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Molecules, Volume 16, Issue 5 (May 2011), Pages 3456-4327

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Open AccessArticle Chemical Composition, and Antioxidant and Antimicrobial Activities of Essential Oil of Phyllostachys heterocycla cv. Pubescens Varieties from China
Molecules 2011, 16(5), 4318-4327; https://doi.org/10.3390/molecules16054318
Received: 11 April 2011 / Revised: 14 May 2011 / Accepted: 17 May 2011 / Published: 24 May 2011
Cited by 6 | PDF Full-text (181 KB)
Abstract
The essential oils of Phyllostachys heterocycla cv. Pubescens, Phyllostachys heterocycla cv. Gracilis, Phyllostachys heterocycla cv. Heterocycla and Phyllostachys kwangsiensis leaves were obtained by steam distillation. Their chemical components were separated and identified by gas chromatography/mass spectrometry (GC/MS). Meanwhile, the effect of
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The essential oils of Phyllostachys heterocycla cv. Pubescens, Phyllostachys heterocycla cv. Gracilis, Phyllostachys heterocycla cv. Heterocycla and Phyllostachys kwangsiensis leaves were obtained by steam distillation. Their chemical components were separated and identified by gas chromatography/mass spectrometry (GC/MS). Meanwhile, the effect of scavenging free radicals of essential oil was assayed by using the DPPH·method with Trolox® as control to evaluate their antioxidant capacities. Gram-positive (Staphyloccocus aureus) and Gram-negative (Escherichia coli) were selected as the indicator microorganisms to evaluate the antimicrobial activity. Antimicrobial properties were estimated by the agar diffusion method. The results show that 63 components were separated and identified by GC/MS from these varieties of bamboo leaves. cis-3-Hexenol, whose content in cv. Pubescens, Gracilis, Heterocycla and Ph. kwangsiensis was 27.11%, 24.62%, 30.51% and 34.65%, respectively, was the main constituent. The relative content of alcohol compounds in these varieties of essential oils ranged from 39.8% to 46.64%. All of the bamboo leaf essential oils possessed certain antioxidant capacity; the corresponding IC50 values were 3.1622, 4.9353, 4.2473, and 5.4746 μL/mL, respectively. Essential oils of all tested bamboo spp. were active against Staphylococcus epidermidis and E. coli, showing a positive correlation with the essential oil concentration of 50.42-300 μL/mL. The results indicated there were no significant differences among three varieties and the related species with respect to their antioxidant and antimicrobial activities. This paper provides evidence for studying the essential composition from different varieties of bamboo leaves. Full article
(This article belongs to the collection Bioactive Compounds)
Open AccessArticle Synthesis, and Antitumor Activity of Some N1-(Coumarin-7-yl) Amidrazones and Related Congeners
Molecules 2011, 16(5), 4305-4317; https://doi.org/10.3390/molecules16054305
Received: 8 April 2011 / Revised: 9 May 2011 / Accepted: 11 May 2011 / Published: 24 May 2011
Cited by 20 | PDF Full-text (191 KB)
Abstract
A series of new N1-(coumarin-7-yl)amidrazones incorporating N-piperazines and related congeners were synthesized by reacting the hydrazonoyl chloride derived from 7-amino-4-methylcoumarin with the appropriate piperazines. The chemical structures of the newly prepared compounds were supported by elemental analyses, 1H-NMR, 13C-NMR,
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A series of new N1-(coumarin-7-yl)amidrazones incorporating N-piperazines and related congeners were synthesized by reacting the hydrazonoyl chloride derived from 7-amino-4-methylcoumarin with the appropriate piperazines. The chemical structures of the newly prepared compounds were supported by elemental analyses, 1H-NMR, 13C-NMR, and ESI-HRMS spectral data. The antitumor activity of the newly synthesized compounds was evaluated. Among all the compounds tested, 7-{2-[1-(4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)piperazin-1-yl)-2-oxopropylidene]hydrazinyl}-4-methyl-2H-chromen-2-one (3n) was the most potent against MCF-7 and K562 cells, with IC50 values of 20.2 and 9.3 μM, respectively. Full article
Open AccessArticle Transformation of Geniposide into Genipin by Immobilized β-Glucosidase in a Two-Phase Aqueous-Organic System
Molecules 2011, 16(5), 4295-4304; https://doi.org/10.3390/molecules16054295
