Synthesis and some pharmacological properties of a conformationally restricted imipramine analogue

1983 ◽  
Vol 5 (6) ◽  
pp. 329-332
Author(s):  
C. J. Grol ◽  
G. Westenberg ◽  
B. Hazelhoff ◽  
J. De Vries
Keyword(s):  
Pharmacological Properties ◽  
Conformationally Restricted

Conformationally restricted C-terminal peptides of substance P. Synthesis, mass spectral analysis and pharmacological properties

1985 ◽  
Vol 28 (10) ◽  
pp. 1536-1539 ◽  
Author(s):  
Dimitrios Theodoropoulos ◽  
Constantin Poulos ◽  
Dimitrios Gatos ◽  
Pane Cordopatis ◽  
Emanuel Escher ◽  
...  
Keyword(s):  
Spectral Analysis ◽  
Substance P ◽  
Pharmacological Properties ◽  
Mass Spectral Analysis ◽  
Mass Spectral ◽  
Conformationally Restricted

scholarly journals Solution structure of conformationally restricted vasopressin analogues.

2004 ◽  
Vol 51 (1) ◽  
pp. 33-49 ◽  
Author(s):  
Emilia Trzepałka ◽  
Marta Oleszczuk ◽  
Maciej Maciejczyk ◽  
Bernard Lammek
Keyword(s):  
Aqueous Solution ◽  
Solution Structure ◽  
Pharmacological Properties ◽  
Spatial Structures ◽  
Conformationally Restricted ◽  
Nmr Data ◽  
Neurohypophyseal Hormones ◽  
Selective Antagonists ◽  
Vasopressin Analogues ◽  
Method Show

In recent years, a massive effort has been directed towards designing potent and selective antagonists of neurohypophyseal hormones substituted at position 3. Modification of vasopressin at position 3 with 4,4'-biphenylalanine results in pharmacologically inactive analogues. Chemically, this substitution appears to vary only slightly from those previously made by us (1-Nal or 2-Nal), which afforded potent agonists of V(2) receptors. In this situation, it seemed worthwhile to study the structure of the analogues with 4,4'-biphenylalanine (BPhe) at position 3 in aqueous solution using NMR spectroscopy and total conformational analysis. This contribution is part of extensive studies aimed at understanding spatial structures of 3-substituted [Arg(8)]vasopressin analogues of different pharmacological properties. NMR data were used to calculate 3D structures for all the analogues using two methods, EDMC with the ECEPP/3 force field, and molecular dynamic with the simulated annealing (SA) algorithm. The structures obtained by the first method show a better fit between the NMR spectral evidence and the calculation for all the peptides.

scholarly journals Synthesis of conformationally restricted glutamate and glutamine derivatives from carbonylation of orthopalladated phenylglycine derivatives

2012 ◽  
Vol 8 ◽  
pp. 1569-1575 ◽  
Author(s):  
Esteban P Urriolabeitia ◽  
Eduardo Laga ◽  
Carlos Cativiela
Keyword(s):  
Glutamic Acid ◽  
Phenyl Ring ◽  
Methyl Esters ◽  
New Method ◽  
Regioselective Synthesis ◽  
Pharmacological Properties ◽  
Conformationally Restricted ◽  
Selective Incorporation ◽  
Carbonyl Species

A new method for the regioselective synthesis of 2-alkoxycarbonyl- and 2-(aminocarbonyl)phenylglycinate methyl esters has been developed. The reaction of the orthopalladated complex [Pd(μ-Cl)(C6H4(CH(CO2Me)NMe2)-2)]2 (1) with nucleophiles HNu under a CO atmosphere results in the selective incorporation of the C(O)Nu moiety to the phenyl ring and formation of the carbonyl species ortho-C6H4(C(O)Nu)(CH(CO2Me)NMe2) (2a–j) (Nu = OR, NHR, NR2). Compounds 2a–j are conformationally restricted analogues of glutamic acid and glutamine and are interesting due to their biological and pharmacological properties. The reaction of [Pd(μ-Cl)(C6H4(CH(CO2Me)NHTf)-2)]2 (3) with nucleophiles in a CO atmosphere results, however, in the formation of the cyclic isoindolinone or the open 2-carboxyphenylglycine methyl esters, with the reaction outcome being driven by the choice of the solvent.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

ASSESSMENT OF TOXICITY OF GERMANIUM COORDINATION COMPOUNDS

2019 ◽  
pp. 16-21
Author(s):  
A. V. Kadomtsevа ◽  
I. V. Zhdanovich ◽  
M. S. Piskunovа ◽  
A. N. Lineva ◽  
A. N. Novikova ◽  
...  
Keyword(s):  
Coordination Compounds ◽  
Organometallic Compounds ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Toxicological Studies ◽  
Methods Of Synthesis ◽  
Promising Area

The synthesis of biologically active coordination compounds and the design on their basis of effective pharmacological preparations is currently the promising area. This paper presents the results of the toxicological studies on digermanium and its complex derivatives. It should be noted that the positive medical properties of organometallic compounds of germanium are confirmed by numerous studies, therefore, the development of the methods of synthesis, as well as investigations of physicochemical and pharmacological properties of these compounds are at the center of attention.

Sign in / Sign up

Export Citation Format

Share Document