalIF":0.0,"publicationDate":"2015-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34118705","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: 0
SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL COUMARIN DERIVATIVES AS ANTIOXIDANT AGENTS. 新型香豆素衍生物抗氧化剂的合成及生物学评价。
Bioorganicheskaia khimiia Pub Date : 2015-05-01 DOI: 10.7868/s0132342315030082
K H Randive, V Jaishree, K Santosh Patil, Kumar Patil
{"title":"SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL COUMARIN DERIVATIVES AS ANTIOXIDANT AGENTS.","authors":"K H Randive,&nbsp;V Jaishree,&nbsp;K Santosh Patil,&nbsp;Kumar Patil","doi":"10.7868/s0132342315030082","DOIUrl":"https://doi.org/10.7868/s0132342315030082","url":null,"abstract":"<p><p>Coumarins have been isolated from plants and reported for antioxidant properties. In the present study, we report synthesis of new coumarin derivatives as prospective therapeutic agents and investigate their antioxidant properties.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 3","pages":"366-74"},"PeriodicalIF":0.0,"publicationDate":"2015-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34118707","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: 0
[Creation and Study of Triterpenoid Nanoparticles and Amphiphilic meso-Arylporphyrins]. [三萜纳米颗粒和两亲性中芳基卟啉的制备与研究]。
Bioorganicheskaia khimiia Pub Date : 2015-03-01
H Q Nguyen, K A Zhdanova, V S Uvarova, N A Bragina, A F Mironov, V V Chupin, V I Svets
{"title":"[Creation and Study of Triterpenoid Nanoparticles and Amphiphilic meso-Arylporphyrins].","authors":"H Q Nguyen,&nbsp;K A Zhdanova,&nbsp;V S Uvarova,&nbsp;N A Bragina,&nbsp;A F Mironov,&nbsp;V V Chupin,&nbsp;V I Svets","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>This work is devoted to the study of nanoparticles based on amphiphilic meso-arylporphyrins and spherical amorphous nanoparticles (SANp), consisting of birch bark triterpenoids mixture. Nanoparticles were investigated by electron microscopy, dynamic light scattering, UV spectroscopy and fluorimetry. It was shown the efficiency of the inclusion of porphyrin sensitizer to the nanoparticles and the use of these nanoparticles as drug delivery system.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 2","pages":"185-94"},"PeriodicalIF":0.0,"publicationDate":"2015-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34280989","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: 0
SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL FUSED THIAZOLO[3,2A]PYRIMIDINES AS POTENTIAL ANALGESIC AND ANTI-INFLAMMATORY AGENTS. 新型融合噻唑[3,2a]嘧啶类镇痛抗炎药的合成及生物学评价。
Bioorganicheskaia khimiia Pub Date : 2015-03-01 DOI: 10.7868/s0132342315020098
Nagy M Khalifa, Mohamed A Al-Omar, Abd El-Galil E Amr, Ayman R Baiuomy, Rehab F Abdel-Rahman
{"title":"SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL FUSED THIAZOLO[3,2A]PYRIMIDINES AS POTENTIAL ANALGESIC AND ANTI-INFLAMMATORY AGENTS.","authors":"Nagy M Khalifa,&nbsp;Mohamed A Al-Omar,&nbsp;Abd El-Galil E Amr,&nbsp;Ayman R Baiuomy,&nbsp;Rehab F Abdel-Rahman","doi":"10.7868/s0132342315020098","DOIUrl":"https://doi.org/10.7868/s0132342315020098","url":null,"abstract":"<p><p>Some novel bicyclic thiazolopyrimidine derivatives bearing various substituents have been synthesized through one-pot three-component method. Structures of the target compounds were confirmed by elemental analysis and spectral data. Some selected members of the newly synthesized compounds were investigated for their analgesic and anti-inflammatory activities and revealed pronounced anti-inflammatory activity greater than that of indomethacin (reference drug).</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 2","pages":"218-26"},"PeriodicalIF":0.0,"publicationDate":"2015-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34280992","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: 0
