Review of the Syntheses and Activities of Some Sulfur-Containing Drugs

2020 ◽  
Vol 17 (3) ◽  
pp. 192-210 ◽  
Author(s):  
Criscieli Taynara Barce Ferro ◽  
Beatriz Fuzinato dos Santos ◽  
Caren Daniele Galeano da Silva ◽  
George Brand ◽  
Beatriz Amaral Lopes da Silva ◽  
...  
Keyword(s):  
Chemical Compounds ◽  
Sulfur Compounds ◽  
Important Class ◽  
Materials Chemistry ◽  
Drug Candidates ◽  
Wide Range ◽  
Synthetic Routes ◽  
Pharmaceutical Properties ◽  
Sulfur Containing ◽  
Sulfur Containing Compounds

Background: Sulfur-containing compounds represent an important class of chemical compounds due to their wide range of biological and pharmaceutical properties. Moreover, sulfur-containing compounds may be applied in other fields, such as biological, organic, and materials chemistry. Several studies on the activities of sulfur compounds have already proven their anti-inflammatory properties and use to treat diseases, such as Alzheimer’s, Parkinson’s, and HIV. Moreover, examples of sulfur-containing compounds include dapsone, quetiapine, penicillin, probucol, and nelfinavir, which are important drugs with known activities. Objective: This review will focus on the synthesis and application of some sulfur-containing compounds used to treat several diseases, as well as promising new drug candidates. Results: Due to the variety of compounds containing C-S bonds, we have reviewed the different synthetic routes used toward the synthesis of sulfur-containing drugs and other compounds.

scholarly journals Sulfur and Sulfur Compounds in Plant Defence

2012 ◽  
Vol 7 (3) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Ifeanyi D. Nwachukwu ◽  
Alan J. Slusarenko ◽  
Martin C. H. Gruhlke
Keyword(s):  
Natural Products ◽  
New Technologies ◽  
Plant Defence ◽  
Sulfur Compounds ◽  
Oxidation States ◽  
Chemical Structures ◽  
Wide Range ◽  
Sulfur Containing ◽  
Sulfur Containing Compounds

The multiplicity of chemical structures of sulfur containing compounds, influenced in part by the element's several oxidation states, directly results in diverse modes of action for sulfur-containing natural products synthesized as secondary metabolites in plants. Sulfur-containing natural products constitute a formidable wall of defence against a wide range of pathogens and pests. Steady progress in the development of new technologies have advanced research in this area, helping to uncover the role of such important plant defence molecules like endogenously-released elemental sulphur, but also deepening current understanding of other better-studied compounds like the glucosinolates. As studies continue in this area, it is becoming increasingly evident that sulfur and sulfur compounds play far more important roles in plant defence than perhaps previously suspected.

scholarly journals Substrate recognition and ATPase activity of the E. coli cysteine/cystine ABC transporter YecSC-FliY

2020 ◽  
Vol 295 (16) ◽  
pp. 5245-5256 ◽  
Author(s):  
Siwar Sabrialabed ◽  
Janet G. Yang ◽  
Elon Yariv ◽  
Nir Ben-Tal ◽  
Oded Lewinson
Keyword(s):  
Atpase Activity ◽  
Abc Transporter ◽  
Conformational Changes ◽  
Binding Protein ◽  
Substrate Binding ◽  
Transporter Family ◽  
Wide Range ◽  
Substrate Binding Protein ◽  
Sulfur Containing ◽  
Sulfur Containing Compounds

Sulfur is essential for biological processes such as amino acid biogenesis, iron–sulfur cluster formation, and redox homeostasis. To acquire sulfur-containing compounds from the environment, bacteria have evolved high-affinity uptake systems, predominant among which is the ABC transporter family. Theses membrane-embedded enzymes use the energy of ATP hydrolysis for transmembrane transport of a wide range of biomolecules against concentration gradients. Three distinct bacterial ABC import systems of sulfur-containing compounds have been identified, but the molecular details of their transport mechanism remain poorly characterized. Here we provide results from a biochemical analysis of the purified Escherichia coli YecSC-FliY cysteine/cystine import system. We found that the substrate-binding protein FliY binds l-cystine, l-cysteine, and d-cysteine with micromolar affinities. However, binding of the l- and d-enantiomers induced different conformational changes of FliY, where the l- enantiomer–substrate-binding protein complex interacted more efficiently with the YecSC transporter. YecSC had low basal ATPase activity that was moderately stimulated by apo FliY, more strongly by d-cysteine–bound FliY, and maximally by l-cysteine– or l-cystine–bound FliY. However, at high FliY concentrations, YecSC reached maximal ATPase rates independent of the presence or nature of the substrate. These results suggest that FliY exists in a conformational equilibrium between an open, unliganded form that does not bind to the YecSC transporter and closed, unliganded and closed, liganded forms that bind this transporter with variable affinities but equally stimulate its ATPase activity. These findings differ from previous observations for similar ABC transporters, highlighting the extent of mechanistic diversity in this large protein family.

