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Asian Journal of Organic & Medicinal Chemistry最新文献

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Synthesis and Evaluation of Novel FluorobenzimidazoleDerivatives as Antibacterial and Antifungal Agents 新型氟苯并咪唑类抗菌及抗真菌药物的合成与评价
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p200
D. Joshi, R. Narigara, G. Jani, K. Parikh
{"title":"Synthesis and Evaluation of Novel Fluorobenzimidazole\u0000Derivatives as Antibacterial and Antifungal Agents","authors":"D. Joshi, R. Narigara, G. Jani, K. Parikh","doi":"10.14233/ajomc.2019.ajomc-p200","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p200","url":null,"abstract":"A new class of fluorobenzimidazole derivatives (IIIa-j)was synthesized to investigate their antimicrobial potential. All the compounds were prepared by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol (I). The compound I was further reacted with different derivatives of 2-chloro-N-phenylacetamide (IIa-j) prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF (solvent); resulting in formation of fluorobenzimidazoles IIIa-j. The compounds IIIa-j were characterized by spectral analysis viz. 1H NMR, 13C NMR, mass spectra, elemental analysis and IR. All these compounds were screened in vitro for their antimicrobial activity against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans). Some of the compounds exhibited promising results (in MIC) against Gram-negative bacterial strains.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"64 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91311158","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
Greens Synthesis of Antimicrobial Nanosilver using in vitro Cultured Dioscorea bulbifera 体外培养黄薯蓣合成抗菌纳米银的研究
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p205
Komal A. Joshi, Sougata Ghosh, A. Dhepe
{"title":"Greens Synthesis of Antimicrobial Nanosilver using in vitro Cultured Dioscorea bulbifera","authors":"Komal A. Joshi, Sougata Ghosh, A. Dhepe","doi":"10.14233/ajomc.2019.ajomc-p205","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p205","url":null,"abstract":"Dioscorea bulbifera is a true yam species which is famous for its medicinal values. The plant is reported to possess anti-inflammatory, antidiabetic and antitumor properties. It has also been found that the D. bulbifera tuber extract is effective in synthesizing silver nanoparticles (AgNPs) because of its unique phytochemistry However, the plant is available in the rainy season only hence in this study in vitro system for maintenance of the D. bulbifera was developed using three media combinations namely basal Murashige and Skoog medium (MS), MS medium supplemented with 5 ppm kinetin (AN) and MS medium enriched with CuSO4·5H2O (CU). Aqueous extracts of these in vitro grown plantlets were found to have significant contents of phenolics, flavonoids and starch. These extracts were found to be effective in rapid synthesis of the AgNPs in 5 h with the optimum temperature of 50 °C and salt concentration equal to 5 mM. Fourier transformed infrared spectroscopy (FTIR) analysis revealed that the polyols in these extracts are responsible for bioreduction. AgNPs synthesized from extracts of Dioscorea bulbifera were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). AgNPs from plantlets growing on MS medium were found to have the smallest size and thus showed maximum antibacterial and antibiofilm potential towards Pseudomonas aeruginosa and Vibrio harveyi. The AgNPs synthesized from the extracts of plant-lets growing on AN and CU medium were also found to be effective. The results also suggested the presence of variation in the mechanism of biofilm inhibition by AgNPs against these two bacteria as biofilm inhibition was found to be greater in Vibrio harveyi. To best of our knowledge no such study has been done before with the in vitro grown Dioscorea bulbifera.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"162 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77810762","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: 10
Formulation Development and Characterization of Rilpivirine Nanosuspension for Improved Solubility by Nanomilling 利匹韦林纳米混悬液的制备及表征
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p210
Satyanarayan Sahoo, C. B. Rao
{"title":"Formulation Development and Characterization of Rilpivirine Nanosuspension for Improved Solubility by Nanomilling","authors":"Satyanarayan Sahoo, C. B. Rao","doi":"10.14233/ajomc.2019.ajomc-p210","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p210","url":null,"abstract":"The objective of this study was to formulate and optimize a stable rilpivirine nanosuspension. In the present study, yttrium stabilized zirconium oxide beads being used as the milling media in nanomilling process. The lyophilized nanocrystals were being characterized by particle size distribution (PSD), polydispersity index (PDI), X-ray diffraction (XRD) and FTIR (Fourier transform infrared spectroscopy). Optimized nanosuspension has mean particle diameter of 266 nm, PDI of 0.158, zeta potential of 22.1 mV and spherical in shape with surface oriented stabilizer molecules. Flow properties like sedimentation volume, poura-bility with the F value of 0.94 and also the redispersability even after 4 weeks of storage was found to be satisfactory for the optimized nano-suspension. Many folds increase in solubility and rate of drug release observed, The lyophilized nanocrystals retains its crystallinity after nanomilling, stable chemically with high drug content, therefore, the developed nanosuspension would be an alternative better formulation than its conventional formulation to address its bioavailability issue. However, this should be further confirmed by appropriate techniques in vivo studies.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"108 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78635490","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
