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March 2013
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41 Reads
a b s t r a c t Several novel cyclopropyl-rigidified c-and d-amino acids 3–4 have been prepared starting from mono-terpene (+)-3-carene 2. These compounds are proposed as chiral analogues of c-aminobutyric acid (GABA) 1 and are expected to be of interest as potential inhibitors of GABA receptors.
August 2010
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62 Reads
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17 Citations
Tetrahedron Asymmetry
Several novel cyclopropyl-rigidified γ- and δ-amino acids 3–4 have been prepared starting from monoterpene (+)-3-carene 2. These compounds are proposed as chiral analogues of γ-aminobutyric acid (GABA) 1 and are expected to be of interest as potential inhibitors of GABA receptors.
August 2010
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1,893 Reads
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104 Citations
Current Medicinal Chemistry
gamma-Amino butyric acid is an extremely important inhibitory neurotransmitter in the mammalian central nervous system and is essential for the overall balance between neuronal excitation and inhibition. It is well documented that GABA deficiency is associated with several important neurological disorders such as Huntington's chorea, Parkinson's and Alzheimer's disease and other psychiatric disorders, like anxiety, depression, pain, panic, or mania. Although, it is known that increasing the brain concentration of GABA prevents convulsions, the high polarity and flexible structure of this compound are probably responsible for its inefficiency as an anticonvulsant when administered orally or intravenously. To resolve this problem, GABA analogues are being designed. Over recent years, there has been increasing interest in the synthesis and pharmacological effect of new GABA derivatives, which can be considered as potent drugs in the treatment of neurodegenerative disorders.
April 2010
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57 Reads
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8 Citations
Tetrahedron Asymmetry
Starting from (+)-3-carene 1, several chiral fragrant compounds with the bicyclo[3.1.0]hexane system were synthesized. These compounds were used as substrates for the biotransformation with lipases as biocatalysts. Pure diastereoisomers were obtained and their absolute configuration was confirmed by X-ray crystallography. The olfactory properties of new compounds were determined.
September 2009
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26 Reads
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1 Citation
ChemInform
In this work we aimed at finding a concise method for the design of the new pharmacologically active compound 6, which is a precursor to obtaining non-protein amino acid 7 considered as GABA analogue, furthermore it can be used to construct enantiopure, conformationally restricted peptides. For this purpose the Schmidt reaction was applied.
April 2009
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55 Reads
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4 Citations
Letters in Organic Chemistry
In this work we aimed at finding a concise method for the design of the new pharmacologically active compound 6, which is a precursor to obtaining non-protein amino acid 7 considered as GABA analogue, furthermore it can be used to construct enantiopure, conformationally restricted peptides. For this purpose the Schmidt reaction was applied.
... Within the terpenoids containing an N-OH moiety, effective anticancer (Kahnt et al. 2018) and antimicrobial agents (Hertiani et al. 2010;Grishko et al. 2014) were found. Chemical modifications of monoterpenoids create a possibility of obtaining novel inhibitors of various enzymes (Gajcy et al. 2010). Librowski et al. (2001) described the strong local anaesthetic activity of hydroxyamino carane derivatives. ...
August 2010
Tetrahedron Asymmetry
... Preliminary studies on the influence of the both amino acids on the behavior of mice indicated their potential usefulness as nootropic compounds. Currently, we are engaging in the design and synthesis of new conformationally constrained cyclopropane amino derivatives , considered as GABA analogues, which we partially presented [112, 113] . The starting material was (+)-3- carene 14 (Fig. 7), a bicyclic hydrocarbon, naturally occurs in gum turpentine. ...
September 2009
ChemInform
... Preliminary studies on the influence of the both amino acids on the behavior of mice indicated their potential usefulness as nootropic compounds. Currently, we are engaging in the design and synthesis of new conformationally constrained cyclopropane amino derivatives, considered as GABA analogues, which we partially presented [112,113]. The starting material was (+)-3carene 14 (Fig. 7), a bicyclic hydrocarbon, naturally occurs in gum turpentine. ...
April 2009
Letters in Organic Chemistry
... (S/R)-1), synthesized from a side product of wood pulp processing, (+)-3carene, was treated by several commercial lipases and none was able to fully transform the preferred one, even after prolonged reaction in batch KR of (S/R)-1. 35 In terms of sensory properties, the main product (R)-2 is described as being woody-balsamic with a honey note, and the product is thus of interest to the perfume and cosmetic industry. 36 Therefore, we deemed it important to undertake studies that had several objectives: i. develop a cost-effective, high-yield continuousflow enzymatic microreactor for the KR of (S/R)-1 P. cepacia adsorptive bound to the monolithic structure, ii. ...
April 2010
Tetrahedron Asymmetry
... Given the low lipophilicity of GABA, most of the analogs that have been synthesized and reported in the literature include structural modifications with functional groups whose purpose is to increase its lipophilicity, such is the case of Pregabalin (3) [20], Vigabatrin (4) [21], and Gabapentin (5) [22] (Figure 1). In fact, Pregabalin and Baclofen include an isobutyl and phenyl group in the β-position, respectively, which increase their lipophilicity [20,23,24]. Because of this, we included these modifications in the proposed analogues in this work, as well as heterocyclic ring systems in the γ-position. ...
August 2010
Current Medicinal Chemistry