Sulfatase regulation and antibiotic synthesis in Cephalosporium acremonium

1969 ◽  
Vol 15 (2) ◽  
pp. 175-181 ◽  
Author(s):  
David W. Dennen ◽  
Diane D. Carver
Keyword(s):  
Amino Acid ◽  
Culture Medium ◽  
Sulfur Compounds ◽  
Cephalosporin C ◽  
Cephalosporium Acremonium ◽  
Antibiotic Synthesis ◽  
Cellular Processes ◽  
High Level ◽  
Sulfur Containing ◽  
Sulfur Containing Compounds

The sulfatase of Cephalosporium acremonium is regulated by exogenous sulfur compounds, repressed in cells in 0.02 M sulfate, and derepressed in 5 × 10−4 M sulfate. Organic sulfur sources, such as cysteine, homocysteine, and methionine, derepress the enzyme in varying degrees while the latter amino acid is also required for maximum synthesis of the antibiotics cephalosporin C and penicillin N. Sulfatase-repressed cells transferred from sulfate to methionine-containing medium produce a high level of these antibiotics in the culture medium and a proportionate derepression of the sulfatase. Cycloheximide inhibits sulfatase derepression in cultures transferred from sulfate to methionine medium while having negligible effect on antibiotic synthesis. Mutant cultures of C. acremonium, with an increased potential to synthesize sulfur-containing antibiotics, have decreased ability to degrade methionine for other cellular requirements and sulfatase derepression is proportionately increased. The sulfatase is thus regulated by the biosynthesis of cephalosporin C and penicillin N at the expense of sulfur-containing compounds required for other cellular processes.

N,N-Diethyl-p-phenylenediamine effectiveness in analysis of polysulfides and polythionates in water

2008 ◽  
Vol 5 (3) ◽  
pp. 226 ◽  
Author(s):  
Stephen Kariuki ◽  
Philippe Babady-Bila ◽  
Breanna Duquette
Keyword(s):  
Oxidation State ◽  
Environmental Samples ◽  
Environmental Pollutants ◽  
Spectrophotometric Analysis ◽  
Sulfur Compounds ◽  
Metallic Ions ◽  
Sulfur Species ◽  
Related Compounds ◽  
Sulfur Containing ◽  
Sulfur Containing Compounds

Environmental context. The importance of hydrogen sulfide as well as some of the reduced sulfur species such as polysulfides as environmental pollutants is a result of their toxicity, unpleasant odour, and their reactivity with metals and metallic ions found in various environmental samples. Although known to be popular, the effectiveness of N,N-diethyl-p-phenylenediamine and other related compounds in the spectrophotometric analysis of such sulfur compounds in water as well as in other environmental samples has not been fully investigated. Our results show that although the quantification of simple sulfides in the environmental samples may be easily accomplished spectrophotometrically by using N,N-diethyl-p-phenylenediamine, the level of difficulty in analysing such compounds may increase with their increasing sulfur chain. Abstract. The analysis of polysulfides, polythionates and other sulfur species likely to be found in poorly aerated environmental samples such as water is presented. In-depth spectrophotometric testing carried out using N,N-diethyl-p-phenylenediamine shows that the well known acidification-and-purge method is not sufficiently suitable for the analysis of polysulfides and other low oxidation-state sulfur compounds that contain a sulfur chain longer than two. Further, this study finds that the use of chromium(II) which acts as a reducing agent to the sulfur-containing compounds improves the spectrophotometric analysis of the polysulfides and polythionates in water, but only slightly. The extent of reduction of polysulfides and polythionates to sulfide by chromium appears dependent upon the oxidation state of sulfur as well as the chain length in the polysulfidic compounds.