Magnetically Retrievable Cobalt Ferrite Nanoparticles as Heterogeneous Catalyst for Synthesis of 1-Oxo-hexahydroxanthenes 磁性可回收钴铁氧体纳米颗粒作为合成1-氧-六羟基蒽的非均相催化剂
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P207
M. Kukade, N. Gavade, A. Kadam, W. Chandane, K. Garadkar, A. J. Bodake
{"title":"Magnetically Retrievable Cobalt Ferrite Nanoparticles as Heterogeneous Catalyst for Synthesis of 1-Oxo-hexahydroxanthenes","authors":"M. Kukade, N. Gavade, A. Kadam, W. Chandane, K. Garadkar, A. J. Bodake","doi":"10.14233/AJOMC.2019.AJOMC-P207","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P207","url":null,"abstract":"In present study, magnetically separable cobalt ferrite nanoparticles (CoFe2O4·NPs) have been prepared by low cost chemical precipitation method and reported as reusable, proficient heterogeneous catalyst for the synthesis of 1-oxo-hexahydroxanthenes among other ferrites. The structural and morphological studies by X-ray diffraction and scanning electron microscopy confirmed the formation of CoFe2O4 nanoparticles. The current protocol evaluated a proficient catalyst for reaction between various salicylaldehydes and 1,3-diketones. The ambient reaction conditions, shorter reaction time, good to excellent yields of the products, ease of purification of the products and reusa-bility of catalyst up to five catalytic cycles without significant loss of catalytic activity making the current protocol promising for its practical application.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"198 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79983556","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: 1
Trimethylsilyl Chloride Catalyzed Highly Efficient Synthesis of Schiff Bases of Thiazole in Glycerol under Microwave Irradiation 微波辐射下三甲基硅酰氯催化甘油中噻唑席夫碱的高效合成
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P170
Mujahed Shaikh, A. Sonone, M. Farooqui, A. Durrani
{"title":"Trimethylsilyl Chloride Catalyzed Highly Efficient Synthesis of Schiff Bases of Thiazole in Glycerol under Microwave Irradiation","authors":"Mujahed Shaikh, A. Sonone, M. Farooqui, A. Durrani","doi":"10.14233/AJOMC.2019.AJOMC-P170","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P170","url":null,"abstract":"A green and environmentally benign protocol is developed for the synthesis of Schiff bases of sulphur containing compound by irradiating thiazole and pyrazole aldehyde in glycerol under microwave irradiation at 70 ºC with trimethylsilyl chloride (TMSCl) as a catalyst. The method has advantages such as excellent yield, use of green solvent, easy work-up and most important the reaction completed within 2.5 min by using TMSCl catalyst. The TMSCl is an acidic catalyst, which enhances the yield of product, reaction time (with microwave, with reflux at 75 ºC and with stirring at room temperature) which can be easily removed from reaction mask.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"72 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88749121","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: 1
Anticancer Evaluation of 1,5-Disubstituted Tetrazoles usingUgi-Azide Four-Component Reactions (UA-4CRs) 1,5-二取代四唑的四组分反应抗癌评价(ua - 4cr)
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p204
C. Pandit, P. Dholaria, K. Kapadiya
{"title":"Anticancer Evaluation of 1,5-Disubstituted Tetrazoles using\u0000Ugi-Azide Four-Component Reactions (UA-4CRs)","authors":"C. Pandit, P. Dholaria, K. Kapadiya","doi":"10.14233/ajomc.2019.ajomc-p204","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p204","url":null,"abstract":"Azide isocyanide-based multicomponent reactions allow the formation of relatively complex molecules through a one-pot synthesis. The proposed reactions have been coupled of four classes of compounds including 3-phenoxybenzaldehyde, various aromatic amines, TMS-N3 and tertiary butylisocyanide, which is known as Ugi-azide four-component reactions (UA-4CRs). It generated a diverse class of 1,5-disubstituted tetrazoles which are an important drug-like scaffold known for their ability to mimic the carcinogenic conformers used in medicinal chemistry. This work presents a concise, novel, general strategy to access a surplus of new heterocyclic scaffolds through the Ugi-azide reaction. Frequency in anticancer drug design can be partly attributed to their being extremely common in nature and there are multiple metabolic pathways and cellular processes within cancer pathology that can be susceptible to heterocycles-based drugs. The anticancer screening of derived molecules were carried out using one dose response study using NCI-60 cell-lines and found most active in breast cancer cell-lines","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"109 5 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89737928","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 of Schiff Base Indolyl-1,3,4-Oxadiazole, Thiazolidinone and Azetidinone as Efficient Antimicrobial, Antioxidant, Antituberculosis and Anticancer Agents 席夫碱吲哚-1,3,4-恶二唑、噻唑烷酮和氮杂二酮高效抗菌、抗氧化、抗结核和抗癌药物的合成
