Quinoline-based Compounds as Key Candidates to Tackle Drug Discovery Programs of Microbicidal Agents

2020 ◽  
Vol 26 ◽  
Author(s):  
Aline Nefertiti Silva da Gama ◽  
Maria de Nazaré Correia Soeiro
Keyword(s):  
Drug Discovery ◽  
Trypanosoma Brucei ◽  
Anticancer Agents ◽  
Biological Effect ◽  
Heterocyclic Compounds ◽  
Neglected Tropical Diseases ◽  
Pharmacological Properties ◽  
Tropical Diseases ◽  
Clinical Use ◽  
Leishmania Spp

: Quinolines are nitrogen heterocyclic compounds ubiquitous in nature and largely used as a structural component of dyes, solvent for resins, terpenes as well as during the production of several other chemical stuffs, including pesticides. Quinolines, such as quinine and chloroquine, exhibit various pharmacological properties, acting as antimalarial drugs, antiparasitic, antibacterial, antiviral, antifungal, and anticancer agents, besides being in clinical use for autoimmune diseases. Presently, a brief review is present regarding the biological effect and clinical use of quinolines and derivatives upon two trypanosomatids agents of important neglected tropical diseases; Trypanosoma cruzi, Trypanosoma brucei spp and Leishmania spp, which trigger Chagas disease, sleeping sickness and leishmaniasis, respectively, also extending to a glance update of their potential application towards other microbes relevant for emerging illness caused by fungi, bacteria and virus, including the pandemic Covid-19.

scholarly journals VLP-Based Vaccines as a Suitable Technology to Target Trypanosomatid Diseases

Vaccines ◽  
2021 ◽  
Vol 9 (3) ◽  
pp. 220
Author(s):  
Aline Maria Vasconcelos Queiroz ◽  
Johny Wysllas de Freitas Oliveira ◽  
Cláudia Jassica Moreno ◽  
Diego M. A. Guérin ◽  
Marcelo Sousa Silva
Keyword(s):  
Trypanosoma Brucei ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Vaccine Adjuvants ◽  
Host Interaction ◽  
Virus Like Particle ◽  
Leishmania Spp ◽  
Potential Use ◽  
A Current ◽  
New Vaccines

Research on vaccines against trypanosomatids, a family of protozoa that cause neglected tropical diseases, such as Chagas disease, leishmaniasis, and sleeping sickness, is a current need. Today, according to modern vaccinology, virus-like particle (VLP) technology is involved in many vaccines, including those undergoing studies related to COVID-19. The potential use of VLPs as vaccine adjuvants opens an opportunity for the use of protozoan antigens for the development of vaccines against diseases caused by Trypanosoma cruzi, Leishmania spp., and Trypanosoma brucei. In this context, it is important to consider the evasion mechanisms of these protozoa in the host and the antigens involved in the mechanisms of the parasite–host interaction. Thus, the immunostimulatory properties of VLPs can be part of an important strategy for the development and evaluation of new vaccines. This work aims to highlight the potential of VLPs as vaccine adjuvants for the development of immunity in complex diseases, specifically in the context of tropical diseases caused by trypanosomatids.

Biologically Active 2,5-Disubstituted-1,3,4-Oxadiazoles

2009 ◽  
Vol 2 (1) ◽  
pp. 390-406
Author(s):  
Harish Rajak ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
Heterocyclic Compounds ◽  
Medical Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Clinical Use ◽  
Synthetic Drugs ◽  
Physiologic Activity ◽  
Pharmacologically Active

There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.

Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

Heterocycles in the Treatment of Neglected Tropical Diseases

2020 ◽  
Vol 27 ◽  
Author(s):  
Kush K. Maheshwari ◽  
Debasish Bandyopadhyay
Keyword(s):  
Developing Countries ◽  
Heterocyclic Compounds ◽  
Neglected Tropical Diseases ◽  
World Health ◽  
Current Status ◽  
Poor People ◽  
Tropical Diseases ◽  
Concise Review ◽  
The World ◽  
Health Organization

Background: Neglected tropical diseases (NTDs) affect a huge population of the world and majority of the victims belong to the poor community of the developing countries. Until now, the World Health Organization (WHO) has identified 20 tropical diseases as NTDs that must be addressed with high priority. However, many heterocyclic scaffolds have demonstrated potent therapeutic activity against several NTDs. Objective: There are three major objectives: (1) To discuss the causes, symptoms, and current status of all the 20 NTDs; (2) To explore the available heterocyclic drugs, and their mechanism of actions (if known) that are being used to treat NTDs; (3) To develop general awareness on NTDs among the medicinal/health research community and beyond. Methods: The 20 NTDs have been discussed according to their alphabetic orders along with the possible heterocyclic remedies. Current status of treatment with an emphasis on the heterocyclic drugs (commercially available and investigational) has been outlined. In addition, brief discussion of the impacts of NTDs on socio-economic condition is included. Results: NTDs are often difficult to diagnose and the problem is worsened by the unhealthy hygiene, improper awareness, and inadequate healthcare in the developing countries where these diseases primarily affect poor people. The statistics include duration of suffering, numbers affected, and access to healthcare and medication. The mechanism of actions of various heterocyclic drugs, if reported, have been briefly summarized. Conclusion: Scientists and pharmaceutical corporations should allocate more resources to reveal the in-depth mechanism of actions of many heterocyclic drugs that are currently being used for the treatment of NTDs. Analysis of current heterocyclic compounds and development of new medications can help in the fight to reduce/remove the devastating effects of NTDs. An opinion-based concise review has been presented. Based on available literature, this is the first effect to present all the 20 NTDs and related heterocyclic compounds under the same umbrella.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