PYRIMIDOOXADIAZINE AND TRIAZOLOPYRIMIDOOXADIAZINE DERIVATIVES: SYNTHESIS AND CYTOTOXIC EVALUATION IN HUMAN CANCER CELL LINES. 嘧啶嘧啶嘧啶和三唑嘧啶嘧啶嘧啶衍生物:人类癌细胞系的合成和细胞毒性评价。
Bioorganicheskaia khimiia Pub Date : 2015-03-01 DOI: 10.7868/s0132342315020074
Seyed-Hadi Mousavi, Hoda Atapour-Mashhad, Mehdi Bakavoli, Ali Shiri, Marzieh Akbarzadeh, Zahra Tayarani-Najaran
{"title":"PYRIMIDOOXADIAZINE AND TRIAZOLOPYRIMIDOOXADIAZINE DERIVATIVES: SYNTHESIS AND CYTOTOXIC EVALUATION IN HUMAN CANCER CELL LINES.","authors":"Seyed-Hadi Mousavi,&nbsp;Hoda Atapour-Mashhad,&nbsp;Mehdi Bakavoli,&nbsp;Ali Shiri,&nbsp;Marzieh Akbarzadeh,&nbsp;Zahra Tayarani-Najaran","doi":"10.7868/s0132342315020074","DOIUrl":"https://doi.org/10.7868/s0132342315020074","url":null,"abstract":"<p><p>In vitro antiproliferative activities of some pyrimido[4,5-e][1,3,4]oxadiazine and [1,2,4]triazolo[4',3':1,2]pyrimido[4,5-e][1,3,4]oxadiazine derivatives were examined in human malignant cancer cell lines. All synthesized compounds inhibited the growth of malignant cells in a dose dependent manner, but among them 1,5,7-trimethyl-3-phenyl-1H-[1,2,4]triazolo[4',3':1,2]pyrimido[4,5-e][1,3,4]oxadiazine and [(1,5-dimethyl-3-phenyl-1H-[1,2,4]triazolo[4',3':1,2]pyrimido[4,5-e][1,3,4]oxadiazin-7-yl)sulfanyl]acetonitrile, both with triazole moiety, were found to be more effective than other compounds; they also induced a sub-G1 peak in the flow cytometry histogram of treated cells compared to controls, indicating that apoptotic cell death is involved in toxicity they induce. The results showed that compounds with triazole moiety fused to pyrimido[4,5-e] [1,3,4]oxadiazine derivatives are more active than those bearing chlorine or pyrrolidine groups at C-7 position.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 2","pages":"227-34"},"PeriodicalIF":0.0,"publicationDate":"2015-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34280994","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: 0
SYNTHESIS AND IN VITRO ANTIMICROBIAL EVALUATION OF PIPERAZINE SUBSTITUTED QUINAZOLINE-BASED THIOUREA/THIAZOLIDINONE/CHALCONE HYBRIDS. 哌嗪取代喹唑啉基硫脲/噻唑烷酮/查尔酮复合物的合成及体外抗菌评价。
Bioorganicheskaia khimiia Pub Date : 2015-03-01
D R Shah, H P Lakum, K H Chikhalia
{"title":"SYNTHESIS AND IN VITRO ANTIMICROBIAL EVALUATION OF PIPERAZINE SUBSTITUTED QUINAZOLINE-BASED THIOUREA/THIAZOLIDINONE/CHALCONE HYBRIDS.","authors":"D R Shah,&nbsp;H P Lakum,&nbsp;K H Chikhalia","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In frames of the search for new biological entities to fight against recent drug-resistant microbial strains, we report a library of quinazoline-based thiourea/4-thiazolidinone/chalcone hybrids. The newly synthesized compounds were studied for efficacy against several bacteria (Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, and Klebsiella pneumoniae) and fungi (Candida albicans and Aspergillus clavatus) using the broth dilution technique. From the biological evaluation, (E)-3-(3,4-dimethoxyphenyl)-1-(4-((4-(4-ethylpiperazin-1-yl)quinazolin-2-yl)amino)phenyl)prop-2-en-1-one was found to be the most active analogue (microbial inhibition concentration 3.12 μg/mL) to inhibit the bacterial growth. The rest of the compounds showed equipotent efficacy (3.12-12.5 μg/mL) as compared to the standard. Final compounds were characterized by FT-IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental analysis.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 2","pages":"235-48"},"PeriodicalIF":0.0,"publicationDate":"2015-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33896672","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: 0
