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International Journal of Medicinal Chemistry最新文献

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p-Sulfonic Acid Calix[4]arene as an Efficient Catalyst for One-Pot Synthesis of Pharmaceutically Significant Coumarin Derivatives under Solvent-Free Condition 对磺酸杯[4]芳烃在无溶剂条件下一锅法合成香豆素衍生物的高效催化剂
International Journal of Medicinal Chemistry Pub Date : 2015-12-20 DOI: 10.1155/2015/738202
H. Tashakkorian, M. Lakouraj, Mona Rouhi
{"title":"p-Sulfonic Acid Calix[4]arene as an Efficient Catalyst for One-Pot Synthesis of Pharmaceutically Significant Coumarin Derivatives under Solvent-Free Condition","authors":"H. Tashakkorian, M. Lakouraj, Mona Rouhi","doi":"10.1155/2015/738202","DOIUrl":"https://doi.org/10.1155/2015/738202","url":null,"abstract":"One-pot and efficient protocol for preparation of some potent pharmaceutically valuable coumarin derivatives under solvent-free condition via direct coupling using biologically nontoxic organocatalyst, calix[4]arene tetrasulfonic acid (CSA), was introduced. Calix[4]arene sulfonic acid has been incorporated lately as a magnificent and recyclable organocatalyst for the synthesis of some organic compounds. Nontoxicity, solvent-free conditions, good-to-excellent yields for pharmaceutically significant structures, and especially ease of catalyst recovery make this procedure valuable and environmentally benign.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"41 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91285551","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: 8
A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model α - 5 GABA(A)苯二氮卓类受体模型药效团的最新研究进展
International Journal of Medicinal Chemistry Pub Date : 2015-11-10 DOI: 10.1155/2015/430248
T. Clayton, M. Poe, S. Rallapalli, P. Biawat, M. Savić, J. Rowlett, G. Gallos, C. Emala, C. Kaczorowski, D. Stafford, L. Arnold, J. Cook
{"title":"A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model","authors":"T. Clayton, M. Poe, S. Rallapalli, P. Biawat, M. Savić, J. Rowlett, G. Gallos, C. Emala, C. Kaczorowski, D. Stafford, L. Arnold, J. Cook","doi":"10.1155/2015/430248","DOIUrl":"https://doi.org/10.1155/2015/430248","url":null,"abstract":"An updated model of the GABA(A) benzodiazepine receptor pharmacophore of the α5-BzR/GABA(A) subtype has been constructed prompted by the synthesis of subtype selective ligands in light of the recent developments in both ligand synthesis, behavioral studies, and molecular modeling studies of the binding site itself. A number of BzR/GABA(A) α5 subtype selective compounds were synthesized, notably α5-subtype selective inverse agonist PWZ-029 (1) which is active in enhancing cognition in both rodents and primates. In addition, a chiral positive allosteric modulator (PAM), SH-053-2′F-R-CH3 (2), has been shown to reverse the deleterious effects in the MAM-model of schizophrenia as well as alleviate constriction in airway smooth muscle. Presented here is an updated model of the pharmacophore for α5β2γ2 Bz/GABA(A) receptors, including a rendering of PWZ-029 docked within the α5-binding pocket showing specific interactions of the molecule with the receptor. Differences in the included volume as compared to α1β2γ2, α2β2γ2, and α3β2γ2 will be illustrated for clarity. These new models enhance the ability to understand structural characteristics of ligands which act as agonists, antagonists, or inverse agonists at the Bz BS of GABA(A) receptors.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"45 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87047019","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: 40
Design and synthesis of novel antileishmanial compounds. 新型抗利什曼原虫化合物的设计与合成。
International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-01-21 DOI: 10.1155/2015/302723
Melanie Loedige
