Insight into Recent Drug Discoveries against Trypanosomatids and Plasmodium spp Parasites: New Metal-based Compounds

2021 ◽  
Vol 28 ◽  
Author(s):  
Cauê Benito Scarim ◽  
Renan Lira de Farias ◽  
Diego Eidy Chiba ◽  
Chung Man Chin
Keyword(s):  
Inorganic Chemistry ◽  
Drug Discovery ◽  
Infectious Diseases ◽  
Chagas Disease ◽  
Human African Trypanosomiasis ◽  
Review Article ◽  
Pharmacological Activities ◽  
Tropical Infectious Diseases ◽  
Medicinal Inorganic Chemistry ◽  
Insight Into

: Scaffolds of metal-based compounds can act as pharmacophore groups in several ligands to treat various diseases, including tropical infectious diseases (TID). In this review article, we investigate the contribution of these moieties to medicinal inorganic chemistry in the last seven years against TID, including American trypanosomiasis (Chagas disease), human African trypanosomiasis (HAT, sleeping sickness), leishmania, and malaria. The most potent metal-based complexes are displayed and highlighted in figures, tables and graphics; according to their pharmacological activities (IC50 > 10µM) against Trypanosomatids and Plasmodium spp parasites. We highlight the current progresses and viewpoints of these metal-based complexes, with a specific focus on drug discovery.

Steroidal pyrazolines as a promising scaffold in drug discovery

2020 ◽  
Vol 12 (10) ◽  
pp. 949-959
Author(s):  
Ranju Bansal ◽  
Ranjit Singh
Keyword(s):  
Drug Discovery ◽  
Broad Spectrum ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Review Article ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Wide Range

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.

scholarly journals An Updated Review on Synthesis and Biological Activities of Thiosemicarbazide Analogs

2021 ◽  
Vol 33 (9) ◽  
pp. 1957-1975
Author(s):  
Akhalesh Kumar ◽  
Rakhi Mishra ◽  
Avijit Mazumder ◽  
Rupa Mazumder ◽  
Arun Kumar
Keyword(s):  
Drug Discovery ◽  
Review Paper ◽  
Biological Activities ◽  
Reaction Scheme ◽  
Review Article ◽  
Pharmacological Activities ◽  
Thiosemicarbazide Derivative ◽  
Synthetic Methodologies ◽  
Thiosemicarbazide Derivatives

This review paper focuses on the different synthetic methodologies that researchers have adopted to synthesize various thiosemicarbazide derivatives with different biological activities of synthesized compounds in the last 20 years. Most of the investigations available in the literature are directed to the biological activities of thiosemicarbazide derivatives with less discussion on its synthetic schemes. This review article presents various reaction scheme, which has been adopted for thiosemicarbazide derivative synthesis along with the reported pharmacological activities of synthesized analogs. The available literature in the article aims to encourage more studies on the synthesis of thiosemicarbazide derivatives, which will help for drug discovery having thiosemicarbazide nucleus.

scholarly journals Natural Products as Potential Lead Compounds for Drug Discovery Against SARS-CoV-2

2021 ◽  
Author(s):  
Oyere Tanyi Ebob ◽  
Smith B. Babiaka ◽  
Fidele Ntie-Kang
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Infectious Diseases ◽  
Review Article ◽  
Literature Survey ◽  
Lead Compounds ◽  
The Past ◽  
The World ◽  
Bacteria And Fungi ◽  
New Vaccines

AbstractFor the past 2 years, the coronavirus responsible for the COVID-19 infection has become a world pandemic, ruining the lives and economies of several nations in the world. This has scaled up research on the virus and the resulting infection with the goal of developing new vaccines and therapies. Natural products are known to be a rich source of lead compounds for drug discovery, including against infectious diseases caused by microbes (viruses, bacteria and fungi). In this review article, we conducted a literature survey aimed at identifying natural products with inhibitory concentrations against the coronaviruses or their target proteins, which lie below 10 µM. This led to the identification of 42 compounds belonging to the alkaloid, flavonoid, terpenoid, phenolic, xanthone and saponin classes. The cut off concentration of 10 µM was to limit the study to the most potent chemical entities, which could be developed into therapies against the viral infection to make a contribution towards limiting the spread of the disease.

scholarly journals NAMI-A and KP1019/1339, Two Iconic Ruthenium Anticancer Drug Candidates Face-to-Face: A Case Story in Medicinal Inorganic Chemistry

Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 1995 ◽  
Author(s):  
Enzo Alessio ◽  
Luigi Messori
Keyword(s):  
Inorganic Chemistry ◽  
Anticancer Drug ◽  
Molecular Mechanisms ◽  
State Of The Art ◽  
Unique Case ◽  
Face To Face ◽  
Drug Candidates ◽  
Medicinal Inorganic Chemistry ◽  
Insight Into ◽  
Pharmacological Profiles

NAMI-A ((ImH)[trans-RuCl4(dmso-S)(Im)], Im = imidazole) and KP1019/1339 (KP1019 = (IndH)[trans-RuCl4(Ind)2], Ind = indazole; KP1339 = Na[trans-RuCl4(Ind)2]) are two structurally related ruthenium(III) coordination compounds that have attracted a lot of attention in the medicinal inorganic chemistry scientific community as promising anticancer drug candidates. This has led to a considerable amount of studies on their respective chemico-biological features and to the eventual admission of both to clinical trials. The encouraging pharmacological performances qualified KP1019 mainly as a cytotoxic agent for the treatment of platinum-resistant colorectal cancers, whereas the non-cytotoxic NAMI-A has gained the reputation of being a very effective antimetastatic drug. A critical and strictly comparative analysis of the studies conducted so far on NAMI-A and KP1019 allows us to define the state of the art of these experimental ruthenium drugs in terms of the respective pharmacological profiles and potential clinical applications, and to gain some insight into the inherent molecular mechanisms. Despite their evident structural relatedness, deeply distinct biological and pharmacological profiles do emerge. Overall, these two iconic ruthenium complexes form an exemplary and unique case in the field of medicinal inorganic chemistry.

scholarly journals Microbial Sterolomics as a Chemical Biology Tool

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2768 ◽  
Author(s):  
Brad Haubrich
Keyword(s):  
Drug Discovery ◽  
Infectious Diseases ◽  
Immune Responses ◽  
Fusidic Acid ◽  
Clinical Relevance ◽  
Chemical Biology ◽  
Insight Into ◽  
Microbial Sources

Metabolomics has become a powerful tool in chemical biology. Profiling the human sterolome has resulted in the discovery of noncanonical sterols, including oxysterols and meiosis-activating sterols. They are important to immune responses and development, and have been reviewed extensively. The triterpenoid metabolite fusidic acid has developed clinical relevance, and many steroidal metabolites from microbial sources possess varying bioactivities. Beyond the prospect of pharmacognostical agents, the profiling of minor metabolites can provide insight into an organism’s biosynthesis and phylogeny, as well as inform drug discovery about infectious diseases. This review aims to highlight recent discoveries from detailed sterolomic profiling in microorganisms and their phylogenic and pharmacological implications.

Research Program in Tropical Infectious Diseases

1990 ◽  
Author(s):  
Bryce C. Redington ◽  
Jose A. Lopez ◽  
Llewellyn J. Legters ◽  
Richard E. Krieg
Keyword(s):  
Infectious Diseases ◽  
Research Program ◽  
Tropical Infectious Diseases

Aim for the Readers! Bromodomains As New Targets Against Chagas’ Disease

2019 ◽  
Vol 26 (36) ◽  
pp. 6544-6563
Author(s):  
Victoria Lucia Alonso ◽  
Luis Emilio Tavernelli ◽  
Alejandro Pezza ◽  
Pamela Cribb ◽  
Carla Ritagliati ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Small Molecules ◽  
Chagas Disease ◽  
Causative Agent ◽  
Current Knowledge ◽  
Sequence Similarity ◽  
Lysine Acetylation ◽  
Specific Manner ◽  
Lysine Residues ◽  
Antiparasitic Drugs

Bromodomains recognize and bind acetyl-lysine residues present in histone and non-histone proteins in a specific manner. In the last decade they have raised as attractive targets for drug discovery because the miss-regulation of human bromodomains was discovered to be involved in the development of a large spectrum of diseases. However, targeting eukaryotic pathogens bromodomains continues to be almost unexplored. We and others have reported the essentiality of diverse bromodomain- containing proteins in protozoa, offering a new opportunity for the development of antiparasitic drugs, especially for Trypansoma cruzi, the causative agent of Chagas’ disease. Mammalian bromodomains were classified in eight groups based on sequence similarity but parasitic bromodomains are very divergent proteins and are hard to assign them to any of these groups, suggesting that selective inhibitors can be obtained. In this review, we describe the importance of lysine acetylation and bromodomains in T. cruzi as well as the current knowledge on mammalian bromodomains. Also, we summarize the myriad of small-molecules under study to treat different pathologies and which of them have been tested in trypanosomatids and other protozoa. All the information available led us to propose that T. cruzi bromodomains should be considered as important potential targets and the search for smallmolecules to inhibit them should be empowered.

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