ChemInform Abstract: Synthesis and Biological Properties of Novel Phosphotriesters: A New Approach to the Introduction of Biologically Active Nucleotides into Cells.

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

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Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽

10.3390/molecules26123579 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3579

Author(s):

Svetlana A. Popova ◽

Evgenia V. Pavlova ◽

Oksana G. Shevchenko ◽

Irina Yu. Chukicheva ◽

Aleksandr V. Kutchin

Keyword(s):

Antioxidant Activity ◽

Antioxidant Properties ◽

Biological Properties ◽

High Reactivity ◽

Biologically Active ◽

Brain Lipids ◽

Wide Range ◽

Privileged Structure ◽

Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

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Nickel(II)- and Silver(I)-Catalyzed C–H Bond Halogenation of Anilides and Carbamates

Synthesis ◽

10.1055/s-0040-1705972 ◽

2020 ◽

Author(s):

Ebrahim Kianmehr ◽

Hadi Afaridoun

Keyword(s):

Biologically Active Compounds ◽

Biologically Active ◽

Silver Catalyst ◽

Active Compounds ◽

Available N ◽

New Approach

Abstract ortho-C–H bond halogenation of anilides and N-aryl carbamates using easily available N-halosuccinimides (NXS) as the active halogenation reagent in the presence of nickel or silver catalyst has been developed. This method provides a new approach to 2-haloanilides and carbamates, which may serve as starting materials for the synthesis of pharmaceutically and biologically active compounds.

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A NEW APPROACH FOR INVESTIGATING HYPOTHALAMO-PITUITARY-GONADAL AND ADRENAL FEEDBACK CONTROL MECHANISMS: ACTIVE IMMUNIZATION WITH STEROIDS

Acta Endocrinologica ◽

10.1530/acta.0.0760556 ◽

1974 ◽

Vol 76 (3) ◽

pp. 556-569 ◽

Cited By ~ 12

Author(s):

E. Nieschlag ◽

K. H. Usadel ◽

H. K. Kley ◽

U. Schwedes ◽

K. Schöffling ◽

...

Keyword(s):

Feedback Control ◽

Leydig Cells ◽

Positive Response ◽

Active Immunization ◽

Biologically Active ◽

Control Group ◽

Control Mechanisms ◽

New Approach ◽

Biological Neutralization ◽

Group Serum

ABSTRACT A new method for the investigation of hypothalamo-pituitary-gonadal and adrenal feedback control mechanisms based on the biological neutralization of gonadal and adrenal steroids by active immunization is proposed. The regulatory influence of a given steroid in the feedback control is proved when reduction of the free, biologically active fraction of this steroid caused by antibody binding induces a positive response of the pituitary, thus effecting gonadal or adrenal hypertrophy and hyperfunction. The advantages and limitations of the new model are demonstrated by the effects of active immunization of rabbits with cortisol (F), aldosterone (Aldo), dehydroepiandrosterone (DHA), androstenedione (Δ4-A), testosterone (T), 5α-dihydrotestosterone (5α-DHT), 5β-DHT and oestradiol (E2). In the immunized animals and in a control group serum concentrations of total corticosteroids (TC), DHA, T, Δ4-A, E1, E2, LH and FSH, the percentage of binding of steroids in serum and the specificity of the antisera are determined. The testes are evaluated by histometry and the nuclear volume of the adrenocortical and Leydig cells is measured.

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Antimicrobial Peptides: Versatile Biological Properties

International Journal of Peptides ◽

10.1155/2013/675391 ◽

2013 ◽

Vol 2013 ◽

pp. 1-15 ◽

Cited By ~ 105

Author(s):

Muthuirulan Pushpanathan ◽

Paramasamy Gunasekaran ◽

Jeyaprakash Rajendhran

Keyword(s):

Antimicrobial Peptides ◽

Recombinant Expression ◽

Biological Properties ◽

Biologically Active ◽

Drug Candidate ◽

Plant Host ◽

Immune Modulators ◽

Signalling Molecule ◽

Interesting Candidate ◽

Pharmaceutical Industries

Antimicrobial peptides are diverse group of biologically active molecules with multidimensional properties. In recent past, a wide variety of AMPs with diverse structures have been reported from different sources such as plants, animals, mammals, and microorganisms. The presence of unusual amino acids and structural motifs in AMPs confers unique structural properties to the peptide that attribute for their specific mode of action. The ability of these active AMPs to act as multifunctional effector molecules such as signalling molecule, immune modulators, mitogen, antitumor, and contraceptive agent makes it an interesting candidate to study every aspect of their structural and biological properties for prophylactic and therapeutic applications. In addition, easy cloning and recombinant expression of AMPs in heterologous plant host systems provided a pipeline for production of disease resistant transgenic plants. Besides these properties, AMPs were also used as drug delivery vectors to deliver cell impermeable drugs to cell interior. The present review focuses on the diversity and broad spectrum antimicrobial activity of AMPs along with its multidimensional properties that could be exploited for the application of these bioactive peptides as a potential and promising drug candidate in pharmaceutical industries.

