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Molecules, Volume 8, Issue 11 (November 2003), Pages 756-865

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Research

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Open AccessArticle Synthesis and Biological Evaluation of Quinazoline-4-thiones
Molecules 2003, 8(11), 756-769; doi:10.3390/81100756
Received: 25 August 2003 / Revised: 30 September 2003 / Accepted: 30 September 2003 / Published: 15 November 2003
Cited by 10 | PDF Full-text (301 KB) | HTML Full-text | XML Full-text
Abstract
Several 2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thiones and 2-methyl-3-phenylquinazoline-4(3H)-thiones were synthesized and tested for their antimycobacterial, photosynthesis-inhibiting, and antialgal activity. Antimycobacterially active compounds were found among the 6-chloro substituted compounds. 6-Chloro-3-(4-isopropylphenyl)-2-methylquinazoline-4(3H)-thione exhibited higher activity than the isoniazid standard against Mycobacterium avium and M. kansasii. Most of [...] Read more.
Several 2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thiones and 2-methyl-3-phenylquinazoline-4(3H)-thiones were synthesized and tested for their antimycobacterial, photosynthesis-inhibiting, and antialgal activity. Antimycobacterially active compounds were found among the 6-chloro substituted compounds. 6-Chloro-3-(4-isopropylphenyl)-2-methylquinazoline-4(3H)-thione exhibited higher activity than the isoniazid standard against Mycobacterium avium and M. kansasii. Most of the compounds possessed photosynthesis-inhibiting activity. 6-Chloro-2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thione and its 3´-chloro- and 3´,4´-dichloro analogs were most effective in the inhibition of oxygen evolution rate in spinach chloroplasts. Of compounds selected for toxicological screening, 6-chloro-3-(4-isopropylphenyl)-2-methyl-quinazoline-4(3H)-thione was the only one active in the brine shrimp bioassay. Full article
Open AccessArticle Structure of Sulfated Monosaccharides Studied by Quantum Chemical Methods
Molecules 2003, 8(11), 770-779; doi:10.3390/81100770
Received: 21 May 2003 / Revised: 15 October 2003 / Accepted: 20 October 2003 / Published: 15 November 2003
Cited by 4 | PDF Full-text (127 KB) | HTML Full-text | XML Full-text
Abstract Ab initio and DFT analysis have been used to study of geometry of sulfated monosaccharides GlcN,6-SO3- and IdoA 2-SO3- in solvent. The computed low conformational barrier between the interconverting conformers of the IdoA 2-SO3- residue is in agreement with experimental data. Full article
Open AccessArticle Synthesis and X-Ray Structure of [N,N-Bis(3,5-dimethylpyrazol-1-ylmethyl)-1-hydroxy-2-aminoethane](3,5-dimethylpyrazole) copper(II) dinitrate
Molecules 2003, 8(11), 780-787; doi:10.3390/81100780
Published: 15 November 2003
Cited by 13 | PDF Full-text (57 KB) | HTML Full-text | XML Full-text
Abstract
The tridentate ligand N,N-Bis(3,5-dimethylpyrazol-1-ylmethyl)-1-hydroxy-2-aminoethane (L) has been prepared in one step by condensation of two equivalents of 1-hydroxymethyl-3,5-dimethylpyrazole with one equivalent of 2-aminoethanol. This reaction is carried out under microwave irradiation (60 W) in the absence of solvent for 20 min [1]. [...] Read more.
The tridentate ligand N,N-Bis(3,5-dimethylpyrazol-1-ylmethyl)-1-hydroxy-2-aminoethane (L) has been prepared in one step by condensation of two equivalents of 1-hydroxymethyl-3,5-dimethylpyrazole with one equivalent of 2-aminoethanol. This reaction is carried out under microwave irradiation (60 W) in the absence of solvent for 20 min [1]. Using this ligand L a new Cu(II) dinitrate complex has been prepared. The singlecrystal X-ray structure of the title compound, [N,N-bis(3,5-dimethylpyrazol-1-ylmethyl)-1-hydroxy-2-aminoethane] (3,5-dimethylpyrazole)copper(II) dinitrate, revels that the copper (II) ion is coordinated to two pyrazole nitrogens, one tertiary amine nitrogen of the ligand L and 3,5-dimethylpyrazole, and in the apical position by an alcohol O atom. Full article
Open AccessArticle Synthesis and Characterization of Chiral Nitrobenzaldehyde - Schiff Base Ligands
Molecules 2003, 8(11), 788-792; doi:10.3390/81100788
Received: 10 June 2003 / Revised: 15 August 2003 / Accepted: 18 August 2003 / Published: 15 November 2003
Cited by 3 | PDF Full-text (53 KB) | HTML Full-text | XML Full-text
Abstract Three chiral nitrobenzaldehyde/Schiff base ligands (2a-c) were prepared by the reaction of ortho, meta, and para-NO2 substituted benzaldehydes (1a-c) with (1R,2R)-(-)-1,2-diaminocyclohexane. The structures of ligands 2a-c were characterized by IR, 1H-NMR, 13C-NMR and elemental analysis. Full article

Review

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Open AccessReview The Chemistry of α-Haloketones and Their Utility in Heterocyclic Synthesis
Molecules 2003, 8(11), 793-865; doi:10.3390/81100793
Received: 21 June 2003 / Revised: 15 August 2003 / Accepted: 18 August 2003 / Published: 15 November 2003
Cited by 75 | PDF Full-text (509 KB) | HTML Full-text | XML Full-text
Abstract The molecular structures and spectral properties of α-haloketones as well as their syntheses are analyzed and reviewed. Their reactivity towards oxygen, nitrogen, and sulfur nucleophiles, carboxylic acids, carbon nucleophiles, alkenes, and alkynes are discussed. Full article

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