Received: 15 February 2011 / Revised: 3 May 2011 / Accepted: 13 May 2011 / Published: 24 May 2011
Cited by 22 | PDF Full-text (278 KB)
Abstract
Genipin is the bioactive compound of geniposide and a natural cross-linking agent. In order to improve the preparation process of genipin, the hydrolysis of geniposide to genipin by immobilized β-glucosidase in an aqueous-organic two-phase system was studied. β-Glucosidase was immobilized by the crosslinking-embedding
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Genipin is the bioactive compound of geniposide and a natural cross-linking agent. In order to improve the preparation process of genipin, the hydrolysis of geniposide to genipin by immobilized β-glucosidase in an aqueous-organic two-phase system was studied. β-Glucosidase was immobilized by the crosslinking-embedding method using sodium alginate as the carrier. The optimum reaction temperature, pH value and time were 55 °C, 4.5 and 2.5 h, respectively. To reduce genipin hydrolysis and byproduct production the reaction was carried out in an aqueous-organic two-phase system comprising ethyl acetate and sodium acetate buffer. The product was analyzed by HPLC, UV, IR, and NMR. The yield of genipin was 47.81% and its purity was over 98% (HPLC). Full article
(This article belongs to the Section Natural Products Chemistry)
Open AccessArticle A Screening of a Library of T7 Phage-Displayed Peptide Identifies E2F-4 as an Etoposide-Binding Protein
Molecules 2011, 16(5), 4278-4294; https://doi.org/10.3390/molecules16054278
Received: 1 March 2011 / Revised: 22 April 2011 / Accepted: 16 May 2011 / Published: 24 May 2011
Cited by 7 | PDF Full-text (506 KB)
Abstract
Etoposide (VP-16) is an anti-tumor compound that targets topoisomerase II (top II). In this study, we have identified an alternative binding protein of etoposide by screening a library of T7 phage-displayed peptides. After four rounds of selection using a biotinylated etoposide derivative immobilized
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Etoposide (VP-16) is an anti-tumor compound that targets topoisomerase II (top II). In this study, we have identified an alternative binding protein of etoposide by screening a library of T7 phage-displayed peptides. After four rounds of selection using a biotinylated etoposide derivative immobilized on a streptavidin-coated plate, T7 phage particles that display a 16-mer peptide NSSASSRGNSSSNSVY (ETBP16) or a 10-mer NSLRKYSKLK (ETBP10) were enriched with the ratio of 40 or 11 out of the 69 clones, respectively. Binding of etoposide to these peptides was confirmed by surface plasmon resonance (SPR) analysis, which showed ETBP16 and ETBP10 to have a kinetic constant of 4.85 × 10−5 M or 6.45 × 10−5 M, respectively. ETBP16 displays similarity with the ser-rich domain in E2F-4, a transcription factor in cell cycle-regulated genes, suggesting that etoposide might interact with E2F-4 via this domain. SPR analysis confirmed the specific binding of etoposide to recombinant E2F-4 is in the order of 10−5 M. Furthermore, etoposide was shown to inhibit luciferase reporter gene expression mediated by the heterodimeric E2F-4/DP complex. Taken together, our results suggest that etoposide directly binds to E2F-4 and inhibits subsequent gene transcription mediated by heterodimeric E2F-4/DP complexes in the nucleus. Full article
(This article belongs to the collection Bioactive Compounds)
Open AccessArticle Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains
Molecules 2011, 16(5), 4264-4277; https://doi.org/10.3390/molecules16054264
Received: 25 February 2011 / Revised: 6 May 2011 / Accepted: 13 May 2011 / Published: 24 May 2011
Cited by 33 | PDF Full-text (468 KB)
Abstract
The anti-HIV-1 activity of mangiferin was evaluated. Mangiferin can inhibit HIV-1B induced syncytium formation at non-cytotoxic concentrations, with a 50% effective concentration (EC50) at 16.90 μM and a therapeutic index (TI) above 140. Mangiferin also showed good activities in