SYNTHESIS AND BIOLOGICAL EVALUATION OF N-(SUBSTITUTED PHENYL)-2-(5H-[1,2,4]TRIAZINO[5,6-b]INDOL-3-YLSULFANYL)ACETAMIDES AS ANTIMICROBIAL, ANTIDEPRESSANT AND ANTICONVULSANT AGENTS. N-(取代苯基)-2-(5H-[1,2,4]三嗪基[5,6-b]吲哚-3-基磺胺基)乙酰胺抗菌、抗抑郁和抗惊厥药物的合成及生物学评价。
Bioorganicheskaia khimiia Pub Date : 2015-03-01 DOI: 10.7868/s0132342315020141
N Shruthi, Boja Poojary, Vasantha Kumar, A Prathibha, Mumtaz Mohammed Hussain, B C Revanasiddappa, Himanshu Joshi
{"title":"SYNTHESIS AND BIOLOGICAL EVALUATION OF N-(SUBSTITUTED PHENYL)-2-(5H-[1,2,4]TRIAZINO[5,6-b]INDOL-3-YLSULFANYL)ACETAMIDES AS ANTIMICROBIAL, ANTIDEPRESSANT AND ANTICONVULSANT AGENTS.","authors":"N Shruthi,&nbsp;Boja Poojary,&nbsp;Vasantha Kumar,&nbsp;A Prathibha,&nbsp;Mumtaz Mohammed Hussain,&nbsp;B C Revanasiddappa,&nbsp;Himanshu Joshi","doi":"10.7868/s0132342315020141","DOIUrl":"https://doi.org/10.7868/s0132342315020141","url":null,"abstract":"<p><p>A new series of N-Aryl-2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylsulfanyl)acetamides were synthesized by condensation of tricyclic compound 2,5-dihydro-3H-[1,2,4]triazino[5,6-b]indole-3-thione with chloro N-phenylacetamides. The tricyclic compound was obtained by condensation of Isatin with thiosemicarbazide. Chloro N-phenylacetamides were obtained from different substituted anilines. Their structures were characterized by IR, 1H NMR, LC-MS and elemental analyses. Newly synthesized compounds were screened for antimicrobial, antidepressant and anticonvulsant activities. Preliminary results indicated that most of the compounds showed lesser MIC value than the standard drug used when tested for antimicrobial activity. Some of the compounds were endowed with very good antidepressant and anticonvulsant activity.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 2","pages":"249-56"},"PeriodicalIF":0.0,"publicationDate":"2015-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33896674","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: 0
ACETYLCHOLINESTERASE INHIBITION ACTIVITY OF SOME QUINOLINYL SUBSTITUTED TRIAZOLOTHIADIAZOLE DERIVATIVES. 喹啉基取代三唑噻二唑衍生物的乙酰胆碱酯酶抑制活性。
Bioorganicheskaia khimiia Pub Date : 2015-03-01 DOI: 10.7868/s0132342315020086
Muhammad Rafiq, Qamar Abbas, Muhammad Saleem, Muhammad Hanif, Ki Hwan Lee, Sung-Yum Seo
{"title":"ACETYLCHOLINESTERASE INHIBITION ACTIVITY OF SOME QUINOLINYL SUBSTITUTED TRIAZOLOTHIADIAZOLE DERIVATIVES.","authors":"Muhammad Rafiq,&nbsp;Qamar Abbas,&nbsp;Muhammad Saleem,&nbsp;Muhammad Hanif,&nbsp;Ki Hwan Lee,&nbsp;Sung-Yum Seo","doi":"10.7868/s0132342315020086","DOIUrl":"https://doi.org/10.7868/s0132342315020086","url":null,"abstract":"<p><p>A series of aralkanoic acids was converted into aralkanoic acid hydrazides through their esters formation. The aralkanoic acid hydrazides upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazinate salts, which on refluxing with aqueous hydrazine hydrate yielded 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles. The target compounds, 3-aralkyl-6-(substitutedquinolinyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, were