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ECSOC-13
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ECSOC-13

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

Deadline for manuscript submissions: closed (31 July 2010) | Viewed by 29284

Special Issue Editor

Dr. Julio A. Seijas Vázquez

E-Mail Website
Guest Editor
Departamen to de QuímicaOrgánica, Facultad de Ciencias, Universidad de Santiago de Compostela, Avda. Alfonso X El Sabio s/n, 27002 Lugo, Spain
Interests: synthesis of compounds with biologic activity; synthesis of compounds with interest for agro-food field; solation, structural determination and synthesis of natural products; microwave organic reactions enhancement
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Published Papers (3 papers)

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Research

412 KiB  
Article
Preparation and Properties of New Co-Crystals of Ibandronate with Gluco- or Galactopyranoside Derivatives
by Zbynek Oktabec, Jiri Kos, Zuzana Mandelova, Lenka Havelkova, Tomas Pekarek, Anna Rezacova, Lukas Placek, Marcela Tkadlecova, Jaroslav Havlicek, Jiri Dohnal and Josef Jampílek
Molecules 2010, 15(12), 8973-8987; https://doi.org/10.3390/molecules15128973 - 8 Dec 2010
Cited by 8 | Viewed by 7398
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 kinetically [...] 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)
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126 KiB  
Article
Bisbenzamidines as Antifungal Agents. Are Both Amidine Functions Required to Observe an Anti-Pneumocystis carinii Activity?
by Julien Laurent, Dimitri Stanicki, Tien L. Huang, Eduardo Dei-Cas, Muriel Pottier, El Mouktar Aliouat and Jean Jacques Vanden Eynde
Molecules 2010, 15(6), 4283-4293; https://doi.org/10.3390/molecules15064283 - 11 Jun 2010
Cited by 11 | Viewed by 9059
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. Those [...] 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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224 KiB  
Article
Molecular Recognition Studies on Naphthyridine Derivatives
by José Carlos Iglesias-Sánchez, Dolores Santa María, Rosa M. Claramunt and José Elguero
Molecules 2010, 15(3), 1213-1222; https://doi.org/10.3390/molecules15031213 - 3 Mar 2010
Cited by 8 | Viewed by 12207
Abstract
The association constants Kb of three hosts I–III designed to have both enhanced hydrogen bonding donor strength and conformational preorganization with biotin analogues 1–5 are reported. 1H-NMR titrations under two different concentration conditions have been employed to [...] Read more.
The association constants Kb of three hosts I–III designed to have both enhanced hydrogen bonding donor strength and conformational preorganization with biotin analogues 1–5 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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