Biological properties of amino acid conjugates of 2,4,5-trichlorophenoxyacetic acid

1979 ◽  
Vol 27 (5) ◽  
pp. 1086-1088 ◽  
Author(s):  
Gayle H. Davidonis ◽  
Masood Arjmand ◽  
Robert H. Hamilton ◽  
Ralph O. Mumma
Keyword(s):  
Amino Acid ◽  
Biological Properties ◽  
Amino Acid Conjugates ◽  
Trichlorophenoxyacetic Acid

Synthesis, physical-chemical and biological properties of amphiphilic amino acid conjugates of nitroxides

2010 ◽  
Vol 34 (9) ◽  
pp. 1909 ◽  
Author(s):  
Grégory Durand ◽  
Fanny Choteau ◽  
Robert A. Prosak ◽  
Antal Rockenbauer ◽  
Frederick A. Villamena ◽  
...  
Keyword(s):  
Amino Acid ◽  
Biological Properties ◽  
Amino Acid Conjugates ◽  
Physical Chemical ◽  
Amphiphilic Amino Acid

scholarly journals Biological Properties of d-Amino Acid Conjugates of 2,4-D

1982 ◽  
Vol 70 (2) ◽  
pp. 357-360 ◽  
Author(s):  
Gayle H. Davidonis ◽  
Robert H. Hamilton ◽  
Remo P. Vallejo ◽  
Robert Buly ◽  
Ralph O. Mumma
Keyword(s):  
Amino Acid ◽  
Biological Properties ◽  
Amino Acid Conjugates

Quercetin-Amino Acid Conjugates are Promising Anti-Cancer Agents in Drug Discovery Projects

2020 ◽  
Vol 20 (2) ◽  
pp. 107-122 ◽  
Author(s):  
Alexey V. Dobrydnev ◽  
Tetiana M. Tkachuk ◽  
Viktor P. Atamaniuk ◽  
Maria V. Popova
Keyword(s):  
Amino Acid ◽  
Structural Diversity ◽  
Pharmacokinetic Profile ◽  
Biological Properties ◽  
Therapeutic Window ◽  
Amino Acid Conjugates ◽  
Anti Cancer ◽  
Resistance Reversal ◽  
Cellular Permeability ◽  
Physicochemical And Biological Properties

Quercetin is a plant flavonoid with great potential for the prevention and treatment of disease. Despite the curative application of quercetin is hampered by low bioavailability, its core serves as a scaffold for generating more potent compounds with amplified therapeutic window. This review aims to describe recent advances in the improvement of the pharmacokinetic profile of quercetin via the amino acid prodrug approach which offers wide structural diversity, physicochemical and biological properties improvement. According to the findings, conjugation of quercetin with amino acids results in increased solubility, stability, cellular permeability as well as biological activity. In particular quercetin- amino acid conjugates exhibited potent anticancer, MDR-reversal and antibiotic resistance reversal activities. The synthetic pathways and examples of quercetin-amino acid conjugates are considered. Practical considerations and challenges associated with the development of these prodrugs are also discussed. This mini-review covers the literature on quercetin-amino acid conjugates since 2001 when the first thematic work was published.

Fluoroquinolone-3-carboxamide Amino Acid Conjugates: Synthesis, Antibacterial Properties And Molecular Modeling Studies

2020 ◽  
Vol 17 (1) ◽  
pp. 71-84
Author(s):  
Riham M. Bokhtia ◽  
Siva S. Panda ◽  
Adel S. Girgis ◽  
Hitesh H. Honkanadavar ◽  
Tarek S. Ibrahim ◽  
...  
Keyword(s):  
Experimental Data ◽  
Antibacterial Activity ◽  
Amino Acid ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Antibacterial Properties ◽  
Computational Studies ◽  
Protecting Group ◽  
Amino Acid Conjugates ◽  
Molecular Modeling Studies

Background: Bacterial infections are considered as one of the major global health threats, so it is very essential to design and develop new antibacterial agents to overcome the drawbacks of existing antibacterial agents. Method: The aim of this work is to synthesize a series of new fluoroquinolone-3-carboxamide amino acid conjugates by molecular hybridization. We utilized benzotriazole chemistry to synthesize the desired hybrid conjugates. Result: All the conjugates were synthesized in good yields, characterized, evaluated for their antibacterial activity. The compounds were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Synthesized conjugates were tested for activity against medically relevant pathogens; Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27856) Staphylococcus aureus (ATCC 25923) and Enterococcus faecalis (ATCC 19433). Conclusion: The observed antibacterial experimental data indicates the selectivity of our synthesized conjugates against E.Coli. The protecting group on amino acids decreases the antibacterial activity. The synthesized conjugates are non-toxic to the normal cell lines. The experimental data were supported by computational studies.