{"title":"Design and synthesis of novel antileishmanial compounds.","authors":"Melanie Loedige","doi":"10.1155/2015/302723","DOIUrl":"https://doi.org/10.1155/2015/302723","url":null,"abstract":"<p><p>According to the WHO, infectious diseases, and in particular neglected tropical diseases in poor developing countries, still play a significant role in a vast number of deaths reported worldwide. Among them, leishmaniasis occurs as a complex and clinically diverse illness caused by protozoan Leishmania species which are transmitted through the bite of sandflies. They develop through a complex life cycle, from promastigotes in sandflies to amastigotes in humans. The severity of disease is determined by the type of infecting Leishmania species and also depends strongly on whether the parasite infection leads to a systemic involvement or not. Since the sensitivity towards diverse medicaments highly differs among the Leishmania species, it is advantageous to treat leishmaniasis with species-specific drugs. Towards this goal we report a synthetic methodology and characterization of novel small molecular agents active against both forms of L. major. This synthetic approach allows for rapid access to new active antileishmanial drug templates and their first derivatives in moderate to very good yields. Although the compounds reported here are bioactive, the detailed biological results are part of a more comprehensive study and will be reported separately by our collaborators. </p>","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2015 ","pages":"302723"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2015/302723","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33058134","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
Facile Synthesis, Characterization, and In Vitro Antimicrobial Screening of a New Series of 2,4,6-Trisubstituted-s-triazine Based Compounds. 2,4,6-三取代-s-三嗪类化合物的简单合成、表征及体外抗菌筛选
International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-01-31 DOI: 10.1155/2015/571836
Ravi Bhushan Singh, Nirupam Das, Md Kamaruz Zaman
{"title":"Facile Synthesis, Characterization, and In Vitro Antimicrobial Screening of a New Series of 2,4,6-Trisubstituted-s-triazine Based Compounds.","authors":"Ravi Bhushan Singh,&nbsp;Nirupam Das,&nbsp;Md Kamaruz Zaman","doi":"10.1155/2015/571836","DOIUrl":"https://doi.org/10.1155/2015/571836","url":null,"abstract":"<p><p>A series of new 2,4,6-trisubstituted-s-triazine was synthesized, assessed for antimicrobial activity, and characterized by FTIR, (1)HNMR, (13)CNMR, and elemental analysis. The tested compounds, 4d, 4g, 4h, 4k, and 4n, have shown considerable in vitro antibacterial efficacy with reference to the standard drug ciprofloxacin (MIC 3.125 μgmL(-1) against B. subtilis, E. coli, and K. pneumoniae). It was observed that compounds 4d and 4h displayed equipotent antibacterial efficacy against B. subtilis (MIC 3.125 μgmL(-1)) and S. aureus (MIC 6.25 μgmL(-1)). The studies demonstrated that the para-fluorophenylpiperazine substituted s-triazine (4n) was potent and exhibited broad spectrum antibacterial activity against S. epidermidis, K. pneumoniae, and P. aeruginosa with MIC of 6.25 μgmL(-1) and for E. coli, it showed an MIC of 3.125 μgmL(-1) equipotent with reference to the standard drug. Among all the compounds under investigation, compound 4g also demonstrated significant antifungal activity (3.125 μgmL(-1)) against C. albicans. </p>","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2015 ","pages":"571836"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2015/571836","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33156373","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: 1
Design and Synthesis of Novel Hybrid Molecules against Malaria. 新型抗疟疾杂交分子的设计与合成。
International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-02-05 DOI: 10.1155/2015/458319
Melanie Lödige, Luisa Hiersch
{"title":"Design and Synthesis of Novel Hybrid Molecules against Malaria.","authors":"Melanie Lödige,&nbsp;Luisa Hiersch","doi":"10.1155/2015/458319","DOIUrl":"https://doi.org/10.1155/2015/458319","url":null,"abstract":"<p><p>The effective treatment of malaria can be very complex: Plasmodium parasites develop in multiple stages within a complex life cycle between mosquitoes as vectors and vertebrates as hosts. For the full and effective elimination of parasites, an effective drug should be active against the earliest stages of the Plasmodium infection: liver stages (reduce the progress of the infection), blood stages (cure the clinical symptoms), and gametocytes (inhibit the transmission cycle). Towards this goal, here we report the design, the synthetic methodology, and the characterization of novel hybrid agents with combined activity against Plasmodium liver stages and blood stages and gametocytes. The divergent synthetic approach allows the access to differently linked primaquine-chloroquine hybrid templates in up to eight steps. </p>","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2015 ","pages":"458319"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2015/458319","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33098001","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
Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents. 降血糖药吡唑-3-酮衍生物的设计与合成。
International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-02-04 DOI: 10.1155/2015/670181
Prasanna A Datar, Sonali R Jadhav
{"title":"Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents.","authors":"Prasanna A Datar,&nbsp;Sonali R Jadhav","doi":"10.1155/2015/670181","DOIUrl":"https://doi.org/10.1155/2015/670181","url":null,"abstract":"<p><p>Pyrazole-3-one compounds were designed on the basis of docking studies of previously reported antidiabetic pyrazole compounds. The amino acid residues found during docking studies were used as guidelines for the modification of aromatic substitutions on pyrazole-3-one structure. Depending on the docking score, the designed compounds were selectively prioritized for synthesis. The synthesized compounds were subjected to in vivo hypoglycemic activity using alloxan induced diabetic rats and metformin as a standard. Compound 4 having sulphonamide derivative was found to be the most potent compound among the series. </p>","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2015 ","pages":"670181"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2015/670181","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33098002","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
Synthesis and biological activity of arylspiroborate salts derived from caffeic Acid phenethyl ester. 咖啡酸苯乙酯衍生物芳基螺硼酸盐的合成及生物活性研究。
International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-03-05 DOI: 10.1155/2015/418362
Martin J G Hébert, Andrew J Flewelling, Trevor N Clark, Natalie A Levesque, Jacques Jean-François, Marc E Surette, Christopher A Gray, Christopher M Vogels, Mohamed Touaibia, Stephen A Westcott
{"title":"Synthesis and biological activity of arylspiroborate salts derived from caffeic Acid phenethyl ester.","authors":"Martin J G Hébert,&nbsp;Andrew J Flewelling,&nbsp;Trevor N Clark,&nbsp;Natalie A Levesque,&nbsp;Jacques Jean-François,&nbsp;Marc E Surette,&nbsp;Christopher A Gray,&nbsp;Christopher M Vogels,&nbsp;Mohamed Touaibia,&nbsp;Stephen A Westcott","doi":"10.1155/2015/418362","DOIUrl":"https://doi.org/10.1155/2015/418362","url":null,"abstract":"<p><p>Two novel boron compounds containing caffeic acid phenethyl ester (CAPE) derivatives have been prepared and characterized fully. These new compounds and CAPE have been investigated for potential antioxidant and antimicrobial properties and their ability to inhibit 5-lipoxygenase and whether chelation to boron improves their biological activity. Sodium salt 4 was generally more active than ammonium salt 5 in the biological assays and surpassed the radical scavenging ability of CAPE. Compounds 4 and 5 were more active than CAPE and Zileuton in human polymorphonuclear leukocytes. These results clearly show the effectiveness of the synthesized salts as transporter of CAPE. </p>","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2015 ","pages":"418362"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2015/418362","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33182963","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
Significance and biological importance of pyrimidine in the microbial world. 嘧啶在微生物界的意义和生物学意义。
International Journal of Medicinal Chemistry Pub Date : 2014-01-01 Epub Date: 2014-03-23 DOI: 10.1155/2014/202784
Vinita Sharma, Nitin Chitranshi, Ajay Kumar Agarwal
