Pyrrolo[1,4]benzodiazepine antitumor antibiotics: relationship of DNA alkylation and sequence specificity to the biological activity of natural and synthetic compounds

1988 ◽  
Vol 1 (5) ◽  
pp. 258-268 ◽  
Author(s):  
Laurence H. Hurley ◽  
Teri Reck ◽  
David E. Thurston ◽  
David R. Langley ◽  
Kenneth G. Holden ◽  
...  
Keyword(s):  
Biological Activity ◽  
Dna Alkylation ◽  
Sequence Specificity ◽  
Antitumor Antibiotics ◽  
Synthetic Compounds ◽  
Relationship Of ◽  
Natural And Synthetic

scholarly journals Relationship of 25-hydroxyvitamin D3 side chain structure to biological activity.

1975 ◽  
Vol 250 (1) ◽  
pp. 226-230
Author(s):  
M F Holick ◽  
M Garabedian ◽  
H K Schnoes ◽  
H F DeLuca
Keyword(s):  
Biological Activity ◽  
Chain Structure ◽  
Side Chain ◽  
Relationship Of

β-Cell-tropin: relationship of structure to biological activity

1983 ◽  
Vol 11 (2) ◽  
pp. 201-201 ◽  
Author(s):  
S. DUNMORE ◽  
J. MORTON ◽  
A. BELOFF-CHAIN ◽  
G. TAYLOR ◽  
H. R. MORRIS
Keyword(s):  
Biological Activity ◽  
Β Cell ◽  
Relationship Of

scholarly journals Experimental Chemotherapy for Chagas Disease: A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones

2011 ◽  
Vol 2011 ◽  
pp. 1-13 ◽  
Author(s):  
Solange L. de Castro ◽  
Denise G. J. Batista ◽  
Marcos M. Batista ◽  
Wanderson Batista ◽  
Anissa Daliry ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Chagas Disease ◽  
Chronic Phase ◽  
Public Health Problem ◽  
Term Therapy ◽  
High Morbidity ◽  
Synthetic Compounds ◽  
Natural And Synthetic

Chagas disease (CD), caused by Trypanosoma cruzi, affects approximately eight million individuals in Latin America and is emerging in nonendemic areas due to the globalisation of immigration and nonvectorial transmission routes. Although CD represents an important public health problem, resulting in high morbidity and considerable mortality rates, few investments have been allocated towards developing novel anti-T. cruzi agents. The available therapy for CD is based on two nitro derivatives (benznidazole (Bz) and nifurtimox (Nf)) developed more than four decades ago. Both are far from ideal due to substantial secondary side effects, limited efficacy against different parasite isolates, long-term therapy, and their well-known poor activity in the late chronic phase. These drawbacks justify the urgent need to identify better drugs to treat chagasic patients. Although several classes of natural and synthetic compounds have been reported to act in vitro and in vivo on T. cruzi, since the introduction of Bz and Nf, only a few drugs, such as allopurinol and a few sterol inhibitors, have moved to clinical trials. This reflects, at least in part, the absence of well-established universal protocols to screen and compare drug activity. In addition, a large number of in vitro studies have been conducted using only epimastigotes and trypomastigotes instead of evaluating compounds' activities against intracellular amastigotes, which are the reproductive forms in the vertebrate host and are thus an important determinant in the selection and identification of effective compounds for further in vivo analysis. In addition, due to pharmacokinetics and absorption, distribution, metabolism, and excretion characteristics, several compounds that were promising in vitro have not been as effective as Nf or Bz in animal models of T. cruzi infection. In the last two decades, our team has collaborated with different medicinal chemistry groups to develop preclinical studies for CD and investigate the in vitro and in vivo efficacy, toxicity, selectivity, and parasite targets of different classes of natural and synthetic compounds. Some of these results will be briefly presented, focusing primarily on diamidines and related compounds and naphthoquinone derivatives that showed the most promising efficacy against T. cruzi.

