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Special Issue "ECSOC-13"

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A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 July 2010)

Special Issue Editor

Guest Editor
Dr. Julio A. Seijas Vázquez (Website)

Departamento de Química Orgánica, Universidad de Santiago de Compostela, Facultad de Ciencias-Campus de Lugo, Alfonso X el Sabio, 27002 Lugo, Spain
Phone: +34 982824062
Fax: +34 982 285 872
Interests: synthesis of compounds with biologic activity; synthesis of compounds with interest for agro-food field; solation, estructural determination and synthesis of natural products; microwave organic reactions enhancement

Published Papers (3 papers)

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Research

Open AccessArticle Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives
Molecules 2010, 15(12), 8973-8987; doi:10.3390/molecules15128973
Received: 22 November 2010 / Revised: 3 December 2010 / Accepted: 7 December 2010 / Published: 8 December 2010
Cited by 4 | PDF Full-text (412 KB)
Abstract
Mixtures of ibandronate monosodium salt with eleven gluco- and/or galacto-pyranoside derivatives as counterions were designed to prepare co-crystals with improved intestinal absorption. In general, gastrointestinal absorption of bisphosphonates after oral administration is approximately 1%. Co-crystals were generated by means of thermodynamically and/or [...] Read more.
Mixtures of ibandronate monosodium salt with eleven gluco- and/or galacto-pyranoside derivatives as counterions were designed to prepare co-crystals with improved intestinal absorption. In general, gastrointestinal absorption of bisphosphonates after oral administration is approximately 1%. Co-crystals were generated by means of thermodynamically and/or kinetically controlled crystallization processes. Seventy-seven prepared samples were analyzed by means of FT-NIR, FT-Raman spectrometry and solid state NMR spectroscopy. New entities of ibandronate monosodium salt with phenyl-β-d-galactopyranoside were found and characterized. The absorption of these potential new co-crystals was investigated by means of PAMPA experiments. In the present study the relationships between the chemical structures of the studied compounds required for co-crystal generation are discussed. Full article
(This article belongs to the Special Issue ECSOC-13)
Open AccessArticle Bisbenzamidines as Antifungal Agents. Are Both Amidine Functions Required to Observe an Anti-Pneumocystis carinii Activity?
Molecules 2010, 15(6), 4283-4293; doi:10.3390/molecules15064283
Received: 26 May 2010 / Revised: 1 June 2010 / Accepted: 7 June 2010 / Published: 11 June 2010
Cited by 6 | PDF Full-text (126 KB)
Abstract
A library of 19 novel 4-(4-phenylpiperazine-1-yl)benzamidines has been synthesized and evaluated in vitro against Pneumocystis carinii. Among these compounds, N-ethyl- and N-hexyl-4-(4-phenylpiperazine-1-yl)benzamidines emerged as the most promising compounds, with inhibition percentages at 10.0 µg/mL of 87% and 96%, respectively. [...] Read more.
A library of 19 novel 4-(4-phenylpiperazine-1-yl)benzamidines has been synthesized and evaluated in vitro against Pneumocystis carinii. Among these compounds, N-ethyl- and N-hexyl-4-(4-phenylpiperazine-1-yl)benzamidines emerged as the most promising compounds, with inhibition percentages at 10.0 µg/mL of 87% and 96%, respectively. Those compounds remained active at 0.1 µg/mL. Full article
(This article belongs to the Special Issue ECSOC-13)
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Open AccessArticle Molecular Recognition Studies on Naphthyridine Derivatives
Molecules 2010, 15(3), 1213-1222; doi:10.3390/molecules15031213
Received: 14 January 2010 / Revised: 8 February 2010 / Accepted: 1 March 2010 / Published: 3 March 2010
Cited by 4 | PDF Full-text (224 KB)
Abstract
The association constants Kb of three hosts IIII designed to have both enhanced hydrogen bonding donor strength and conformational preorganization with biotin analogues 15 are reported. 1H-NMR titrations under two different concentration conditions have been employed [...] Read more.
The association constants Kb of three hosts IIII designed to have both enhanced hydrogen bonding donor strength and conformational preorganization with biotin analogues 15 are reported. 1H-NMR titrations under two different concentration conditions have been employed to determine the association constants Kb. A statistical analysis using a presence absence matrix has been applied to calculate the different contributions. Hydrogen bond interactions make naphthyridine derivatives II and III potent binders and effective receptors for (+)-biotin methyl ester (1), due to the complex stabilization by additional hydrogen bonds. Full article
(This article belongs to the Special Issue ECSOC-13)
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