Search results for "Biological activity"

Activity–Bioavailability balance in Oral Drug Development for a Selected Group of 6‐Fluoroquinolones

2002

Abstract A nomogram is proposed to select the best candidate in drug development studies with quinolones and is intended to substitute other possible models. The nomogram is referred to as an activity–bioavailability balance (ABB) because it includes the following two criteria: ABB= 1 / gm MIC ( drug candidate ) 1 /gm MIC ( ciprofloxacin ) · F calc \( drug candidate \) F calc ( ciproflaxacin ) . The in vitro activity of a group of 4′ N ‐alkyl‐ciprofloxacin derivatives was determined together with that of ciprofloxacin, initially against some reference strains and subsequently against 159 clinical isolates of eight selected species. The inverse of the geometric mean of the lowest concentrati…

Eight-membered heterocycles with two heteroatoms in a 1,3-relationship of interest in medicinal chemistry

2022

This chapter deals with 1,3-diheterocines, eight-membered heterocyclic systems with two heteroatoms, N, O and S, in a 1,3 relationship, exhibiting biological properties and exhaustively covers the literature from 2007 to the end of November 2019. The biological results of 1,3-diazocines, 1,3-oxazocines, 1,3-dioxocins and 1,3-thiazocines, that are the largest class of 1,3-diheterocines, were collected together with the few results available for 1,3-oxathiocin and 1,3-dithiocin derivatives at that time.

Iron oxide/oleic acid magnetic nanoparticles possessing biologically active choline derivatives

2018

Abstract In recent years, synthetic magnetic nanoparticles have made a major contribution to biomedicine. Interest in iron oxide magnetic nanoparticles conditioned by the fact that they are nontoxic, and possess the unique opportunity to deliver medicines to certain organs by external magnetic field. We have developed a synthetic procedure, which is based on binding of the first biologically active substance with the magnetic core, and subsequent immobilization of another biologically active substance (ligand) on the modified surface of nanoparticles thus creating plasma membrane-like structures. Using the proposed methodology, we have obtained new nontoxic magnetic nanoparticles, functiona…

Aggregation versus Biological Activity in Gold(I) Complexes. An Unexplored Concept

2021

The aggregation process of a series of mono- and dinuclear gold(I) complexes containing a 4-ethynylaniline ligand and a phosphane at the second coordination position (PR3-Au-C≡CC6H4-NH2, complexes 1-5, and (diphos)(Au-C≡CC6H4-NH2)2, complexes 6-8), whose biological activity was previously studied by us, has been carefully analyzed through absorption, emission, and NMR spectroscopy, together with dynamic light scattering and small-angle X-ray scattering. These experiments allow us to retrieve information about how the compounds enter the cells. It was observed that all compounds present aggregation in fresh solutions, before biological treatment, and thus they must be entering the cells as a…

Electrochemical Monitoring of the Pharmacological Activity of Natural Products

2015

Abstract Electrochemical techniques have largely been applied to characterize the redox reactivity of natural and synthetic compounds and to determine natural and synthetic compounds in solution. A series of new applications of electrochemistry that has emerged in the last few decades and aims to obtain information on the pharmacological activity of natural products is reviewed. Such applications involve the following: (1) electrochemical testing of specific pharmacological activity via electrochemical screening; (2) in situ evaluation of drug–substrate interactions, including the study of pharmacologically active natural products and their metabolites; (3) electrochemical mimicry of select…

The Orange Peel: An Outstanding Source of Chemical Resources

2021

Citrus sinensis (L.) Osbeck is a very common cultivar belonging to the Rutaceae family. It is largely diffused in several areas of the world characterized by mild to warm climate conditions. Its abundant worldwide production (up to 107 Tons. per year) and consumption both as the edible part of the fruit and as several types of derivative products imply the production of a huge amount of waste, such as the fruit pomace. Several ways of recycling this material have been developed in recent years: employment as fertilizer, fodder ingredient, and even cloth material. However, the chemical added value of Citrus sinensis peel has been underestimated despite the diversified and significant content…

ChemInform Abstract: Pyrrolidino Enaminones Structurally Related to Gyrase Inhibitors: Synthesis, Cyclization and Pharmacological Activity.

2010

Antivirale Wirkstoffe, 27. Mitt. Die Aminomethinylierung von 5-Oxo-2-pyrazolin-3-carbonsäurederivaten

1986

Aus der mit s-Triazin (1) durchgefuhrten Aminomethinylierung der 5-Oxo-2-pyrazolin-3-carbonsaurederivate 2a,b gehen die 4-Aminomethylen-5-oxo-2-pyrazolin-3-carbonsaurederivat 4a,b und die C-Rubazonsauren 5a,b hervor. Bei 4a deuten die spektroskopischen Daten auf das Vorliegen der Z-Form (Abb. 1), fur 5a auf das der Z-s-cis-(OH)-Form (Abb. 2) hin. Die Strukturtypen 4 und 5 weisen Vertreter mit antiviraler, entzundungshemmender, temperatursenkender und antimykotischer Wirkung auf. Antiviral Agents, XXVII: Aminomethynylation of 5-Oxo-2-pyrazoline-3-carboxylic Acid Derivatives Aminomethynylation of the 5-oxo-2-pyrazoline-3-carboxylic acid derivatives 2a,b by means of s-triazine (1) yields the 4…

ChemInform Abstract: Synthesis of Amino-1,2,4-triazoles by Reductive ANRORC Rearrangements of 1,2,4-Oxadiazoles.

2011

The hydrazinolysis of the oxadiazoles under optimized conditions allows a general synthesis of functionalized aminotriazole products which are of interest due to the biological activity of the heterocyclic system.

Anti-inflammatory drimane sesquiterpene lactones from an Aspergillus species

2014

Abstract IFN-γ inducible protein 10 (IP-10, CXCL10) is a 10 kDa chemokine, which is secreted from various cell types after exposure to pro-inflammatory stimuli. This chemokine is a ligand for the CXCR3 receptor and regulates immune responses by activating and recruiting leukocytes such as T cells, eosinophils, monocytes, and NK cells to sites of inflammation. Altered expression of CXCL10 has been associated with chronic inflammatory and infectious diseases and therefore CXCL10 represents a promising target for the development of new anti-inflammatory drugs. In a search for inhibitors of CXCL10 promoter activity, three structurally related drimane sesquiterpene lactones (compounds 1–3) were …