Natural and synthetic naphthoquinones as potential anti-infective agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Eyra Ortiz-Pérez ◽  
Karina Vázquez ◽  
Gildardo Rivera ◽  
Cristian O. Salas ◽  
J. José Zarate-Ramos ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Effects ◽  
Plasmodium Falciparum Malaria ◽  
Toxocara Canis ◽  
Chemotherapeutic Agents ◽  
Parasitic Diseases ◽  
Antiprotozoal Activity ◽  
Wide Range ◽  
Leishmania Spp ◽  
Natural And Synthetic

Background: Naphthoquinones are a class of aromatic compounds relevant for their chemical characteristics, structural properties, and biological activity. These compounds are found in nature with a wide range of effects, highlighting their antibacterial, antifungal, and antiprotozoal properties. Additionally, naphthoquinones are used as a scaffold to obtain new derivatives with pharmacological potential, mainly compounds against parasitic diseases. Objective: The purpose of this work was to carry out a comprehensive review of naphthoquinones and their derivatives obtained from both natural and synthetic sources, also, to well as analyze their biological activity against Leishmania spp (Leishmaniasis), Trypanosoma cruzi (Chagas disease), Plasmodium falciparum (Malaria), Toxoplasma gondii (Toxoplasmosis), and Toxocara canis (Toxocariasis). All of these agents are responsible for relevant diseases worldwide. Results : Natural naphthoquinones, such as plumbagin, diospyrin, burmanin, lapachol, lawsone and psychorubrin, show an antiprotozoal activity similar or enhanced antiprotozoal activity to reference drugs. Some naphthoquinones obtained by synthesis or semi-synthesis shown better biological activity or less toxic effects than natural compounds. Conclusion: In this review, natural and synthetic naphthoquinone showed antiparasitic activity, in the most cases with improved results than current drugs currently used in clinical trials. A modification of their structure with different functional groups can enhance their biological effects, improve solubility, and reduce undesirable side effects. Therefore, naphthoquinones are important molecules in the development of new chemotherapeutic agents against parasitic diseases.

scholarly journals New details of assembling bioactive films from dispersions of amphiphilic molecules on titania surfaces

RSC Advances ◽  
2020 ◽  
Vol 10 (65) ◽  
pp. 39854-39869
Author(s):  
Leonardo Francisco Gonçalves Dias ◽  
Stephani Stamboroski ◽  
Michael Noeske ◽  
Dirk Salz ◽  
Klaus Rischka ◽  
...  
Keyword(s):  
Biological Activity ◽  
Structure Property ◽  
Property Relationship ◽  
Amphiphilic Molecules ◽  
Structure Property Relationship ◽  
Relationship Of

Structure–property relationship of amphiphilic molecules on smooth substrates was explored through a multi-step approach and its influence on biological activity.

Plasmonic Effects, Size and Biological Activity Relationship of Au-Ag Alloy Nanoparticles

2018 ◽  
Vol 54 ◽  
pp. 98-111 ◽  
Author(s):  
Ahson Jabbar Shaikh ◽  
Maria Batool ◽  
Muhammad Arfat Yameen ◽  
Amir Waseem
Keyword(s):  
Biological Activity ◽  
Gradual Increase ◽  
Reducing Agent ◽  
Alloy Nanoparticles ◽  
Ag Nps ◽  
Uniform Size ◽  
Vis Spectroscopy ◽  
Plasmonic Effects ◽  
Lower Temperature ◽  
Relationship Of

The plasmonic effects of Au-Ag alloy nanoparticles, gold nanoparticles (AuNPs), and silver nanoparticles (AgNPs) are studied and compared to their size. Various factors that affect the size of alloy nanoparticles are varied such as concentration and ratio of gold and silver salt, time of addition of reducing agent, temperature and pH. Addition of reducing agent at different time intervals for the synthesis of pure and alloy Au-Ag NPs shows a gradual increase in size, as well as increase in heterogeneity of nanoparticles with delayed addition of reducing agent. Temperature dependent alloy nanoparticles also shows a gradual increase in size with increase in temperature. pH dependent alloy nanoparticles show decrease in size with increase in pH from 4 to 8. Their size is characterized by SEM and corelated with UV-Vis spectroscopy. Furthermore, alloy nanoparticles synthesized by varying temperature are also characterized for their antibacterial studies against Escherichia coli and Staphylococcus aureus strains. Nanoparticles synthesized at high temperature (100°C) have shown higher bioactivity against both organisms due to small and uniform size nanoparticles, while nanoparticles synthesized at lower temperature (50°C) have lower biological activity. Alloy nanoparticles synthesized at 60°C and 70°C are more active against E. coli while those of 80°C and 90°C are more active against S. aureus.

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