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P175
Vaijinath A. Verma, A. R. Saundane, Rajkumar S. Meti
{"title":"Synthesis of Schiff Base Indolyl-1,3,4-Oxadiazole, Thiazolidinone and Azetidinone as Efficient Antimicrobial, Antioxidant, Antituberculosis and Anticancer Agents","authors":"Vaijinath A. Verma, A. R. Saundane, Rajkumar S. Meti","doi":"10.14233/AJOMC.2019.AJOMC-P175","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P175","url":null,"abstract":"The present investigation was under-taken to synthesize the Schiff base indole derivatives bearing of 1,3,4-oxadiazole thiazolidinone and azetidinone moieties. New series of 5-(5-substituted-3-phenyl-1H-indol-2-yl)-N-[(5-substituted-2-phenyl-1H-indol-3-yl)methylene]-1,3,4-oxadiazol-2-amines and screened their biological activities. Compound 4a showed excellent antibacterial and radical scavenging activities. Compound 5a revealed efficient to antifungal activity. In addition, compound 4a was found to be most active against H37Rv strain Mycobacterium tuberculosis. In case of anticancer activity methoxy compounds 4e and 6e against all the three tumor cell lines manifested remarkable cytotoxic activity. Compounds 4e, 5e and 6e have shown strong ferrous ions (Fe3+) reducing antioxidant power (FRAP) among the compounds screened. Compound 5b showed more potent of metal chelating on Fe2+ ions activity at all concentrations.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"163 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78140393","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 Activity of Some Thiosemicarbazide 某些硫代氨基脲的合成及其生物活性研究
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p206
Rohit. R. Wakodkar, M. Farooqui, P. Kulkarni, D. D. Kayande
{"title":"Synthesis and Biological Activity of Some Thiosemicarbazide","authors":"Rohit. R. Wakodkar, M. Farooqui, P. Kulkarni, D. D. Kayande","doi":"10.14233/ajomc.2019.ajomc-p206","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p206","url":null,"abstract":"In this paper, thiosemicarbazone derivatives have been prepared from substituted aromatic aldehyde and thiosemicarbazide in presence of sodium chloride. This method is an efficient, mild, inexpensive, non-toxic and environment benign catalyst. This protocol includes the reaction followed by using sodium chloride to accelerate the reaction in aqueous ethanol. The structure of synthesized compounds were determined by IR, 1H NMR, 13C NMR and mass spectroscopies as well as the compounds were also screened for antibacterial and antifungal activity against certain Gram-negative and Gram-positive bacteria and fungal pathogens.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80798653","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 of Fabricated Polyurethane Matrix Based TiO2–HAp Material 复合聚氨酯基TiO2-HAp材料的合成
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P146
Mamta Sharma, S. Tomar
{"title":"Synthesis of Fabricated Polyurethane Matrix Based TiO2–HAp Material","authors":"Mamta Sharma, S. Tomar","doi":"10.14233/AJOMC.2019.AJOMC-P146","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P146","url":null,"abstract":"In this research work, the composition of polyurethane, titanium di oxide and hydroxyapatite were optimized to obtain a stable polymer nanocomposite microfilm with excellent flexibility and durability, through simple sol-gel synthetic method. The obtained films were further cut by nesting and formed to obtain a flawless stent structure with desirable mechanical, biocompatibility and drug delivery properties. XRD, FTIR, SEM characterizations were performed to study their physical, chemical and biocompatible properties. The tensometer tests, simulated body fluid tests and blood interaction tests showed competitive results that match the properties of conventional materials such as metals and alloys.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86976824","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
Regression Analysis and Docking Study of 4-Quinolylhydrazone Based Compounds as Antituberculosis Agents 4-喹啉腙类抗结核药物的回归分析与对接研究
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p237
C. V. Bisen, M. R. Patle, R. Patle
{"title":"Regression Analysis and Docking Study of 4-Quinolylhydrazone Based Compounds as Antituberculosis Agents","authors":"C. V. Bisen, M. R. Patle, R. Patle","doi":"10.14233/ajomc.2019.ajomc-p237","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p237","url":null,"abstract":"In present study, at the beginning, the molecules whose biological properties are known are well-thought-out as a known set for regression analysis model building purpose. Using the Datawarrior software the descriptors were calculated for known set. Novel substituted 4-hydrazinylqunoline molecules were designed, improved and their descriptors were calculated. Morever, the regression analysis model was used to determine the biological activities of these new molecules. Along with this, the inhibition studies for 1QPQ and 1KNC by molecular docking method were also carried out to validate the therapeutic nature of these molecules. Accordingly, it can be concluded that these moieties on further studies may evident to be therapeutic representative against Mycobacterium tuberculosis.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"82 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90039197","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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