In vitro solubility, stability and permeability of novel quercetin–amino acid conjugates

Neomycin–nucleobase–amino acid conjugates bind to pre-miR-372 and inhibit Dicer-mediated processing thus leading to decreased levels of oncogenic miR-372 in vitro and in gastric adenocarcinoma cells.

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Amino Acid Conjugates of Aminothiazole and Aminopyridine as Potential Anticancer Agents: Synthesis, Molecular Docking and in vitro Evaluation

Drug Design Development and Therapy ◽

10.2147/dddt.s297013 ◽

2021 ◽

Vol Volume 15 ◽

pp. 1459-1476

Author(s):

Shagufta Naz ◽

Fawad Ali Shah ◽

Humaira Nadeem ◽

Sadia Sarwar ◽

Zhen Tan ◽

...

Keyword(s):

Molecular Docking ◽

Amino Acid ◽

Anticancer Agents ◽

In Vitro Evaluation ◽

Amino Acid Conjugates

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Design, Synthesis, Phloem Mobility, and Bioactivities of a Series of Phenazine-1-Carboxylic Acid-Amino Acid Conjugates

Molecules ◽

10.3390/molecules23092139 ◽

2018 ◽

Vol 23 (9) ◽

pp. 2139 ◽

Cited By ~ 5

Author(s):

Linhua Yu ◽

Di Huang ◽

Xiang Zhu ◽

Min Zhang ◽

Zongli Yao ◽

...

Keyword(s):

Amino Acid ◽

Carboxylic Acid ◽

Design Synthesis ◽

Phloem Sap ◽

Amino Acid Conjugates ◽

Highly Active ◽

Vascular Pathogens ◽

Phloem Mobility ◽

Active Parent

Developing fungicides with phloem mobility that can be applied to leaves to control root or vascular pathogens has long been desirable. To achieve this goal, an efficient and economical strategy involves introducing an amino acid into the existing highly active parent pesticide molecule. Hence, 12 L-phenazine-1-carboxylic acid (PCA)-amino acid conjugates 4a–l were designed and synthesized via a simple synthetic route. In vitro bioassays results showed that all synthesized compounds 4a–l exhibited certain fungicidal activities against six tested fungi. Compound 4c exhibited relatively good fungicidal activity against Rhizoctonia solani, and the EC50 value was 0.084 ± 0.006 mmol/L. The phloem mobility experiments revealed that introducing an amino acid to PCA could effectively endow PCA with phloem mobility in R. communis L. Among them, nine conjugates were found in phloem sap, and L-PCA-Valine 4d exhibited the highest phloem mobility. Analysis results from the prediction of the Kleier model indicated that an active carrier-mediated mechanism may be involved in L-PCA-amino acid conjugates—a result that needs to be confirmed and complemented with further tests. The current research provides useful data for modifying non-phloem-mobile fungicidal molecules to phloem-mobile types.

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Design, synthesis, and in vitro antiplasmodial activity of 4-aminoquinolines containing modified amino acid conjugates

Medicinal Chemistry Research ◽

10.1007/s00044-016-1555-5 ◽

2016 ◽

Vol 25 (6) ◽

pp. 1148-1162 ◽

Cited By ~ 8

Author(s):

Kondaparla Srinivasarao ◽

Pooja Agarwal ◽

Kumkum Srivastava ◽

W. Haq ◽

Sunil K. Puri ◽

...