scholarly journals Editorial: Cheminformatics Approaches in Drug Discovery for Neglected Tropical Diseases

2021 ◽  
Vol 9 ◽  
Author(s):  
Luciana Scotti ◽  
Eugene Muratov ◽  
Alejandro Speck-Planche ◽  
Marcus T. Scotti
Keyword(s):  
Drug Discovery ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases

scholarly journals WIPO Re:Search: Catalyzing Public-Private Partnerships to Accelerate Tropical Disease Drug Discovery and Development

2019 ◽  
Vol 4 (1) ◽  
pp. 53 ◽  
Author(s):  
Cathyryne Manner ◽  
Katy Graef ◽  
Jennifer Dent
Keyword(s):  
Drug Discovery ◽  
Intellectual Property ◽  
Neglected Tropical Diseases ◽  
Tropical Disease ◽  
New Drugs ◽  
World Intellectual Property Organization ◽  
Tropical Diseases ◽  
Middle Income ◽  
Drug Discovery And Development ◽  
Partnership Model

Tropical diseases, including malaria and a group of infections termed neglected tropical diseases (NTDs), pose enormous threats to human health and wellbeing globally. In concert with efforts to broaden access to current treatments, it is also critical to expand research and development (R&D) of new drugs that address therapeutic gaps and concerns associated with existing medications, including emergence of resistance. Limited commercial incentives, particularly compared to products for diseases prevalent in high-income countries, have hindered many pharmaceutical companies from contributing their immense product development know-how and resources to tropical disease R&D. In this article we present WIPO Re:Search, an international initiative co-led by BIO Ventures for Global Health (BVGH) and the World Intellectual Property Organization (WIPO), as an innovative and impactful public-private partnership model that promotes cross-sector intellectual property sharing and R&D to accelerate tropical disease drug discovery and development. Importantly, WIPO Re:Search also drives progress toward the United Nations Sustainable Development Goals (SDGs). Through case studies, we illustrate how WIPO Re:Search empowers high-quality tropical disease drug discovery researchers from academic/non-profit organizations and small companies (including scientists in low- and middle-income countries) to leapfrog their R&D programs by accessing pharmaceutical industry resources that may not otherwise be available to them.

scholarly journals Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform

2019 ◽  
Vol 24 (3) ◽  
pp. 346-361 ◽  
Author(s):  
Carolina B. Moraes ◽  
Gesa Witt ◽  
Maria Kuzikov ◽  
Bernhard Ellinger ◽  
Theodora Calogeropoulou ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Trypanosoma Brucei ◽  
Value Chain ◽  
Neglected Tropical Diseases ◽  
World Health ◽  
Synthetic Compound ◽  
Antiparasitic Activity ◽  
Compound Libraries ◽  
Health Organization

According to the World Health Organization, more than 1 billion people are at risk of or are affected by neglected tropical diseases. Examples of such diseases include trypanosomiasis, which causes sleeping sickness; leishmaniasis; and Chagas disease, all of which are prevalent in Africa, South America, and India. Our aim within the New Medicines for Trypanosomatidic Infections project was to use (1) synthetic and natural product libraries, (2) screening, and (3) a preclinical absorption, distribution, metabolism, and excretion–toxicity (ADME-Tox) profiling platform to identify compounds that can enter the trypanosomatidic drug discovery value chain. The synthetic compound libraries originated from multiple scaffolds with known antiparasitic activity and natural products from the Hypha Discovery MycoDiverse natural products library. Our focus was first to employ target-based screening to identify inhibitors of the protozoan Trypanosoma brucei pteridine reductase 1 ( TbPTR1) and second to use a Trypanosoma brucei phenotypic assay that made use of the T. brucei brucei parasite to identify compounds that inhibited cell growth and caused death. Some of the compounds underwent structure-activity relationship expansion and, when appropriate, were evaluated in a preclinical ADME-Tox assay panel. This preclinical platform has led to the identification of lead-like compounds as well as validated hits in the trypanosomatidic drug discovery value chain.

Sign in / Sign up

Export Citation Format

Share Document