synthesized by condensing various quinolinyl substituted carboxylic acids with 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles in phosphorus oxychloride. The structures of the newly synthesized triazolothiadiazoles were characterized by IR, 1H NMR, 13C NMR, and elemental analysis studies. The structure of one of the 5-aralkyl-4-amino-3-mercapto-1,2,4-triazoles was unambiguously deduced by single crystal X-ray diffraction analysis. All the synthesized compounds were screened for their acetylcholinesterase inhibition activities. Four of the triazolothiadiazoles exhibited excellent acetylcholinesterase inhibition activities as compared to the reference inhibitor.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 2","pages":"195-202"},"PeriodicalIF":0.0,"publicationDate":"2015-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"34280990","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: 0
Anti-inflammatory activities of some newly synthesized pyridinyl- and indazolyl benzamide derivatives. 一些新合成的吡啶基和茚唑基苯酰胺衍生物的抗炎活性。
Bioorganicheskaia khimiia Pub Date : 2015-01-01 DOI: 10.7868/s0132342314050157
Azza A Hussain, Mohamed M Abdulla, Abd-El Galil E Amr, Mohamed A Al-Omar, Ahmed F A Shalaby
{"title":"Anti-inflammatory activities of some newly synthesized pyridinyl- and indazolyl benzamide derivatives.","authors":"Azza A Hussain,&nbsp;Mohamed M Abdulla,&nbsp;Abd-El Galil E Amr,&nbsp;Mohamed A Al-Omar,&nbsp;Ahmed F A Shalaby","doi":"10.7868/s0132342314050157","DOIUrl":"https://doi.org/10.7868/s0132342314050157","url":null,"abstract":"<p><p>A series of substituted (pyridin-4-yl)phenyl-2-methoxybenzamide and their derivatives were prepared and screened for their anti-inflammatory activities. Initially the acute toxicity of the compounds was assayed via the determination of their LD50. Some of the newly synthesized compounds exhibited better pharmacological and biological responses than the reference controls with low concentrations. The structures of newly synthesized compounds were confirmed by chemical, elemental and spectroscopic evidences.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 1","pages":"102-11"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33367724","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: 0
[Synthesis and membrane protective properties of sulfanylimines based on neomenthane and isobornane thiols]. [基于甲烷和异硼烷硫醇的磺胺胺的合成及其膜保护性能]。
Bioorganicheskaia khimiia Pub Date : 2015-01-01
E S Izmest'ev, D V Sudarikov, O G Shevchenko, S A Rubtsova, A V Kutchin
{"title":"[Synthesis and membrane protective properties of sulfanylimines based on neomenthane and isobornane thiols].","authors":"E S Izmest'ev,&nbsp;D V Sudarikov,&nbsp;O G Shevchenko,&nbsp;S A Rubtsova,&nbsp;A V Kutchin","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Synthesis of sulfanylimines based on neomenthane and isobornane thiol was carried out with yields up to 85%. On the model of H2O2- and AAPH-induced hemolysis of blood erythrocytes it was found that the sulfenimines have membrane protective and antioxidant activities and inhibit the accumulation of secondary products of lipid peroxidation and oxidation of hemoglobin.</p>","PeriodicalId":9325,"journal":{"name":"Bioorganicheskaia khimiia","volume":"41 1","pages":"90-6"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33367805","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: 0
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