scholarly journals A greatly improved procedure for the synthesis of an antibiotic-drug candidate 2,4-diacetylphloroglucinol over silica sulphuric acid catalyst: multivariate optimisation and environmental assessment protocol comparison by metrics

RSC Advances ◽  
2020 ◽  
Vol 10 (53) ◽  
pp. 31824-31837
Author(s):  
Triana Kusumaningsih ◽  
Wahyu Eko Prasetyo ◽  
Maulidan Firdaus
Keyword(s):  
Sulphuric Acid ◽  
Environmental Assessment ◽  
Acid Catalyst ◽  
Drug Candidate ◽  
Synthetic Method ◽  
Assessment Protocol ◽  
Antibiotic Drug

A greatly improved procedure for the synthesis of antibiotic 2,4-diacetylphloroglucinol has been developed via a newly advanced synthetic method.

Brilacidin, a COVID-19 Drug Candidate, demonstrates broad-spectrum antiviral activity against human coronaviruses OC43, 229E and NL63 through targeting both the virus and the host cell

2021 ◽  
Author(s):  
Yanmei Hu ◽  
Hyunil Jo ◽  
William DeGrado ◽  
Jun Wang
Keyword(s):  
Antiviral Activity ◽  
Cell Surface ◽  
Host Cell ◽  
Mechanism Of Action ◽  
Broad Spectrum ◽  
Drug Candidate ◽  
Host Defense Peptides ◽  
Antibiotic Drug ◽  
Host Cell Surface ◽  
Human Coronaviruses

Brilacidin, a mimetic of host defense peptides (HDPs), is currently in phase 2 clinical trial as an antibiotic drug candidate. A recent study reported that brilacidin has antiviral activity against SARS-CoV-2 by inactivating the virus. In this work, we discovered an additional mechanism of action of brilacidin by targeting heparan sulfate proteoglycans (HSPGs) on host cell surface. Brilacidin, but not acetyl brilacidin, inhibits the entry of SARS-CoV-2 pseudovirus into multiple cell lines, and heparin, a HSPG mimetic, abolishes the inhibitory activity of brilacidin on SARS-CoV-2 pseudovirus cell entry. In addition, we found that brilacidin has broad-spectrum antiviral activity against multiple human coronaviruses (HCoVs) including HCoV-229E, HCoV-OC43, and HCoV-NL63. Mechanistic studies revealed that brilacidin has a dual antiviral mechanism of action including virucidal activity and binding to coronavirus attachment factor HSPGs on host cell surface. Brilacidin partially loses its antiviral activity when heparin was included in the cell cultures, supporting the host-targeting mechanism. Drug combination therapy showed that brilacidin has a strong synergistic effect with remdesivir against HCoV-OC43 in cell culture. Taken together, this study provides appealing findings for the translational potential of brilacidin as a broad-spectrum antiviral for coronaviruses including SARS-CoV-2.

Efficient and Eco-Friendly Synthesis of Fluorenone Azines by Using Sulphated Titania Acid Catalyst

2015 ◽  
Vol 58 ◽  
pp. 137-143 ◽  
Author(s):  
V. Arun ◽  
K.R. Sankaran
Keyword(s):  
Reaction Time ◽  
Acid Catalyst ◽  
Recyclable Catalyst ◽  
Synthetic Method ◽  
Synthetic Route ◽  
Operating Method

Conjugated unsymmetrical azines have been synthesized in the presence of acid catalyst sulphated-titania (TiO2-SO42-) from fluorenone hydrazone with substituted aldehydes and acetophenones by using mortar and pestle. The scope of present synthetic route avoid in solvents, simple operating method and shorter reaction time. Special feature of synthetic method is recyclable catalyst for all in reactions.

scholarly journals THE SYNTHESIS OF 1,3-DIMETHYL-6,7-DIMETHOXY-3,4-DIHYDROISOQUINOLINE FROM METHYLEUGENOL : APPLICATION OF RITTER REACTION FOR DIRECTLY CYCLIZATION

2010 ◽  
Vol 6 (3) ◽  
pp. 286-291 ◽  
Author(s):  
M. Farid Rahman ◽  
Elvina Dhiaul Iftitah
Keyword(s):  
Sulphuric Acid ◽  
Room Temperature ◽  
Acid Catalyst ◽  
Empirical Method ◽  
Low Energy ◽  
Ritter Reaction ◽  
Experimental Laboratory ◽  
Semi Empirical

The synthesis of 1,3-dimethyl-6,7-dimethoxy-3,4-dihydroisoquinoline from methyleugenol with application of Ritter reaction for directly cyclization was presented. This research was carried out in 2 steps : (1) Determination of intermediate stability that undergo in the reaction by using hyperchem version 6 with AM 1 semi empirical method, and (2) Synthesis of dihydroisoquinoline from methyleugenol and acetonitrile with acid catalyst (H2SO4) in the laboratory. The result of AM 1 calculation found that generally, the intermediate encourage the formation dihydroisoquinoline product, had low energy were compared with the intermediate in other product. Therefore, the dihydroisoquinoline product was easily formed. The result of experimental laboratory found that dihydroisoquinoline could be synthesed from methyleugenol and acetonitrile in the presence sulphuric acid under reflux in 74,92% yields. In despite, the minor product was formed with amount 6,74%. While the reaction at room temperature gave dihydroisoquinoline in poor yield about 11,42%.   Keywords: stability of intermediate, dihydroisoquinoline, Ritter reaction

scholarly journals Integrated Environmental Assessment of streams in the Sinos River basin in the state of Rio Grande do Sul, Brazil