Keyword(s):

Amino Acid ◽

Antiplasmodial Activity ◽

Design Synthesis ◽

Amino Acid Conjugates

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Electron probe x-ray microanalysis and electron microscopy of amino acid absorption and transport by the small intestine: inhibition by chemical poisons and correlation to the elemental composition of the epithelial cells

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100142311 ◽

1986 ◽

Vol 44 ◽

pp. 134-135

Author(s):

A. J. Tousimis

Keyword(s):

Small Intestine ◽

Amino Acid ◽

Epithelial Cells ◽

Elemental Composition ◽

Isotope Labeling ◽

Structural Components ◽

X Ray ◽

Human Small Intestine ◽

Transport Studies

The elemental composition of amino acids is similar to that of the major structural components of the epithelial cells of the small intestine and other tissues. Therefore, their subcellular localization and concentration measurements are not possible by x-ray microanalysis. Radioactive isotope labeling: I131-tyrosine, Se75-methionine and S35-methionine have been successfully employed in numerous absorption and transport studies. The latter two have been utilized both in vitro and vivo, with similar results in the hamster and human small intestine. Non-radioactive Selenomethionine, since its absorption/transport behavior is assumed to be the same as that of Se75- methionine and S75-methionine could serve as a compound tracer for this amino acid.

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Faculty Opinions recommendation of In vitro biosynthesis of the nonproteinogenic amino acid methoxyvinylglycine.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.733025302.793551891 ◽

2018 ◽

Author(s):

Zixin Deng ◽

Xudong Qu

Keyword(s):

Amino Acid ◽

In Vitro Biosynthesis

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

Medicinal Chemistry ◽

10.2174/1573406415666190904143852 ◽

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.

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Oxytocin analogues with non-coded amino acid residues in position 8: [8-Neopentylglycine]oxytocin and [8-cycloleucine]oxytocin

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19872317 ◽

1987 ◽

Vol 52 (9) ◽

pp. 2317-2325 ◽

Cited By ~ 5

Author(s):

Jan Hlaváček ◽

Jan Pospíšek ◽

Jiřina Slaninová ◽

Walter Y. Chan ◽

Victor J. Hruby

Keyword(s):

Amino Acid ◽

Solid Phase Synthesis ◽

Solid Phase ◽

The Other ◽

Amino Acid Residues ◽

Phase Synthesis ◽

Other Hand ◽

Fragment Condensation

[8-Neopentylglycine]oxytocin (II) and [8-cycloleucine]oxytocin (III) were prepared by a combination of solid-phase synthesis and fragment condensation. Both analogues exhibited decreased uterotonic potency in vitro, each being about 15-30% that of oxytocin. Analogue II also displayed similarly decreased uterotonic potency in vivo and galactogogic potency. On the other hand, analogue III exhibited almost the same potency as oxytocin in the uterotonic assay in vivo and in the galactogogic assay.

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Synthesis of Fragments of the Vasoactive Intestinal Peptide (VIP) and Analysis of Their Residual Biological Activities

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19951229 ◽

1995 ◽

Vol 60 (7) ◽

pp. 1229-1235 ◽

Cited By ~ 2

Author(s):

Ivana Zoulíková ◽

Ivan Svoboda ◽

Jiří Velek ◽

Václav Kašička ◽

Jiřina Slaninová ◽

...

Keyword(s):

Amino Acid ◽

Biological Activities ◽

Residual Activity ◽

Detailed Examination ◽

Amino Acid Residues ◽

Linear Peptide ◽

Zone Electrophoresis ◽

Capillary Zone

The vasoactive intestinal (poly)peptide (VIP) is a linear peptide containing 28 amino acid residues, whose primary structure indicates a low metabolic stability. The following VIP fragments, as potential metabolites, and their analogues were prepared by synthesis on a solid: [His(Dnp)1]VIP(1-10), VIP(11-14), [D-Arg12]VIP(11-14), [Lys(Pac)15,21,Arg20]VIP(15-22), and VIP(23-28). After purification, the peptides were characterized by amino acid analysis, mass spectrometry, RP HPLC, and capillary zone electrophoresis. In some tests, detailed examination of the biological activity of the substances in vivo and in vitro gave evidence of a low, residual activity of some fragments, viz. a depressoric activity in vivo for [His(Dnp)1]VIP(1-10) and a stimulating activity for the release of α-amylase in vitro and in vivo for [Lys(Pac)15,21,Arg20]VIP(15-22) and VIP(23-28).

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