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The anti-HIV-1 activity of mangiferin was evaluated. Mangiferin can inhibit HIV-1B induced syncytium formation at non-cytotoxic concentrations, with a 50% effective concentration (EC50) at 16.90 μM and a therapeutic index (TI) above 140. Mangiferin also showed good activities in other laboratory-derived strains, clinically isolated strains and resistant HIV-1 strains. Mechanism studies revealed that mangiferin might inhibit the HIV-1 protease, but is still effective against HIV peptidic protease inhibitor resistant strains. A combination of docking and pharmacophore methods clarified possible binding modes of mangiferin in the HIV-1 protease. The pharmacophore model of mangiferin consists of two hydrogen bond donors and two hydrogen bond acceptors. Compared to pharmacophore features found in commercially available drugs, three pharmacophoric elements matched well and one novel pharmacophore element was observed. Moreover, molecular docking analysis demonstrated that the pharmacophoric elements play important roles in binding HIV-1 protease. Mangiferin is a novel nonpeptidic protease inhibitor with an original structure that represents an effective drug development strategy for combating drug resistance. Full article
(This article belongs to the Special Issue Antivirals)
Open AccessArticle Cytotoxicity and Pro-Apoptotic Activity of 2,2´-Bis[4,5-bis(4-hydroxybenzyl)-2-(4-hydroxyphenyl)cyclopent-4-en-1,3-dione], a Phenolic Cyclopentenedione Isolated from the Cyanobacterium Strain Nostoc sp. str. Lukešová 27/97
Molecules 2011, 16(5), 4254-4263; https://doi.org/10.3390/molecules16054254
Received: 14 March 2011 / Revised: 13 May 2011 / Accepted: 18 May 2011 / Published: 23 May 2011
Cited by 7 | PDF Full-text (399 KB)
Abstract
The cytotoxicity of the polyphenol 2,2´-bis[4,5-bis(4-hydroxybenzyl)-2-(4-hydroxyphenyl)cyclopent-4-en-1,3-dione], nostotrebin 6 (NOS-6), was tested under in vitro conditions using mouse fibroblasts (BALB/c cells). Identification of NOS-6 and its uptake into fibroblasts was examined by multi-stage mass spectrometry analysis with the following fragmentation pattern: MS (m/z
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The cytotoxicity of the polyphenol 2,2´-bis[4,5-bis(4-hydroxybenzyl)-2-(4-hydroxyphenyl)cyclopent-4-en-1,3-dione], nostotrebin 6 (NOS-6), was tested under in vitro conditions using mouse fibroblasts (BALB/c cells). Identification of NOS-6 and its uptake into fibroblasts was examined by multi-stage mass spectrometry analysis with the following fragmentation pattern: MS (m/z) [M+H]+ 799.1 → MS2 399.1 → MS3 305.1 → MS4 277.1. Using several cell viability assays, the IC50 of NOS-6 after 24 h incubation was found to be 8.48 ± 0.16/12.15 ± 1.96 µM (neutral red/MTT assay) which was higher than that of doxorubicin. It was found that NOS-6 is capable of inducing both types of cell death, apoptosis and necrosis in a dose-dependent manner. The biological activities of the cyclopentenediones and preliminary data on NOS-6 cytotoxicity are discussed. Full article
(This article belongs to the collection Bioactive Compounds)
Open AccessArticle In Vitro Antibacterial and Antifungal Activity of Lavandula x intermedia Emeric ex Loisel. ‘Budrovka’
Molecules 2011, 16(5), 4241-4253; https://doi.org/10.3390/molecules16054241
Received: 13 April 2011 / Revised: 18 May 2011 / Accepted: 18 May 2011 / Published: 23 May 2011
Cited by 6 | PDF Full-text (111 KB)
Abstract
This study aimed to evaluate the in vitro antibacterial and antifungal activities of Lavandula x intermedia Emeric ex Loisel. ‘Budrovka’, an indigenous Croatian cultivar of lavandin. For that purpose the activity of ethanolic extracts of flowers, inflorescence stalks and leaves against thirty one
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This study aimed to evaluate the in vitro antibacterial and antifungal activities of Lavandula x intermedia Emeric ex Loisel. ‘Budrovka’, an indigenous Croatian cultivar of lavandin. For that purpose the activity of ethanolic extracts of flowers, inflorescence stalks and leaves against thirty one strains of bacteria, yeasts, dermatophytes and moulds were studied using both the agar well diffusion and broth dilution assays. Among the investigated extracts found to be effective against a broad spectrum of microorganisms, the flower extract was considered to be the most potent one. Linalool and rosmarinic acid, as the most abundant constituents found, are very likely major contributors to the observed antimicrobial effects. The results suggest that flowers of lavandin ‘Budrovka’ could serve as a rich source of natural terpene and polyphenol antimicrobial agents. Full article
