New organometallic ruthenium(ii) complexes with purine analogs – a wide perspective on their biological application

2021 ◽  
Author(s):  
Marzena Fandzloch ◽  
Tomasz Jędrzejewski ◽  
Liliana Dobrzańska ◽  
Ginés M. Esteban-Parra ◽  
Joanna Wiśniewska ◽  
...  

Three new Ru(ii) piano-stool complexes with purine analogs, such as triazolopyrimidines represent a wide perspective in therapeutical use as anticancer, antimetastatic and antiparasitic agents.

Author(s):  
Toichiro Kuwabara

Although scanning electron microscopy has a great potential in biological application, there are certain limitations in visualization of the biological structure. Satisfactory techniques to demonstrate natural surfaces of the tissue and the cell have been reported by several investigators. However, it is commonly found that the surface cell membrane is covered with a minute amount of mucin, secretory substance or tissue fluid as physiological, pathological or artefactual condition. These substances give a false surface appearance, especially when the tissue is fixed with strong fixatives. It seems important to remove these coating substances from the surface of the cell for demonstration of the true structure.


2019 ◽  
Author(s):  
Jumpei Morimoto ◽  
Yasuhiro Fukuda ◽  
Takumu Watanabe ◽  
Daisuke Kuroda ◽  
Kouhei Tsumoto ◽  
...  

<div> <div> <div> <p>“Peptoids” was proposed, over decades ago, as a term describing analogs of peptides that exhibit better physicochemical and pharmacokinetic properties than peptides. Oligo-(N-substituted glycines) (oligo-NSG) was previously proposed as a peptoid due to its high proteolytic resistance and membrane permeability. However, oligo-NSG is conformationally flexible and is difficult to achieve a defined shape in water. This conformational flexibility is severely limiting biological application of oligo-NSG. Here, we propose oligo-(N-substituted alanines) (oligo-NSA) as a new peptoid that forms a defined shape in water. A synthetic method established in this study enabled the first isolation and conformational study of optically pure oligo-NSA. Computational simulations, crystallographic studies and spectroscopic analysis demonstrated the well-defined extended shape of oligo-NSA realized by backbone steric effects. The new class of peptoid achieves the constrained conformation without any assistance of N-substituents and serves as an ideal scaffold for displaying functional groups in well-defined three-dimensional space, which leads to effective biomolecular recognition. </p> </div> </div> </div>


Biomics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 344-377
Author(s):  
A.R. Sakhabutdinova ◽  
K.I. Mikhailenko ◽  
R.R. Garafutdinov ◽  
O.Yu. Kiryanova ◽  
M.A. Sagitova ◽  
...  

2020 ◽  
Vol 26 (36) ◽  
pp. 4658-4674 ◽  
Author(s):  
Christina Kannigadu ◽  
David. D. N'Da

: 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.


2020 ◽  
Vol 21 ◽  
Author(s):  
Amritpal Kaur ◽  
Gaurav Chaudhary ◽  
Pargat Singh ◽  
Sandeep Arora ◽  
Rajwinder Kaur

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.


Author(s):  
Jaya Dwivedi ◽  
Neetu Yaduvanshi ◽  
Shruti Shukla ◽  
Sonika Jain

: Since 1887, phenoxazine derivatives have attracted attention of chemist due to its versatile utility, industrially and pharmacologically. Literature is found abundant with various pharmacological activities of phenoxazine derivatives like antitumor, anticancer, antifungal, antibacterial, anti-inflammatory, anti-diabetic, anti-viral, anti-malarial, antidepressant, analgesic and many other drug resistance reversal activities. This review covers detailed over-view on pharmacological application of phenoxazine nucleus, its chemistry and reactivity and also illustrating the incorporation of different group at different positions enhancing its biological application, besides some synthetic procedures.


2010 ◽  
Vol 2 (4) ◽  
pp. 227-238 ◽  
Author(s):  
Gerardo Perozziello ◽  
Giuseppina Simone ◽  
Patrizio Candeloro ◽  
Francesco Gentile ◽  
Natalia Malara ◽  
...  

2021 ◽  
Vol 15 (1) ◽  
Author(s):  
Moayad Moawia ZainElabdin Ahmed ◽  
Haytham Hussein Mohammed Osman ◽  
Alaa Hatim Ameer Mohamed ◽  
Alaaeldin Ginawi

Abstract Background Schistosomiasis is a parasitic infection that commonly affects the gastrointestinal and genitourinary tracts. Cerebral schistosomiasis is rare, and few operative cases have been reported in the literature. Diagnosis is usually challenging due to the similarity of the lesion to many other brain conditions. Treatment usually requires surgical resection combined with the use of antiparasitic agents, which often results in good outcomes and excellent prognosis. Case presentation A 24-year-old, previously healthy Afro-asiatic man presented to our neurosurgical outpatient clinic complaining of headache and an attack of convulsions. On examination, he had bilateral lower limb weakness more on the right side. Laboratory investigations including stool and urine general test results were unremarkable. Magnetic resonance imaging of the brain was performed and showed an intra-axial left parietal mass; a granulomatous lesion was suggested in the differential diagnoses. The patient underwent craniotomy and total resection of the lesion. Histopathology confirmed the presence of active cerebral Schistosoma mansoni infection. Orally administered praziquantel was initiated at a dose of 20 mg/kg twice a day for a total of 3 days along with oral administration of corticosteroids for 2 weeks. The patient improved postoperatively without residual weakness and with no further convulsions. Conclusion Cerebral schistosomiasis is a rare but important consideration in the list of differential diagnoses of cerebral space-occupying lesions. This is of particular importance in in endemic areas like Sudan. In order to reach a diagnosis, careful social and occupational history need to be obtained and correlated with the clinical, laboratory, and radiological findings. Surgical resection along with the use of proper antiparasitic agents usually provides the best clinical outcomes.


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