The Novell- andd-Amino Acid Derivatives of Hydroxyurea and Hydantoins:  Synthesis, X-ray Crystal Structure Study, and Cytostatic and Antiviral Activity Evaluations

2005 ◽  
Vol 48 (2) ◽  
pp. 475-482 ◽  
Author(s):  
Ninoslav Opačić ◽  
Monika Barbarić ◽  
Branka Zorc ◽  
Mario Cetina ◽  
Ante Nagl ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Amino Acid ◽  
Antiviral Activity ◽  
Structure Study ◽  
Amino Acid Derivatives ◽  
X Ray ◽  
Derivatives Of

α-(Disilylallenyl) α-amino acid derivatives from the Claisen rearrangement of propargyl glycinates

2009 ◽  
Vol 74 (6) ◽  
pp. 927-934 ◽  
Author(s):  
Mustafa Mohamed ◽  
Michael A. Brook
Keyword(s):  
Crystal Structure ◽  
Amino Acid ◽  
Good Yield ◽  
Claisen Rearrangement ◽  
Crystal Structure Analysis ◽  
Amino Acid Derivatives ◽  
X Ray ◽  
Sigmatropic Rearrangements ◽  
Acid Methyl ◽  
Glycine Derivatives

Silylpropargyl glycinate esters undergo [3,3]-sigmatropic rearrangements to give 2-(disilylallenyl)glycine derivatives, interesting highly functional synthons, in moderate to good yield (30 to 85%) and in high diastereoselectivity when directed by a large silylpropargyl group (9:1 to 22:1). The highly functional amino acid, methyl (R)-2-(Boc-amino)-3,5-bis(trimethylsilyl)hexa-3,4-dienoate was isolated and characterized by X-ray crystal structure analysis.

scholarly journals Novel Nucleoside Phosphoramidates as Inhibitors of HIV: Studies on the Stereochemical Requirements of the Phosphoramidate Amino Acid

1996 ◽  
Vol 7 (4) ◽  
pp. 184-188 ◽  
Author(s):  
C. McGuigan ◽  
A. Salgado ◽  
C. Yarnold ◽  
T.Y. Harries ◽  
E. De Clercq ◽  
...  
Keyword(s):  
Amino Acids ◽  
Amino Acid ◽  
Antiviral Activity ◽  
Antiviral Effect ◽  
Amino Acid Derivatives ◽  
Free Nucleotides ◽  
Nucleoside Phosphoramidates ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Marked Dependence

Novel phosphoramidate derivatives of the anti-HIV nucleoside analogue d4T were designed to act as labile membrane-soluble prodrugs of the bio-active free nucleotide d4TMP. We herein reveal the very marked dependence of the antiviral activity of these phosphoramidates upon the stereochemistry of the amino acid attached to the phosphate centre; with a strong preference for the L-stereochemistry. These phosphate triesters were shown to liberate amino acid derivatives of the nucleotide intracellularly. These novel analogues, typified by alaninyl d4T monophosphate, may act as intracellular sources of the free nucleotides. The alaninyl d4T adducts themselves exert an antiviral effect when administered extracellularly, but again with clear distinctions between the L- and D-series. This evidence indicates that extracellularly administered blocked triesters derived from L-amino acids can generate d4TMP intracellularly, by a new pathway which is highly dependent on the amino acid stereochemistry.

scholarly journals N4-amino-acid derivatives of 6-azacytidine: structure-activity relationship.

2000 ◽  
Vol 47 (1) ◽  
pp. 95-101 ◽  
Author(s):  
I Alexeeva ◽  
L Palchikovskaya ◽  
A Shalamay ◽  
L Nosach ◽  
V Zhovnovataya ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antiviral Activity ◽  
Chemical Structure ◽  
Specific Activity ◽  
Biological Properties ◽  
Activity Relationship ◽  
Amino Acid Derivatives ◽  
Condensation Method ◽  
Structure Activity ◽  
Derivatives Of

Several N4-derivatives of 6-azacytidine were synthesized using of Vorbrüggen's condensation method. Their antiviral activity with respect to the adenovirus serotypes 2 and 5 in Hep-2 cells culture was studied and primary specific activity was determined. Correlation between chemical structure of new 6-azacytidine derivatives and their biological properties is discussed.