(This article belongs to the Section Natural Products Chemistry)
Open AccessArticle The Effect of Ultrasound on the Functional Properties of Wheat Gluten
Molecules 2011, 16(5), 4231-4240; https://doi.org/10.3390/molecules16054231
Received: 21 March 2011 / Revised: 13 May 2011 / Accepted: 18 May 2011 / Published: 23 May 2011
Cited by 17 | PDF Full-text (702 KB)
Abstract
In this study, the effect of ultrasound on the foaming and emulsifying properties of wheat gluten as well as its electrophoretic and rheology properties were investigated. The foam capacity and foam stability of ultrasound treated wheat gluten proteins gradually increased as the treatment
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In this study, the effect of ultrasound on the foaming and emulsifying properties of wheat gluten as well as its electrophoretic and rheology properties were investigated. The foam capacity and foam stability of ultrasound treated wheat gluten proteins gradually increased as the treatment power increased, and were more pronounced at 100% power level. Excluding those of the raw wheat gluten, the lowest emulsifying capacity values and emulsifying stability were obtained with the samples ultrasound treated at 60% power level. In general, ultrasound treatment did not cause major changes on the protein electrophoretic patterns of gluten samples at the power levels used. Ultrasound affected the storage and the loss moduli with typical U-shape alteration. Full article
Open AccessReview Synthesis, Properties Characterization and Applications of Various Organobismuth Compounds
Molecules 2011, 16(5), 4191-4230; https://doi.org/10.3390/molecules16054191
Received: 15 April 2011 / Revised: 9 May 2011 / Accepted: 12 May 2011 / Published: 20 May 2011
Cited by 19 | PDF Full-text (418 KB)
Abstract
Organobismuth chemistry was emphasized in this review article due to the low price, low toxicity and low radioactivity characteristics of bismuth. As an environmentally-friendly class of organometallic compounds, different types of organobismuth compounds have been used in organic synthesis, catalysis, materials, etc. The
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Organobismuth chemistry was emphasized in this review article due to the low price, low toxicity and low radioactivity characteristics of bismuth. As an environmentally-friendly class of organometallic compounds, different types of organobismuth compounds have been used in organic synthesis, catalysis, materials, etc. The synthesis and property characterization of many organobismuth compounds had been summarized. This review article also presented a survey of various applications of organobismuth compounds in organic transformations, as reagents or catalysts. The reactivity, reaction pathways and mechanisms of reactions with organobismuths were discussed. Less common and limiting aspects of organobismuth compounds were also briefly mentioned. Full article
(This article belongs to the Special Issue Organometallic Chemistry)
Open AccessArticle Involvement of Carbohydrate, Protein and Phenylanine Ammonia Lyase in Up-Regulation of Secondary Metabolites in Labisia pumila under Various CO2 and N2 Level
Molecules 2011, 16(5), 4172-4190; https://doi.org/10.3390/molecules16054172
Received: 8 March 2011 / Revised: 25 April 2011 / Accepted: 26 April 2011 / Published: 20 May 2011
Cited by 25 | PDF Full-text (210 KB)
Abstract
A split plot factorial 2 × 3 experiment was designed to examine and characterize the relationships among secondary metabolites (total phenolics, TP; total flavonoids, TF), carbohydrate content, C/N ratio, protein synthesis and L–phenylalanine ammonia lyase (PAL; EC 4.3.1.5) activity in the Malaysian medicinal
