Direct diversification of unmasked quinazolin-4(3H)-ones through orthogonal reactivity modulation

2017 ◽  
Vol 53 (75) ◽  
pp. 10394-10397 ◽  
Author(s):  
Jae Bin Lee ◽  
Mi Eun Kang ◽  
Joohee Kim ◽  
Chang Young Lee ◽  
Jung-Min Kee ◽  
...  
Keyword(s):  
Synthetic Analogues ◽  
Reactivity Modulation

An orthogonal reactivity modulation strategy affords diverse synthetic analogues from unmasked quinazolin-4(3H)-ones.

Semi-synthesis as a tool for broadening the health applications of bioactive olive secoiridoids: a critical review

2021 ◽  
Author(s):  
Manuela Oliverio ◽  
Monica Nardi ◽  
Maria Luisa Di Gioia ◽  
Paola Costanzo ◽  
Sonia Bonacci ◽  
...  
Keyword(s):  
Critical Review ◽  
Natural Compounds ◽  
Effective Strategy ◽  
Synthetic Analogues ◽  
Health Applications ◽  
Natural And Synthetic

Semi-synthesis is an effective strategy to obtain both natural and synthetic analogues of the olive secoiridoids, starting from easy accessible natural compounds.

SUBACUTE THYROIDITIS

1960 ◽  
Vol XXXIII (III) ◽  
pp. 457-472 ◽  
Author(s):  
B.-A. Lamberg ◽  
G. Hintze ◽  
R. Jussila ◽  
M. Berlin
Keyword(s):  
Thyroid Function ◽  
Early Phase ◽  
Radioactive Iodine ◽  
Serum Proteins ◽  
Conversion Ratio ◽  
Subacute Thyroiditis ◽  
Synthetic Analogues ◽  
The Third ◽  
Thyroid Uptake ◽  
Iodine Metabolism

ABSTRACT A series of cases of clinically diagnosed subacute thyroiditis comprising 11 patients is reported. Studies on the iodine metabolism, electrophoretic distribution of the serum proteins and the responsiveness to TSH were carried out. The patients were observed for periods up to 16 months from the onset of the disease. In the early phase there was an elevation of the serum PBI in a few cases and hyperthyroid signs in some, accompanied by depressed thyroid uptake of radioactive iodine and a fairly good response to TSH. Later, the thyroid grew hard and the iodine metabolism changed. In several cases there was a marked increase in the conversion ratio and the serum PB131I level. The responses to TSH was variable for different parameters of thyroid function, suggesting a state of »low thyroid reserve« as defined by Jefferies et al. (1956). Hypothyroidism developed in 3 cases; in two of them there was a response to exogenous TSH, in the third no response was seen at this stage of the disease. Cortisone and synthetic analogues seem to be of great benefit in the treatment of the acute symptoms of the disease.

scholarly journals Synthesis and Biological Activities of Cyclodepsipeptides of Aurilide Family from Marine Origin

Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 55
Author(s):  
Synthia Michon ◽  
Florine Cavelier ◽  
Xavier J. Salom-Roig
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Natural Compounds ◽  
Cancer Cell Lines ◽  
Hydroxy Ester ◽  
Marine Cyanobacteria ◽  
Synthetic Analogues ◽  
Marine Origin ◽  
Total Syntheses

Aurilides are a class of depsipeptides occurring mainly in marine cyanobacteria. Members of the aurilide family have shown to exhibit strong cytotoxicity against various cancer cell lines. These compounds bear a pentapeptide, a polyketide, and an α-hydroxy ester subunit in their structure. A large number of remarkable studies on aurilides have emerged since 1996. This comprehensive account summarizes the biological activities and total syntheses of natural compounds of the aurilide family as well as their synthetic analogues.

Synthesis and antibacterial activities of marine natural product Ianthelliformisamines and subereamine synthetic analogues

2021 ◽  
pp. 127883
Author(s):  
Shivaji Narayan Khadake ◽  
Shaik Karamathulla ◽  
Tapan Kumar Jena ◽  
Mohan Monisha ◽  
Nikhil Kumar Tuti ◽  
...  
Keyword(s):  
Natural Product ◽  
Antibacterial Activities ◽  
Marine Natural Product ◽  
Synthetic Analogues

Pheromones and 25 years of pheromonotherapy: what are they and how do they work?

2021 ◽  
Vol 12 (3) ◽  
pp. 116-122
Author(s):  
Claire Hargrave
Keyword(s):  
Veterinary Medicine ◽  
Animal Welfare ◽  
Companion Animals ◽  
Individual Member ◽  
Insect Pheromones ◽  
Synthetic Analogues ◽  
Insect Infestations ◽  
Veterinary Surgeon

The capacity of animals to communicate via pheromones is long established and, for generations, pheromones have been unwittingly used by man to manage the behaviour of animals in agriculture — using the chemicals produced by an individual member of a species to alter the behaviour of another member of that species. More recently, insect pheromones have been used in managing insect infestations of crops. However, approximately 25 years ago the French veterinary surgeon, Patrick Pageat, began to investigate the production of pheromones in both farm and companion animals and how synthetic analogues of pheromones could be used to improve animal welfare, creating a new field in veterinary medicine — pheromonotherapy. This article aims to summarise the main developments in pheromonotherapy over the last 25 years.