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Constitutive and Regulated Shedding of Soluble FGF Receptors Releases Biologically Active Inhibitors of FGF-2

International Journal of Molecular Sciences ◽

10.3390/ijms22052712 ◽

2021 ◽

Vol 22 (5) ◽

pp. 2712

Author(s):

Anne Hanneken ◽

Maluz Mercado ◽

Pamela Maher

Keyword(s):

Cell Surface ◽

Ligand Binding ◽

Cellular Proliferation ◽

Biological Activities ◽

Biological Properties ◽

Matrix Metalloproteases ◽

Biologically Active ◽

Ectodomain Shedding ◽

High Affinity

The identification of soluble fibroblast growth factor (FGF) receptors in blood and the extracellular matrix has led to the prediction that these proteins modulate the diverse biological activities of the FGF family of ligands in vivo. A recent structural characterization of the soluble FGF receptors revealed that they are primarily generated by proteolytic cleavage of the FGFR-1 ectodomain. Efforts to examine their biological properties are now focused on understanding the functional consequences of FGFR-1 ectodomain shedding and how the shedding event is regulated. We have purified an FGFR-1 ectodomain that is constitutively cleaved from the full-length FGFR-1(IIIc) receptor and released into conditioned media. This shed receptor binds FGF-2; inhibits FGF-2-induced cellular proliferation; and competes with high affinity, cell surface FGF receptors for ligand binding. FGFR-1 ectodomain shedding downregulates the number of high affinity receptors from the cell surface. The shedding mechanism is regulated by ligand binding and by activators of PKC, and the two signaling pathways appear to be independent of each other. Deletions and substitutions at the proposed cleavage site of FGFR-1 do not prevent ectodomain shedding. Broad spectrum inhibitors of matrix metalloproteases decrease FGFR-1 ectodomain shedding, suggesting that the enzyme responsible for constitutive, ligand-activated, and protein kinase C-activated shedding is a matrix metalloprotease. In summary, shedding of the FGFR-1 ectodomain is a highly regulated event, sharing many features with a common system that governs the release of diverse membrane proteins from the cell surface. Most importantly, the FGFR ectodomains are biologically active after shedding and are capable of functioning as inhibitors of FGF-2.

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RECENTES AVANÇOS NA FUNCIONALIZAÇÃO SELETIVA DE QUINOLINAS

Química Nova ◽

10.21577/0100-4042.20170701 ◽

2021 ◽

Author(s):

Dartagnan Ferreira ◽

Valter Murie ◽

Thiago Santos ◽

Paulo Vieira ◽

Giuliano Clososki

Keyword(s):

Wide Spectrum ◽

Structural Diversity ◽

Biological Properties ◽

Biologically Active ◽

Chemical Transformations ◽

Heterocyclic Molecules ◽

Point Of Interest ◽

Selective Functionalization ◽

Biological Interest ◽

Approved Drugs

RECENT ADVANCES IN SELECTIVE FUNCTIONALIZATION OF QUINOLINES. Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing their use in several approved drugs nowadays. Due to its importance, the synthesis of molecules containing this nucleus becomes a point of interest for synthetic chemists. In this way, several methodologies have been recently developed to prepare quinoline derivatives with high structural diversity. Such chemical transformations allow the chemical modification of these rings with high selectivity and tolerance to diverse functional groups and these properties have been conveniently used in the preparation of biologically active molecules containing this unit. Herein, we present a review of the main methodologies employed in the selective functionalization of quinolines in the last twenty years. In this context, a brief introduction addressing general synthetic and medicinal aspects related to the functionalization positions of the quinoline ring is presented. Several methodologies used in the functionalization of this moiety are discussed, as well relevant synthetic applications, both in the preparation and functionalization of substances of biological interest.

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Secondary metabolites of a marine-derived Penicillium ochrochloron

Notulae Scientia Biologicae ◽

10.15835/nsb13311020 ◽

2021 ◽

Vol 13 (3) ◽

pp. 11020

Author(s):

Peter M. EZE ◽

Ying GAO ◽

Yang LIU ◽

Lasse Van GEELEN ◽

Chika P. EJIKEUGWU ◽

...

Keyword(s):

Antibacterial Activity ◽

Secondary Metabolites ◽

Biological Properties ◽

Industrial Applications ◽

Biologically Active ◽

Fungal Isolation ◽

The North ◽

Wide Range ◽

Extremophilic Fungi ◽

Fungal Secondary Metabolites

Extremophilic fungi have received considerable attention recently as new promising sources of biologically active compounds with potential pharmaceutical applications. This study investigated the secondary metabolites of a marine-derived Penicillium ochrochloron isolated from underwater sea sand collected from the North Sea in St. Peter-Ording, Germany. Standard techniques were used for fungal isolation, taxonomic identification, fermentation, extraction, and isolation of fungal secondary metabolites. Chromatographic separation and spectroscopic analyses of the fungal secondary metabolites yielded eight compounds: talumarin A (1), aspergillumarin A (2), andrastin A (3), clavatol (4), 3-acetylphenol (5), methyl 2,5-dihydro-4-hydroxy-5-oxo-3-phenyl-2-furanpropanoate (6), emodin (7) and 2-chloroemodin (8). After co-cultivation with Bacillus subtilis, the fungus was induced to express (-)-striatisporolide A (9). Compound 1 was evaluated for antibacterial activity against Staphylococcus aureus, Acinetobacter baumannii, Mycobacterium smegmatis, and M. tuberculosis, as well as cytotoxicity against THP-1 cells. The compound, however, was not cytotoxic to THP-1 cells and had no antibacterial activity against the microorganisms tested. The compounds isolated from P. ochrochloron in this study are well-known compounds with a wide range of beneficial biological properties that can be explored for pharmaceutical, agricultural, or industrial applications. This study highlights the bioprospecting potential of marine fungi and confirms co-cultivation as a useful strategy for the discovery of new natural products.

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A new approach for the synthesis of biologically active chromene compounds using a photo catalyst TiO2-Ag

Synthetic Communications ◽

10.1080/00397911.2021.2016836 ◽

2021 ◽

pp. 1-21

Author(s):

George Kupar Kharmawlong ◽

Ridaphun Nongrum ◽

John Elisa Kumar ◽

Bhusan Chhetri ◽

Arun Kumar Yadav ◽

...

Keyword(s):

Biologically Active ◽

New Approach ◽

Photo Catalyst

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