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A split plot factorial 2 × 3 experiment was designed to examine and characterize the relationships among secondary metabolites (total phenolics, TP; total flavonoids, TF), carbohydrate content, C/N ratio, protein synthesis and L–phenylalanine ammonia lyase (PAL; EC 4.3.1.5) activity in the Malaysian medicinal herb Labisia pumila (Blume) Fern-Vill. under different CO2 concentrations (400 = ambient and 1,200 µmol mol−1 CO2) and three levels of nitrogen fertilization (0, 90 and 270 kg N ha−1) for 15 weeks. The interaction between CO2 and nitrogen levels imposed a significant impact on plant secondary metabolite production, protein, PAL activity and fructose levels. Highest TP and TF were recorded under 1,200 µmol mol−1 CO2 when N fertilizer was not applied; lowest values were obtained at 400 µmol mol−1 CO2 fertilized with the highest N level. Concurrently, fructose contents increased tremendously. Increase in fructose content might also enhance erythose-4-phosphate production (substrate for lignin and phenolic compounds), which shares a common precursor transdalolase in the pentose phosphate pathway. PAL activity was noted to be highest under 1,200 µmol mol−1 CO2 + 0 kg N ha−1 coinciding with subsequent recording of the lowest protein content. The results implied that the increase in plant secondary metabolites production under the tested conditions might be due to diversion of phenylalanine for protein synthesis to production of secondary metabolites. It was also found that the sucrose to starch ratio was also high under high levels of nitrogen fertilization, indicating an enhanced sucrose phosphate synthase activity (SPS; EC 2.4.1.14) under such condition. Full article
(This article belongs to the Section Natural Products Chemistry)
Open AccessCommunication A Regioselective Synthesis of E-Guggulsterone
Molecules 2011, 16(5), 4165-4171; https://doi.org/10.3390/molecules16054165
Received: 18 April 2011 / Revised: 17 May 2011 / Accepted: 18 May 2011 / Published: 20 May 2011
Cited by 4 | PDF Full-text (158 KB)
Abstract
We have successfully prepared E-guggulsterone from 16,17-epoxy-pregnenolone in 84% yield over two steps via a hydrazine reduction and Oppenhauer oxidation. Additionally, isomerization was induced by heat, light (hn) and acid catalysis to convert E- guggulsterone into the corresponding Z isomer. Full article
Open AccessReview Aminolevulinic Acid (ALA) as a Prodrug in Photodynamic Therapy of Cancer
Molecules 2011, 16(5), 4140-4164; https://doi.org/10.3390/molecules16054140
Received: 3 February 2011 / Accepted: 3 May 2011 / Published: 19 May 2011
Cited by 77 | PDF Full-text (456 KB)
Abstract
Aminolevulinic acid (ALA) is an endogenous metabolite normally formed in the mitochondria from succinyl-CoA and glycine. Conjugation of eight ALA molecules yields protoporphyrin IX (PpIX) and finally leads to formation of heme. Conversion of PpIX to its downstream substrates requires the activity of
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Aminolevulinic acid (ALA) is an endogenous metabolite normally formed in the mitochondria from succinyl-CoA and glycine. Conjugation of eight ALA molecules yields protoporphyrin IX (PpIX) and finally leads to formation of heme. Conversion of PpIX to its downstream substrates requires the activity of a rate-limiting enzyme ferrochelatase. When ALA is administered externally the abundantly produced PpIX cannot be quickly converted to its final product - heme by ferrochelatase and therefore accumulates within cells. Since PpIX is a potent photosensitizer this metabolic pathway can be exploited in photodynamic therapy (PDT). This is an already approved therapeutic strategy making ALA one of the most successful prodrugs used in cancer treatment. Full article
(This article belongs to the Special Issue Prodrugs)
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Open AccessArticle Effects of Agronomic Practices on Volatile Composition of Hyssopus officinalis L. Essential Oils
Molecules 2011, 16(5), 4131-4139; https://doi.org/10.3390/molecules16054131
Received: 24 March 2011 / Revised: 6 May 2011 / Accepted: 12 May 2011 / Published: 19 May 2011
Cited by 9 | PDF Full-text (257 KB)
Abstract
The chemical composition of Hyssopus officinalis (Lamiaceae) essential oil grown in southeastern Spain was analyzed by GC-MS. Due to the high relevance of this species in the world market, the study is focused on chemical heterogeneity of different oil batches and their extraction
