scholarly journals A new synthesis and preliminary evaluation of some analogues of mecamylamine – a compound with anti-addiction properties

2016 ◽  
Vol 14 (46) ◽  
pp. 10787-10798 ◽  
Author(s):  
David Mangan ◽  
Neasa McNabola ◽  
Emily H. Clark ◽  
Isabel Bermudez ◽  
Susan Wonnacott ◽  
...  
Keyword(s):  
Biological Activity ◽  
Preliminary Evaluation ◽  
New Synthesis

A new synthesis of mecamylamine allowed the preparation of analogues to probe biological activity.

New synthesis and biological activity of the cyclic tetrapeptides tentoxin and [Pro 1] tentoxin

2009 ◽  
Vol 28 (6) ◽  
pp. 603-612 ◽  
Author(s):  
JUDSON V. EDWARDS ◽  
ALAN R. LAX ◽  
EIVIND B. LILLEHOJ ◽  
GORDON J. BOUDREAUX
Keyword(s):  
Biological Activity ◽  
New Synthesis ◽  
Cyclic Tetrapeptides

Synthesis of CpM(CO)3-DAB and -PAMAM Dendrimer Conjugates and Preliminary Evaluation of Their Biological Activity

2015 ◽  
Vol 2015 (9) ◽  
pp. 1505-1510 ◽  
Author(s):  
Wanning Hu ◽  
Jan Hoyer ◽  
Ines Neundorf ◽  
Preshendren Govender ◽  
Gregory S. Smith ◽  
...  
Keyword(s):  
Biological Activity ◽  
Pamam Dendrimer ◽  
Preliminary Evaluation ◽  
Dendrimer Conjugates

scholarly journals Synthesis and Preliminary Evaluation of Biological Activity of Glycoconjugates Analogues of Acyclic Uridine Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2017 ◽  
Author(s):  
Roman Komor ◽  
Gabriela Pastuch-Gawolek ◽  
Ewelina Krol ◽  
Wieslaw Szeja
Keyword(s):  
Biological Activity ◽  
Bovine Milk ◽  
Nucleoside Analogues ◽  
Preliminary Evaluation ◽  
Synthetic Compounds ◽  
Enzyme Action ◽  
Enzyme Substrates ◽  
Donor Type ◽  
Natural Enzyme ◽  
Activity Of Enzymes

Herein we present the methodology for obtaining glycosyltransferase inhibitors, analogues of natural enzyme substrates of donor-type: UDP-glucose and UDP-galactose. The synthesis concerned glycoconjugates, nucleoside analogues containing an acyclic ribose mimetic linked to a uracil moiety in their structure. The biological activity of the synthesised compounds was determined on the basis of their ability to inhibit the model enzyme action of β-1,4-galactosyltransferase from bovine milk. The obtained results allowed to expand and supplement the existing library of synthetic compounds that are able to regulate the biological activity of enzymes from the GT class.

New synthesis and conformational analysis of lipid A: biological activity and supramolecular assembly

1999 ◽  
Vol 5 (1-2) ◽  
pp. 46-51 ◽  
Author(s):  
Koichi Fukase ◽  
Masato Oikawa ◽  
Yasuo Suda ◽  
Wen-Chi Liu ◽  
Yoshiyuki Fukase ◽  
...  
Keyword(s):  
Biological Activity ◽  
Conformational Analysis ◽  
Lipid A ◽  
Supramolecular Assembly ◽  
New Synthesis

Total Synthesis of the Depsipeptide FR901375 and Preliminary Evaluation of Its Biological Activity

2016 ◽  
Vol 2016 (34) ◽  
pp. 5667-5677
Author(s):  
Koichi Narita ◽  
Yuya Katoh ◽  
Ken-ichi Ojima ◽  
Singo Dan ◽  
Takao Yamori ◽  
...  
Keyword(s):  
Biological Activity ◽  
Total Synthesis ◽  
Preliminary Evaluation

Synthesis of Analogues of GABA. II. 4-Alkyl-4-aminobut-2-enoic Acids and a New Synthesis of Some Vinyl α-Amino Acids

1979 ◽  
Vol 32 (11) ◽  
pp. 2507 ◽  
Author(s):  
RD Allan
Keyword(s):  
Amino Acids ◽  
Biological Activity ◽  
Gaba Uptake ◽  
Synthetic Route ◽  
Conformationally Restricted ◽  
Enzyme Systems ◽  
New Synthesis ◽  
Methylene Groups ◽  
By Products

A series of 4-alkyl-4-aminobut-2-enoic acids (2)-(5) has been prepared as conformationally restricted analogues of GABA. The synthetic route which involved allylic bromination followed by displacement with ammonia also gave vinyl glycine analogues (7)-(9) as readily purified by-products of the reaction. The low biological activity in vitro against GABA uptake, binding and enzyme systems of (E)-2-aminocyclohexylideneacetic acid (4) and (E)-2-aminocyclopentylideneacetic acid (5) has been interpreted in terms of steric hindrance by the ring-forming methylene groups at the particularactive sites concerned.

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