Distribution of Sulfur Forms in Low Temperature Pyrolysis of Coal

2012 ◽  
Vol 512-515 ◽  
pp. 834-837
Author(s):  
Qiu Xiang Yao ◽  
Mei Li Du ◽  
Shui Li Wang ◽  
Jing Liu ◽  
Jian Li Yang ◽  
...  
Keyword(s):  
Low Temperature ◽  
Coal Tar ◽  
Northwest China ◽  
Sulfur Compounds ◽  
Organic Sulfur ◽  
Total Sulfur ◽  
Low Temperature Pyrolysis ◽  
Sulfur Containing ◽  
Sulfur Containing Compounds ◽  
Typical Method

The distribution of sulfur forms in the products of low temperature pyrolysis of Carboniferous high sulfur coal from Northwest China was investigated. The typical method of Gray-King assay was used to carry out the low temperature pyrolysis experiments. GC-MS analysis was used to investigate the composition of sulfur compounds in the coal tar. The results show that sulfur mainly remained in the semi-coke and accounted for 80.97% of the total sulfur. Pyrites decomposed and transformed into sulfates and organic sulfur. 5 sulfur containing compounds were detected in the coal tar and they are dibenzothiophene, benzonaphthothiophene and their substituted homologs.

Privileged Structures in the Design of Potential Drug Candidates for Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4323-4354 ◽  
Author(s):  
Ana Cristina Lima Leite ◽  
José Wanderlan Pontes Espíndola ◽  
Marcos Veríssimo de Oliveira Cardoso ◽  
Gevanio Bezerra de Oliveira Filho
Keyword(s):  
Biologically Active ◽  
Neglected Diseases ◽  
Financial Return ◽  
Drug Candidates ◽  
Lead Compounds ◽  
Wide Range ◽  
Methods Of Synthesis ◽  
Current Therapies ◽  
Resistant Strains ◽  
Privileged Structures

Background: Privileged motifs are recurring in a wide range of biologically active compounds that reach different pharmaceutical targets and pathways and could represent a suitable start point to access potential candidates in the neglected diseases field. The current therapies to treat these diseases are based in drugs that lack of the desired effectiveness, affordable methods of synthesis and allow a way to emergence of resistant strains. Due the lack of financial return, only few pharmaceutical companies have been investing in research for new therapeutics for neglected diseases (ND). Methods: Based on the literature search from 2002 to 2016, we discuss how six privileged motifs, focusing phthalimide, isatin, indole, thiosemicarbazone, thiazole, and thiazolidinone are particularly recurrent in compounds active against some of neglected diseases. Results: It was observed that attention was paid particularly for Chagas disease, malaria, tuberculosis, schistosomiasis, leishmaniasis, dengue, African sleeping sickness (Human African Trypanosomiasis - HAT) and toxoplasmosis. It was possible to verify that, among the ND, antitrypanosomal and antiplasmodial activities were between the most searched. Besides, thiosemicarbazone moiety seems to be the most versatile and frequently explored scaffold. As well, phthalimide, isatin, thiazole, and thiazolidone nucleus have been also explored in the ND field. Conclusion: Some described compounds, appear to be promising drug candidates, while others could represent a valuable inspiration in the research for new lead compounds.

Therapeutic Properties of Several Chemical Compounds from Salvia officinalis L. in Alzheimer’s Disease

2020 ◽  
Vol 21 ◽  
Author(s):  
Georgiana Uță ◽  
Denisa Ștefania Manolescu ◽  
Speranța Avram
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Side Effects ◽  
Chemical Compounds ◽  
Natural Compounds ◽  
Salvia Officinalis ◽  
Chemical Structures ◽  
In Silico Studies ◽  
Wide Range ◽  
Salvia Officinalis L