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The chemical composition of Hyssopus officinalis (Lamiaceae) essential oil grown in southeastern Spain was analyzed by GC-MS. Due to the high relevance of this species in the world market, the study is focused on chemical heterogeneity of different oil batches and their extraction yield, cultivated under irrigation and non-irrigation conditions and with different harvesting dates. All essential oil samples have two main terpene compounds which are pinocamphone and iso-pinocamphone, accounting for approximately 35–40% of the total oil content. Other relevant compounds were identified, with β-pinene, which accounted for 10–17% contribution to the total composition, standing out. Significant differences between their volatile composition have been observed between treatments, being limonene, (E)-β-ocimene, pinocarveol, α-pinene and β-phellandrene the compounds that contributed most to the discrimination. It was also observed that the irrigation period is the most favourable for the cultivation of hyssop in this region, specially for batch 7 which gives the highest extraction yield and the best EO quality. Full article
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Open AccessArticle The Influence of t-Butyl and Cyclododecyl Substitution on Ethylene/1-Hexene Copolymerization Using Ansa-Fluorenylamidodimethyltitanium Derivatives
Molecules 2011, 16(5), 4122-4130; https://doi.org/10.3390/molecules16054122
Received: 9 March 2011 / Revised: 9 May 2011 / Accepted: 12 May 2011 / Published: 19 May 2011
Cited by 2 | PDF Full-text (399 KB)
Abstract
In the present study, copolymerization of ethylene and 1-hexene was conducted with a series of ansa-fluorenylamidodimethyltitanium complexes, including [t-BuNSiMe2Flu]TiMe2 (complex 1), [cyclododecylNSiMe2Flu]TiMe2 (complex 2) and [t-BuNSiMe2(2,7-t-Bu2Flu)]TiMe2
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In the present study, copolymerization of ethylene and 1-hexene was conducted with a series of ansa-fluorenylamidodimethyltitanium complexes, including [t-BuNSiMe2Flu]TiMe2 (complex 1), [cyclododecylNSiMe2Flu]TiMe2 (complex 2) and [t-BuNSiMe2(2,7-t-Bu2Flu)]TiMe2 (complex 3), activated by MMAO. The effect of these catalysts on catalytic behavior, namely activity, molecular weight and monomer reactivity ratios, has been investigated. The results showed that all of them acted by a single site polymerization mechanism and the molecular weight distribution is independent of catalyst structure. Based on the study, it revealed that the introduction of a t-butyl at the 2,7 position on the fluorenyl ligand is able to enhance both catalytic activity and copolymer molecular weight more than introducing a cyclododecyl on the amine, which is probably associated with the electronic effect exerted by the t-butyl substituent. The comonomer incorporation content was controllable over a wide range by adjusting the comonomer feed ratio. Moreover, referring to monomer reactivity ratio exploration, it seems that the substitution on the ansa-fluorenylamidodimethyltitanium complex tends to hinder the insertion of 1-hexene into the polymer chain, leading to the highest 1-hexene content for traditional complex 1. Full article
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Open AccessArticle Solid-Phase Synthesis of Arylpiperazine Derivatives and Implementation of the Distributed Drug Discovery (D3) Project in the Search for CNS Agents
Molecules 2011, 16(5), 4104-4121; https://doi.org/10.3390/molecules16054104
Received: 13 April 2011 / Revised: 14 May 2011 / Accepted: 16 May 2011 / Published: 19 May 2011
Cited by 3 | PDF Full-text (318 KB)
Abstract
We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically active compounds. As an outcome
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We have successfully implemented the concept of Distributed Drug Discovery (D3) in the search for CNS agents. Herein, we demonstrate, for the first time, student engagement from different sites around the globe in the development of new biologically active compounds. As an outcome we have synthesized a 24-membered library of arylpiperazine derivatives targeted to 5-HT1A and 5-HT2A receptors. The synthesis was simultaneously performed on BAL-MBHA-PS resin in Poland and the United States, and on BAL-PS-SynPhase Lanterns in France. The D3 project strategy opens the possibility of obtaining potent 5-HT1A/5-HT2A agents in a distributed fashion. While the biological testing is still centralized, this combination of distributed synthesis with screening will enable a D3 network of students world-wide to participate, as part of their education, in the synthesis and testing of this class of biologically active compounds. Full article
(This article belongs to the Section Medicinal Chemistry)
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