scholarly journals Amino acids and derivatives of thiazole-4-carboxylic acid as constituents of thiopeptin B.

1977 ◽  
Vol 30 (5) ◽  
pp. 383-387 ◽  
Author(s):  
ICHIRO MURAMATSU ◽  
YOSHIAKI MOTOKI ◽  
MASAAKI AOYAMA ◽  
HIDEO SUZUKI
Keyword(s):  
Amino Acids ◽  
Carboxylic Acid ◽  
Amino Acids And Derivatives ◽  
Derivatives Of

FORMATION OF UREA IN LIVER HOMOGENATES FROM CITRULLINE AND VARIOUS N-ALKYL DERIVATIVES OF ASPARTIG ACID

1963 ◽  
Vol 41 (1) ◽  
pp. 2297-2305 ◽  
Author(s):  
R. Charbonneau ◽  
L. Berlinguet
Keyword(s):  
Amino Acids ◽  
Carboxylic Acid ◽  
Aspartic Acid ◽  
Metabolic Pathways ◽  
Inhibitory Effect ◽  
Urea Synthesis ◽  
Alkyl Derivatives ◽  
Amino Acid Analogues ◽  
Liver Homogenates ◽  
Derivatives Of

The effects of various N-alkylated derivatives of aspartic acid on the synthesis of urea by rat liver homogenates have been studied. At 5 × 10−3 M concentration, N-methyl, N-ethyl, N-isopropyl, and N-cyclohexyl aspartic acids are not utilized and have no effect on the formation of urea. At this concentration, N-allyl-DL-aspartic acid inhibits the formation of endogenous urea by 77%. At concentrations of 2.5 to 7.5 × 10−2 M, N-methyl, N-ethyl, and N-isopropyl aspartic acids slightly increase the formation of endogenous urea; this is about 15% of the value obtained when aspartic acid alone is added at the same concentration. In the case of simple N-alkylated aspartic acids, liver homogenates are able to cleave the alkylated chain with the result that a small amount of urea synthesis is possible. N-allylaspartic acid totally inhibits the formation of urea from aspartic acid at a relatively low concentration of 6.2 × 10−3 M. N-cyclohexylaspartic acid has also an inhibitory effect which is ten times less pronounced than that of the N-allyl derivative.Natural amino acids such as DL- and L-valine, DL- and L-leucine, DL- and L-lysine, DL-alanine and glycine, at concentrations of 1.2 to 5 × 10−2 M, also inhibit the formation of urea. This inhibition is probably due to the fact that other metabolic pathways, used by these amino acids, have priority over the formation of urea. Amino acid analogues, such as 1-aminocyclopentane carboxylic acid and 1-amino-2-methylcyclopentane-carboxylic acid, do not have any effect on the synthesis of urea.A free amino group in the aspartic acid molecule seems to be essential for the synthesis of argininosuccinic acid.

On the synthesis of 3,4-dihydroxyprolines. I. cis-Glycolation of 3,4-dehydroproline derivatives

1968 ◽  
Vol 21 (3) ◽  
pp. 769 ◽  
Author(s):  
CB Hudson ◽  
AV Robertson ◽  
WRJ Simpson
Keyword(s):  
Amino Acids ◽  
Carboxylic Acid ◽  
Free Amino Acids ◽  
Free Amino ◽  
High Yields ◽  
Proline Derivatives ◽  
Derivatives Of

The interaction of OsO4 and protected derivatives of 3,4-dehydro-DL-proline gives high yields of 2,3-trans-3,4-cis-3,4-dihydroxy-DL-proline derivatives, with only traces of the 2,3-cis-3,4-cis diastereoisomers. Corresponding α-glycolation with KMnO4 gives mixtures of the 2,3-trans-3,4-cis and 2,3-cis-3,4-cis isomers in the ratio 1 : 1. Separation of the components of such mixtures is extremely difficult. The free amino acids in these two families of the 3,4-dihydroxy-DL-prolines have been characterized. Epimerization at C2 of 2,3-cis derivatives occurs readily. O-Tosylation of the 2,3-cis series occurs more readily than for other hydroxyprolines. Esters of N,O,O-tritosyl-2,3-trans-3,4-cis-3,4-dihydroxyproline are converted very rapidly by mild alkali into the equivalent esters of X-tosylpyrrole-2-carboxylic acid. For the corresponding N,O,O-tritosyl carboxylic acid, decarboxylation also takes place during aromatization, to yield N-tosylpyrrole.

FORMATION OF UREA IN LIVER HOMOGENATES FROM CITRULLINE AND VARIOUS N-ALKYL DERIVATIVES OF ASPARTIG ACID

1963 ◽  
Vol 41 (11) ◽  
pp. 2297-2305 ◽  
Author(s):  
R. Charbonneau ◽  
L. Berlinguet
Keyword(s):  
Amino Acids ◽  
Carboxylic Acid ◽  
Aspartic Acid ◽  
Metabolic Pathways ◽  
Inhibitory Effect ◽  
Urea Synthesis ◽  
Alkyl Derivatives ◽  
Amino Acid Analogues ◽  
Liver Homogenates ◽  
Derivatives Of

The effects of various N-alkylated derivatives of aspartic acid on the synthesis of urea by rat liver homogenates have been studied. At 5 × 10−3 M concentration, N-methyl, N-ethyl, N-isopropyl, and N-cyclohexyl aspartic acids are not utilized and have no effect on the formation of urea. At this concentration, N-allyl-DL-aspartic acid inhibits the formation of endogenous urea by 77%. At concentrations of 2.5 to 7.5 × 10−2 M, N-methyl, N-ethyl, and N-isopropyl aspartic acids slightly increase the formation of endogenous urea; this is about 15% of the value obtained when aspartic acid alone is added at the same concentration. In the case of simple N-alkylated aspartic acids, liver homogenates are able to cleave the alkylated chain with the result that a small amount of urea synthesis is possible. N-allylaspartic acid totally inhibits the formation of urea from aspartic acid at a relatively low concentration of 6.2 × 10−3 M. N-cyclohexylaspartic acid has also an inhibitory effect which is ten times less pronounced than that of the N-allyl derivative.Natural amino acids such as DL- and L-valine, DL- and L-leucine, DL- and L-lysine, DL-alanine and glycine, at concentrations of 1.2 to 5 × 10−2 M, also inhibit the formation of urea. This inhibition is probably due to the fact that other metabolic pathways, used by these amino acids, have priority over the formation of urea. Amino acid analogues, such as 1-aminocyclopentane carboxylic acid and 1-amino-2-methylcyclopentane-carboxylic acid, do not have any effect on the synthesis of urea.A free amino group in the aspartic acid molecule seems to be essential for the synthesis of argininosuccinic acid.

scholarly journals Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

2021 ◽  
Vol 11 (3) ◽  
pp. 1180
Author(s):  
Kinga Paruch ◽  
Łukasz Popiołek ◽  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Malm ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acid ◽  
Bacterial Infections ◽  
Acid Hydrazide ◽  
Antimicrobial Effect ◽  
In Vitro Antimicrobial Activity ◽  
Research Goal ◽  
New Compounds ◽  
Derivatives Of

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

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