Vasopressin analogues with effect on central nervous system: Synthesis and biological properties

1983 ◽  
Vol 48 (10) ◽  
pp. 2862-2873 ◽  
Author(s):  
František Brtník ◽  
Ivan Krejčí ◽  
Běla Kupková ◽  
Pavel Hrbas ◽  
Jana Škopková ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Amino Acid ◽  
Passive Avoidance ◽  
Biological Properties ◽  
Passive Avoidance Test ◽  
System Synthesis ◽  
Avoidance Test ◽  
Vasopressin Analogues

Synthesis of four vasopressin analogues which do not contain the glycinamine residue in position 9 and have a basic non-coded amino acid in position 8 is described. All the analogues exhibit very low endocrine activities and are effective in the passive avoidance test.

Biological Function and Chemistry of Endothelin. A Review

1999 ◽  
Vol 64 (8) ◽  
pp. 1211-1252 ◽  
Author(s):  
Jan Hlaváček ◽  
Renáta Marcová
Keyword(s):  
Biological Activity ◽  
Amino Acid ◽  
Biological Function ◽  
Biological Properties ◽  
Structural Basis ◽  
Amino Acid Residues ◽  
Snake Venoms ◽  
Vasoactive Peptides ◽  
Physico Chemical ◽  
Endothelin A

The first part of this review deals with the biosynthesis and a biological function of strongly vasoactive peptides named endothelins (ETs) including vasoactive intestinal contractor. Where it was useful, snake venoms sarafotoxins which are structural endothelin derivatives, were also mentioned. In the second part, an attention is paid to structural basis of the ETs biological activity, with respect to alterations of amino acid residues in the parent peptides modifying the conformation and consequently the physico-chemical and biological properties in corresponding ETs analogs. Special attention is focussed on the area of ETs receptors and their interaction with peptide and non peptide agonists and antagonists, important in designing selective inhibitors of ETs receptors potentially applicable as drugs in a medicine. A review with 182 references.

scholarly journals Nicotinamide riboside–amino acid conjugates that are stable to purine nucleoside phosphorylase

2020 ◽  
Vol 18 (15) ◽  
pp. 2877-2885
Author(s):  
Faisal Hayat ◽  
Marie E. Migaud
Keyword(s):  
Amino Acid ◽  
Acid Ester ◽  
Purine Nucleoside Phosphorylase ◽  
Amino Acid Ester ◽  
Purine Nucleoside ◽  
Nucleoside Phosphorylase ◽  
Amino Acid Conjugates ◽  
Nicotinamide Riboside

O5′ amino acid ester conjugates of nicotinamide riboside, generated via a reduced intermediate, are stable to purine nucleoside phosphorylase.

Further characterization and determination of the single amino acid change in thetsI138reovirus thermosensitive mutant

2012 ◽  
Vol 58 (5) ◽  
pp. 589-595
Author(s):  
Guy Lemay ◽  
Martin Bisaillon
Keyword(s):  
Amino Acid ◽  
Amino Acid Change ◽  
Genetic Alterations ◽  
Biological Properties ◽  
Single Amino Acid ◽  
Temperature Sensitive ◽  
Nonpermissive Temperature ◽  
Gene Encoding ◽  
Viral Particles ◽  
Single Amino Acid Change

Many temperature-sensitive mutants have been isolated in early studies of mammalian reovirus. However, the biological properties and nature of the genetic alterations remain incompletely explored for most of these mutants. The mutation harbored by the tsI138 mutant was already assigned to the L3 gene encoding the λ1 protein. In the present study, this mutant was further studied as a possible tool to establish the role of the putative λ1 enzymatic activities in viral multiplication. It was observed that synthesis of viral proteins is only marginally reduced, while it was difficult to recover viral particles at the nonpermissive temperature. A single nucleotide substitution resulting in an amino acid change was found; the position of this amino acid is consistent with a probable defect in assembly of the inner capsid at the nonpermissive temperature.

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