Background.: Currently, the pharmacological management in Alzheimer's disease is based on several chemical structures, represented by acetylcholinesterase and N-methyl-D-aspartate (NMDA) receptor ligands, with still unclear molecular mechanisms, but severe side effects. For this reason, a challenge for Alzheimer's disease treatment remains to identify new drugs with reduced side effects. Recently, the natural compounds, in particular certain chemical compounds identified in the essential oil of peppermint, sage, grapes, sea buckthorn, have increased interest as possible therapeutics. Objectives.: In this paper, we have summarized data from the recent literature, on several chemical compounds extracted from Salvia officinalis L., with therapeutic potential in Alzheimer's disease. Methods.: In addition to the wide range of experimental methods performed in vivo and in vitro, also we presented some in silico studies of medicinal compounds. Results. Through this mini-review, we present the latest information regarding the therapeutic characteristics of natural compounds isolated from Salvia officinalis L. in Alzheimer's disease. Conclusion.: Thus, based on the information presented, we can say that phytotherapy is a reliable therapeutic method in a neurodegenerative disease.

1,4-Diazepines: A Review on Synthesis, Reactions and Biological Significance

2019 ◽  
Vol 16 (5) ◽  
pp. 709-729 ◽  
Author(s):  
Muhammad A. Rashid ◽  
Aisha Ashraf ◽  
Sahibzada S. Rehman ◽  
Shaukat A. Shahid ◽  
Adeel Mahmood ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Significance ◽  
Biological Evaluation ◽  
Wide Range ◽  
Pharmaceutical Industries ◽  
Biological Aspects ◽  
Synthetic Routes ◽  
Biological Attributes ◽  
Synthesis Reactions ◽  
Potential Use

Background:1,4-Diazepines are two nitrogen containing seven membered heterocyclic compounds and associated with a wide range of biological activities. Due to its medicinal importance, scientists are actively involved in the synthesis, reactions and biological evaluation of 1,4-diazepines since number of decades.Objective:The primary purpose of this review is to discuss the synthetic schemes and reactivity of 1,4- diazepines. This article also describes biological aspects of 1,4-diazepine derivatives, that can be usefully exploited for the pharmaceutical sector.Conclusion:This review summarizes the abundant literature on synthetic routes, chemical reactions and biological attributes of 1,4-diazepine derivatives. We concluded that 1,4-diazepines have significant importance due to their biological activities like antipsychotic, anxiolytic, anthelmintic, anticonvulsant, antibacterial, antifungal and anticancer. 1,4-diazepine derivatives with significant biological activities could be explored for potential use in the pharmaceutical industries.

Cucurbitacins as Anticancer Agents: A Patent Review

2019 ◽  
Vol 14 (2) ◽  
pp. 133-143 ◽  
Author(s):  
Hidayat Hussain ◽  
Ivan R. Green ◽  
Muhammad Saleem ◽  
Khanzadi F. Khattak ◽  
Muhammad Irshad ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Wide Spectrum ◽  
Biological Effects ◽  
Therapeutic Effects ◽  
Cytotoxic Effects ◽  
Natural Sources ◽  
Oh Groups ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

Background: Cucurbitacins belong to a group of tetracyclic triterpenoids that display a wide range of biological effects. In the past, numerous cucurbitacins have been isolated from natural sources and many active compounds have been synthesized using the privileged scaffold in order to enhance its cytotoxic effects. Objective: his review covers patents on the therapeutic effects of natural cucurbitacins and their synthetic analogs published during the past decade. By far, the majority of patents published are related to cancer and Structure-Activity Relationships (SAR) of these compounds are included to lend gravitas to this important class of natural products. Methods: The date about the published patents was downloaded via online open access patent databases. Results: Cucurbitacins display significant cytotoxic properties, in particular cucurbitacins B and D which possess very potent effects towards a number of cancer cells. Numerous cucurbitacins isolated from natural sources have been derivatized through chemical modification at the C(2)-OH and C(25)- OH groups. Most importantly, an acyl ester of the C(25)-OH and, iso-propyl, n-propyl and ethyl ether groups of the C(2)-OH demonstrated the most increased cytotoxic activity. Conclusion: The significant cytotoxic effects of natural and semi-synthetic cucurbitacins make them attractive as new drug candidates. Moreover, cucurbitacins have the capability to form conjugates with other anticancer drugs which will synergistically enhance their anticancer effects. The authors believe that in order to get lead compounds, there should be a greater focus on the synthesis of homodimers, heterodimers, and halo derivatives of cucurbitacins. In the opinion of the authors the analysis of the published patents on the cucurbitacins indicates that these compounds can be developed into a regimen to treat a wide spectrum of cancers.

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