Formation of synthetic analogues of double metal-hydroxy carbonate minerals under controlled pH conditions: I. The synthesis of pyroaurite and reevesite

Clay Minerals ◽  
1990 ◽  
Vol 25 (2) ◽  
pp. 161-179 ◽  
Author(s):  
H. C. B. Hansen ◽  
R. M. Taylor
Keyword(s):  
Oxidation Rate ◽  
Reasonable Agreement ◽  
Single Phase ◽  
Morphological Features ◽  
Air Oxidation ◽  
Synthetic Analogues ◽  
Synthesis Technique ◽  
Homogeneous Product ◽  
Ph Conditions ◽  
Hydroxy Carbonate

AbstractTwo-layered Fe(III)-M(II) hydroxy carbonates (M(II) = Ni or Mg) have been synthesized by induced hydrolysis using controlled air oxidation of an aqueous Fe(II)-M(II) mixture (M(II)/Fe(II) ratio >3) at a pH below which the hydroxide of the M(II) cation precipitates. The crystalline, homogeneous product can be a single phase consisting of very thin circular to hexagonal plates (0·2–0·8 µm diam.). For synthetic reevesite (Ni(II)-Fe(III) hydroxy carbonate), stable spherular aggregates are formed. The well crystallized products have an M(II)/Fe(III) ratio of about two. However, by varying the pH, the initial M(II)-Fe(III) ratio and the oxidation rate, the M(II)/Fe(III) ratio in the product and its crystallinity can be varied. The derived formulae are in reasonable agreement with the known composition of pyroaurite-type compounds. Possible synthesis pathways are discussed. The ability to control some physical and morphological features of the products indicates that the synthesis technique could prove advantageous in the preparation of certain catalyst precursors.

scholarly journals Secondary structure and biophysical activity of synthetic analogues of the pulmonary surfactant polypeptide SP-C

1995 ◽  
Vol 307 (2) ◽  
pp. 535-541 ◽  
Author(s):  
J Johansson ◽  
G Nilsson ◽  
R Strömberg ◽  
B Robertson ◽  
H Jörnvall ◽  
...  
Keyword(s):  
Secondary Structure ◽  
Pulmonary Surfactant ◽  
Transmembrane Helix ◽  
Helical Structure ◽  
Helical Conformation ◽  
Synthetic Analogues ◽  
Charged Amino Acids ◽  
Phospholipid Micelles ◽  
Helical Content ◽  
Biophysical Activity

Native pulmonary-surfactant-associated lipopolypeptide SP-C, its chemically depalmitoylated form and several synthetic analogues lacking the palmitoylcysteine residues were analysed for secondary structure in phospholipid micelles and for biophysical activity in 1,2-dipalmitoyl-sn-glycero-3- phosphocholine/phosphatidylglycerol/palmitic acid (68:22:9, by wt.). Compared with the native molecule, with the entire poly-valyl part in a known alpha-helical conformation, depalmitoylated SP-C was found to be still mainly alpha-helical, but with an approx. 20% decrease in the helical content. A synthetic hybrid polypeptide where the entire poly-valyl alpha-helical part of native SP-C had been replaced with the amino acid sequence of a transmembrane helix of bacteriorhodopsin is also predominantly alpha-helical. In contrast, synthetic SP-C analogues lacking only the palmitoyl groups, by replacement of the palmitoylcysteine residues with cysteine, phenylalanine or serine, or lacking the positively charged amino acids by replacement with alanine, are considerably less alpha-helical than both native and depalmitoylated SP-C. The data indicate that the SP-C palmitoyl groups are important for maintenance of the alpha-helical conformation in parts of the polypeptide, and that the poly-valyl alpha-helical conformation is not fully formed in synthetic SP-C polypeptides. Furthermore, the helical structure of both native and depalmitoylated SP-C in dodecylphosphocholine micelles is very resistant to thermal denaturation, exhibiting ordered structure at 90 degrees C. The alpha-helical content grossly parallels the peptide-induced acceleration of the spreading of phospholipids at an air/water interface and the increase of surface pressure. The data suggest that the alpha-helical conformation itself, rather than just the covalent structure, is of prime importance for the biological function of synthetic pulmonary-surfactant peptides.

An easy route to synthetic analogues of radicamine B, codonopsine and codonopsinine from d-mannitol

2014 ◽  
Vol 12 (27) ◽  
pp. 4983 ◽  
Author(s):  
Suresh Dharuman ◽  
Ashok Kumar Palanivel ◽  
Yashwant D. Vankar
Keyword(s):  
Synthetic Analogues
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