{"title":"Significance and biological importance of pyrimidine in the microbial world.","authors":"Vinita Sharma, Nitin Chitranshi, Ajay Kumar Agarwal","doi":"10.1155/2014/202784","DOIUrl":"10.1155/2014/202784","url":null,"abstract":"<p><p>Microbes are unique creatures that adapt to varying lifestyles and environment resistance in extreme or adverse conditions. The genetic architecture of microbe may bear a significant signature not only in the sequences position, but also in the lifestyle to which it is adapted. It becomes a challenge for the society to find new chemical entities which can treat microbial infections. The present review aims to focus on account of important chemical moiety, that is, pyrimidine and its various derivatives as antimicrobial agents. In the current studies we represent more than 200 pyrimidines as antimicrobial agents with different mono-, di-, tri-, and tetrasubstituted classes along with in vitro antimicrobial activities of pyrimidines derivatives which can facilitate the development of more potent and effective antimicrobial agents. </p>","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2014 ","pages":"202784"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2014/202784","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32804740","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: 184
Mannich bases: an important pharmacophore in present scenario. 曼尼希碱:一种重要的药效团。
International Journal of Medicinal Chemistry Pub Date : 2014-01-01 Epub Date: 2014-11-12 DOI: 10.1155/2014/191072
Suman Bala, Neha Sharma, Anu Kajal, Sunil Kamboj, Vipin Saini
{"title":"Mannich bases: an important pharmacophore in present scenario.","authors":"Suman Bala,&nbsp;Neha Sharma,&nbsp;Anu Kajal,&nbsp;Sunil Kamboj,&nbsp;Vipin Saini","doi":"10.1155/2014/191072","DOIUrl":"https://doi.org/10.1155/2014/191072","url":null,"abstract":"Mannich bases are the end products of Mannich reaction and are known as beta-amino ketone carrying compounds. Mannich reaction is a carbon-carbon bond forming nucleophilic addition reaction and is a key step in synthesis of a wide variety of natural products, pharmaceuticals, and so forth. Mannich reaction is important for the construction of nitrogen containing compounds. There is a number of aminoalkyl chain bearing Mannich bases like fluoxetine, atropine, ethacrynic acid, trihexyphenidyl, and so forth with high curative value. The literature studies enlighten the fact that Mannich bases are very reactive and recognized to possess potent diverse activities like anti-inflammatory, anticancer, antifilarial, antibacterial, antifungal, anticonvulsant, anthelmintic, antitubercular, analgesic, anti-HIV, antimalarial, antipsychotic, antiviral activities and so forth. The biological activity of Mannich bases is mainly attributed to α, β-unsaturated ketone which can be generated by deamination of hydrogen atom of the amine group.","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2014 ","pages":"191072"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2014/191072","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32882128","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: 69
Docking studies and biological activity of fosinopril analogs. 福辛普利类似物的对接研究及其生物活性。
International Journal of Medicinal Chemistry Pub Date : 2014-01-01 Epub Date: 2014-07-06 DOI: 10.1155/2014/721834
Jayant Choudary, Suvarna G Kini, Sreedhara Ranganath Pai Karkala, Muhammad Mubeen
{"title":"Docking studies and biological activity of fosinopril analogs.","authors":"Jayant Choudary,&nbsp;Suvarna G Kini,&nbsp;Sreedhara Ranganath Pai Karkala,&nbsp;Muhammad Mubeen","doi":"10.1155/2014/721834","DOIUrl":"https://doi.org/10.1155/2014/721834","url":null,"abstract":"<p><p>The purpose of the present study was to determine the angiotensin-I converting enzyme inhibitory activity of few novel Fosinopril derivatives which were predicted to possess better ACE inhibitory activity and lesser side effects than the existing drug molecule. In vitro study was carried out to determine ACE inhibitory activity of six different Fosinopril analogs by spectrophotometric assay procedure. Analog A2 showed the highest activity compared to other analogs and as well as Fosinopril itself. Docking studies of the compounds were done with the help of VLife MDS 3.0 software using GRIP batch docking method to find out which derivative had a better docking with ACE. The compounds which showed the highest negative score in docking have also exhibited good ACE inhibitory activity. </p>","PeriodicalId":14082,"journal":{"name":"International Journal of Medicinal Chemistry","volume":"2014 ","pages":"721834"},"PeriodicalIF":0.0,"publicationDate":"2014-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2014/721834","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32803660","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
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