New Derivatives of Ascomycin with Modifications in the Amino Acid Region - Synthesis and Biological Activities, and X-Ray Crystal Structure of 5,6-Dehydroascomycin

2009 ◽  
Vol 92 (5) ◽  
pp. 839-889 ◽  
Author(s):  
Murty A. R. C. Bulusu ◽  
Peter Waldstätten ◽  
Thomas Tricotet ◽  
Christophe Rochais ◽  
Andrea Steck ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Amino Acid ◽  
Biological Activities ◽  
X Ray ◽  
Amino Acid Region ◽  
Derivatives Of ◽  
Acid Region

Metallkomplexe mit biologisch wichtigen Liganden, CIV [1]. ortho-Palladierte Komplexe von N,N-Dimethyl-C-phenyl-glycinmethylester. Synthese von α-Aminosäure-Derivaten durch Insertion von Isocyaniden, CO, Alkenen und Alkinen in die Pd-C-Bindung / Metal Complexes of Biologically Important Ligands, CIV [ 1]. ortho-Palladated Complexes of N,N-Dimethyl-C-phenylglycine-methylester. Synthesis of α-Amino Acid Derivatives by Insertion of Isocyanides, CO, Alkenes, and Alkynes into the Pd-C Bond

1998 ◽  
Vol 53 (4) ◽  
pp. 448-458 ◽  
Author(s):  
Andreas Böhm ◽  
Kurt Polborn ◽  
Karlheinz Sünkel ◽  
Wolfgang Beck
Keyword(s):  
Acetic Acid ◽  
Amino Acid ◽  
Metal Complexes ◽  
Crystal Structures ◽  
Trinuclear Complex ◽  
Amino Acid Derivatives ◽  
X Ray Diffraction ◽  
X Ray ◽  
Derivatives Of ◽  
Amine Ligand

Abstract N,N-Dimethyl-C-phenylglycinemethylester reacts with Pd(OAc)2 in acetic acid to give the orthopalladated, acetato bridged complex 1. Treatment of 1 with sodium halide affords the chloro, bromo, and iodo bridged compounds [Me2NC(H)(CO2Me)C6H4PdX]2 (2a -c) (X = halide). From 2a and 1,1′-bis(diphenylphosphino)ferrocene the phosphine bridged trinuclear complex 3 is obtained. Substitution of the amine ligand of 2a by the phosphino group is observed for the reaction of 2a with Ph2PC(Me)C(Me)PPh2. Insertion of 2,6-dimethyl-phenylisocyanide, CO, alkyl-vinyl-ketones, and diphenylacetylene into the Pd-C bond o f 2a -c provides the orthosubstituted organic and organometallic derivatives of phenylglycine 6a -c, 7, 8a -b and 9a -c. The crystal structures of 1, 4a, 6a, 7 and 9a were determined by X-ray diffraction.

Synthesis and X-ray crystal structure study of the hydroxyurea and hydantoin derivatives of l-valine

2005 ◽  
Vol 66 (2) ◽  
pp. 85-93 ◽  
Author(s):  
N. Opacic ◽  
B. Zorc ◽  
M. Cetina ◽  
D. Mrvos-Sermek ◽  
S. Raic-Malic ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Structure Study ◽  
X Ray ◽  
Hydantoin Derivatives ◽  
Derivatives Of

Three Amino Acid Derivatives of Valproic Acid: Design, Synthesis, Theoretical and Experimental Evaluation as Anticancer Agents

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Amino Acid ◽  
Anticancer Agents ◽  
Experimental Evaluation ◽  
Amino Acid Derivatives ◽  
Design Synthesis ◽  
Derivatives Of
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