The melanocyte stimulating activity of N-nitroso-2-chloroethyl-carbamoyl derivatives of α-melanotropin fragments

1988 ◽  
Vol 53 (11) ◽  
pp. 2574-2582 ◽  
Author(s):  
Hedvig Medzihradszky-Schweiger ◽  
Helga Süli-Vargha ◽  
József Bódi ◽  
Kálmán Medzihradszky
Keyword(s):  
Biological Activity ◽  
Active Site ◽  
Frog Skin ◽  
Terminal Sequence ◽  
Subsequent Reaction ◽  
Affinity Labels ◽  
Derivatives Of

A number of N-nitroso-2-chloroethyl-carbamoyl (Q(NO)) derivatives of α-melanotropin fragments have been synthesized and their effect on the frog skin melanocytes studied. Peptides substituted in this way possess the biological activity of the parent compounds, indicating that they preserved their receptor recognizing ability. These compounds can therefore serve as affinity labels. Some of these derivatives, related to the C-terminal sequence of α-melanotropin show prolonged darkening reaction, which does not influence the subsequent reaction of melanocytes with α-melanotropin. The Q(NO)-derivative of a fragment derived from the classical active site of the hormone shows, however, inhibition of the effect of α-melanotropin. It can be concluded that the latter peptide acts through the melanotropin receptor, while others, related to the C-terminal sequence of the hormone through another mechanism.

Synthesis of arylacetic acids and their effect on activation of fibrinolysis. Quantitative relations between structure and biological activity

1980 ◽  
Vol 45 (5) ◽  
pp. 1401-1409 ◽  
Author(s):  
Miroslav Kuchař ◽  
Bohumila Brunová ◽  
Zdeněk Roubal ◽  
Jiří Schlanger ◽  
Oldřich Němeček
Keyword(s):  
Biological Activity ◽  
Regression Analysis ◽  
Active Site ◽  
Reversed Phase ◽  
Heat Denaturation ◽  
Arylacetic Acids ◽  
Layer Chromatography ◽  
Derivatives Of ◽  
Lipophilicity Parameters ◽  
Hydrophobic Bonding

A series of arylacetic acids, III, has been prepared and evaluated for activation of fibrinolysis and inhibition of heat-denaturation of serum albumin. regression analysis revealed that either activity was influenced mainly by lipophilicity of the aromatic substituents. The graph showing activation of fibrinolysis by acids III takes a linear course up to a maximum, followed by a step decrease. Also included in the series are p-benzyloxy derivatives of the arylacetic acids. Their lipophilicity has been evaluated by thin-layer chromatography, the method of reversed phase being employed. However, the lipophilicity parameters thus obtained fail to describe the hydrophobic bonding of these derivatives to the active site; tabulated values of the parameter π were better in this respect.

Acyl-Enzymes as Thrombolytic Agents in Dog Models of Venous Thrombosis and Pulmonary Embolism

1984 ◽  
Vol 51 (02) ◽  
pp. 248-253 ◽  
Author(s):  
R J Dupe ◽  
P D English ◽  
R A G Smith ◽  
J Green
Keyword(s):  
Pulmonary Embolism ◽  
Side Effects ◽  
Venous Thrombosis ◽  
Active Site ◽  
Acute Pulmonary Embolism ◽  
Quantitative Model ◽  
Beagle Dog ◽  
Thrombosis Model ◽  
Derivatives Of

SummaryA quantitative model of venous thrombosis in the beagle dog is described. The model was adapted to permit ageing of isolated experimental clots in vivo. A model of acute pulmonary embolism in this species is also described. In the venous thrombosis model, infusion of streptokinase (SK) or SK-activated human plasmin gave significant lysis but bolus doses of SK. plasmin complex were ineffective. Active site anisoylated derivatives of SK. plasminogen complex, SK-activated plasmin and activator-free plasmin were all active when given as bolus doses in both models. At lytic doses, the acyl-enzymes caused fewer side-effects attributable to plasminaemia than the corresponding unmodified enzymes.

Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Building Blocks ◽  
Vital Role ◽  
Review Of Literature ◽  
Drug Discovery Process ◽  
Active Compounds ◽  
Lead Compounds ◽  
Synthetic Approaches ◽  
Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates

2013 ◽  
Vol 9 (7) ◽  
pp. 920-925 ◽  
Author(s):  
Yi Bi ◽  
Jinyi Xu ◽  
Fei Sun ◽  
Xiaoming Wu ◽  
Wencai Ye ◽  
...  
Keyword(s):  
Biological Activity ◽  
Betulinic Acid ◽  
Antitumor Agent ◽  
Amide Derivatives ◽  
Derivatives Of

Two metal complex derivatives of pyridine thiazole ligand: synthesis, characterization and biological activity

2021 ◽  
Author(s):  
Xunzhong Zou ◽  
Pingyi Shi ◽  
Ansheng Feng ◽  
Meng Mei ◽  
Yu Li
Keyword(s):  
Biological Activity ◽  
Metal Complex ◽  
Ligand Synthesis ◽  
Derivatives Of

scholarly journals Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimalarial Drug ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

scholarly journals SYNTHESIS OF NOVEL TRYPTOPHAN DERIVATIVES OF POTENTIAL BIOLOGICAL ACTIVITY

2009 ◽  
Vol 54 (2) ◽  
Author(s):  
RAFAT M MOHAREB ◽  
NADIA A LOUCA ◽  
GAMAL A ELMEGEED ◽  
HANAA Y HANA
Keyword(s):  
Biological Activity ◽  
Potential Biological Activity ◽  
Derivatives Of ◽  
Tryptophan Derivatives

scholarly journals Synthesis and biological activity of (7S)-O-epoxyalkyl derivatives of daunomycinone.

1985 ◽  
Vol 38 (12) ◽  
pp. 1714-1718 ◽  
Author(s):  
VÊRA PRIKRYLOVÁ ◽  
HELENA LIPAVSKÁ ◽  
JOSEF V. JIZBA ◽  
JÁN FUSKA ◽  
MILOSLAV PODOJIL ◽  
...  
Keyword(s):  
Biological Activity ◽  
Derivatives Of
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