From Magic Bullet to Magic Bomb: Reductive Bioactivation of Antiparasitic Agents

: Infectious diseases commonly occur in tropical and sub-tropical countries. The pathogens of such diseases are able to multiply in human hosts, warranting their continual survival. Infections that are commonplace include malaria, chagas, trypanosomiasis, giardiasis, amoebiasis, toxoplasmosis and leishmaniasis. Malaria is known to cause symptoms, such as high fever, chills, nausea and vomiting, whereas chagas disease causes enlarged lymph glands, muscle pain, swelling and chest pain. People suffering from African trypanosomiasis may experience severe headaches, irritability, extreme fatigue and swollen lymph nodes. As an infectious disease progresses, the human host may also experience personality changes and neurologic problems. If left untreated, most of these diseases can lead to death. : Parasites, microbes and bacteria are increasingly adapting and generating strains that are resistant to current clinical drugs. Drug resistance creates an urgency for the development of new drugs to treat these infections. Nitro containing drugs, such as chloramphenicol, metronidazole, tinidazole and secnidazole had been banned for use as antiparasitic agents due to their toxicity. However, recent discoveries of nitrocontaining anti-tuberculosis drugs, i.e. delamanid and pretonamid, and the repurposing of flexinidazole for use in combination with eflornithine for the treatment of human trypanosomiasis, have ignited interest in nitroaromatic scaffolds as viable sources of potential anti-infective agents. : This review highlights the differences between old and new nitration methodologies. It furthermore offers insights into recent advances in the development of nitroaromatics as anti-infective drugs.

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Targeted Delivery of siRNA Therapeutics using Ligand Mediated Biodegradable Polymeric Nanocarriers

Current Pharmaceutical Design ◽

10.2174/1381612824666180702113345 ◽

2018 ◽

Vol 24 (16) ◽

pp. 1788-1800 ◽

Cited By ~ 1

Author(s):

Kye-Soo Cho ◽

Seo-Jin Hong ◽

Min-Hye Ahn ◽

Sukdeb Pal ◽

Pill-Hoon Choung ◽

...

Keyword(s):

Cancer Treatment ◽

Delivery System ◽

Targeted Delivery ◽

Sirna Delivery ◽

Public Health Issue ◽

Magic Bullet ◽

Bodily Fluids ◽

Low Cytotoxicity ◽

Genetic And Environmental Factors ◽

Sirna Delivery System

Background: Cancer poses a major public health issue, is linked with high mortality rates across the world, and shows a strong interplay between genetic and environmental factors. To date, common therapeutics, including chemotherapy, immunotherapy, and radiotherapy, have made significant contributions to cancer treatment, although diverse obstacles for achieving the permanent “magic bullet” cure have remained. Recently, various anticancer therapeutic agents designed to overcome the limitations of these conventional cancer treatments have received considerable attention. One of these promising and novel agents is the siRNA delivery system; however, poor cellular uptake and altered siRNA stability in physiological environments have limited its use in clinical trials. Therefore, developing the ideal siRNA delivery system with low cytotoxicity, improved siRNA stability in the body’s circulation, and prevention of its rapid clearance from bodily fluids, is rapidly emerging as an innovative therapeutic strategy to combat cancer. Moreover, active targeting using ligand moieties which bind to over-expressed receptors on the surface of cancer cells would enhance the therapeutic efficiency of siRNA. Conclusion: In this review, we provide 1) an overview of the non-viral carrier associated with siRNA delivery for cancer treatment, and 2) a description of the five major cancer-targeting ligands.

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Remdesivir and Hydroxychloroquine: A Compassionate Use in Covid-19

Current Drug Targets ◽

10.2174/1389450121999201228212842 ◽

2020 ◽

Vol 21 ◽

Author(s):

Amritpal Kaur ◽

Gaurav Chaudhary ◽

Pargat Singh ◽

Sandeep Arora ◽

Rajwinder Kaur

Keyword(s):

Literature Search ◽

Review Paper ◽

Off Label Use ◽

Compassionate Use ◽

Off Label ◽

Parenteral Route ◽

Randomized Controlled ◽

Novel Coronavirus ◽

Microsoft Office ◽

Antiparasitic Agents

Objective:: Early in December 2019, a mass of sufferers with Novel Coronavirus Pneumonia (SAS-CoV-19) in Wuhan (China) roused worldwide concern. Hardly any drugs showed the light of hope concerning the depletion in the period of treatment and virological suppression is troubled. Furthermore, numerous sufferers have undergone off-label use or compassionate use treatments as well as antiretroviral, antiparasitic agents, anti-inflammatory compounds, and convales-cent plasma in either oral/parenteral route. This study aims to compile and analyze the efficient value of Remdesivir and Hydroxychloroquine and give an insight to their drug profile in the treatment and management of COVID-19 patients. Method:: The literature search from PubMed, Crossref, Springer, Bentham Sciences, Google Scholar, DOAJ, ScienceDirect, and MEDLINE by using keywords like COVID-19, SAS-COV-2, Remdesivir, and hydroxychloroquine was done and ap-propriate peer-reviewed review articles, as well as research articles, were included and compiled in this review paper. The figures were prepared by using ChemOffice 2016 (ChemDraw Professional 2016) and Microsoft Office. Results:: The results of this study indicate that remdesivir in 5/10 studies from collected literature show a reduction in time of recovery and 5/10 shows no variance and having limitations. However, 6/12 shows an increase in the survival/reduction in time of recovery and 6/12 shows no effect or has limitations in the case of hydroxychloroquine. Conclusion:: There is a need to assess more pharmacokinetics and randomized controlled trials (RCT) for both remdesivir and hydroxychloroquine. Furthermore, studies should be conducted in different combinations along with hydroxychloro-quine and remdesivir to get efficient results.

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