2015 ◽  
Vol 75 (2 suppl) ◽  
pp. 105-113 ◽  
Author(s):  
MA Kieling-Rubio ◽  
T Benvenuti ◽  
GM Costa ◽  
CT Petry ◽  
MAS Rodrigues ◽  
...  
Keyword(s):  
River Basin ◽  
Environmental Assessment ◽  
Rapid Assessment ◽  
Habitat Diversity ◽  
Human Consumption ◽  
Assessment Protocol ◽  
Integrated Diagnosis ◽  
Tradescantia Pallida ◽  
Integrated Environmental Assessment ◽  
Biological Methods

<p>The deterioration of environmental quality in the Sinos River basin is directly associated with the impacts of intense industrialization and urbanization. An integrated environmental assessment (IEA) was conducted in July and September of 2012, in areas along the sources of the EstânciaVelha/Portão, Pampa and Schmidt streams using physical, chemical and biological methods. The water in the three sampling sites was not proper for human consumption, presented a low toxic contamination index (TCI) and mesotrophic characteristics. One site was included in Class 4, and two, in Class 3, according to current legislation. The rapid assessment protocol (RAP) indicated a natural environmental condition for habitat diversity and environmental impact in the three sites. The <italic>Tradescantia pallida</italic> (Rose) D.R. Hunt var. <italic>purpurea</italic> Boom biomarker showed water genotoxicity in two of the sites. The integrated diagnosis of water quality in these streams is fundamentally important to ensure the sustainable management of water resources and their multiple uses, as well to estimate their contribution to pollution in this river basin.</p>

An Efficient Large-Scale Synthesis of EDP-420, a First-in-Class Bridged Bicyclic Macrolide (BBM) Antibiotic Drug Candidate

2010 ◽  
Vol 14 (3) ◽  
pp. 504-510 ◽  
Author(s):  
Guoyou Xu ◽  
Datong Tang ◽  
Yonghua Gai ◽  
Guoqiang Wang ◽  
Heejin Kim ◽  
...  
Keyword(s):  
Large Scale ◽  
Drug Candidate ◽  
Antibiotic Drug ◽  
Large Scale Synthesis

scholarly journals Synthesis and Physical Properties of Estolide Ester Using Saturated Fatty Acid and Ricinoleic Acid

2011 ◽  
Vol 2011 ◽  
pp. 1-4 ◽  
Author(s):  
Jumat Salimon ◽  
Neeranjini Nallathamby ◽  
Nadia Salih ◽  
Bashar Mudhaffar Abdullah
Keyword(s):  
Fatty Acid ◽  
Low Temperature ◽  
Physical Properties ◽  
Sulphuric Acid ◽  
Ricinoleic Acid ◽  
Saturated Fatty Acid ◽  
Acid Catalyst ◽  
Flash Point ◽  
Viscosity Range

A study was conveyed to produce estolide ester using ricinoleic acid as the backbone. The ricinoleic acid reacted with saturated fatty acid from C8–C18. These reactions were conducted under vacuum at 60°C for 24 h without solvent. The reaction used acid catalyst, sulphuric acid. The new saturate ricinoleic estolide esters show superior low-temperature properties (−52 ± 0.08°C) and high flash point (>300°C). The yield of the neat estolide esters ranged from 52% to 96%. The viscosity range was 51 ± 0.08 to 86 ± 0.01 cp. These new saturated estolide esters were also compared with saturated branched estolide esters.

scholarly journals A Facile Approach to the Synthesis of 3-Acylisoxazole Derivatives by the Use of Reusable Solid Acid Catalysts

Synthesis ◽  
2021 ◽  
Author(s):  
Ken-ichi Itoh ◽  
Mamiko Hayakawa ◽  
Rina Abe ◽  
Shinji Takahashi ◽  
Kenta Hasegawa ◽  
...  
Keyword(s):  
Silica Gel ◽  
Heterogeneous Catalysts ◽  
Solid Acid ◽  
Solid Acid Catalyst ◽  
Acid Catalyst ◽  
Solid Acid Catalysts ◽  
Synthetic Method ◽  
Acid Catalysts ◽  
Amberlyst 15 ◽  
Nitrile Oxides

Nitrile oxides were obtained from α-nitro ketones by the use of silica-gel supported sodium hydrogensulfate (NaHSO4/SiO2) or Amberlyst 15 as solid acid catalyst, and then the corresponding 3-acylisoxaszoles were obtained from alkynes via the 1,3-dipolar ([3+2]) cycloaddition. These heterogeneous catalysts are easily separable from the reaction mixture, and reused up to the synthesis. This synthetic method provides a facile, efficient and reusable production of 3-acylisoxazoles.

scholarly journals A SOFTWARE SYSTEM FOR PREDICTING AND RESEARCHING ANTIFUNGAL ANTIBIOTICS’ PROPERTIES

2021 ◽  
pp. 68-74
Author(s):  
Eldar E. Musayev ◽  
◽  
Tamara B. Chistyakova ◽  
Valery V. Belakhov ◽  
◽  
...  
Keyword(s):  
Drug Binding ◽  
Drug Candidate ◽  
Software System ◽  
Binding Prediction ◽  
Client Server ◽  
Deterministic Algorithms ◽  
Antifungal Antibiotics ◽  
Antibiotic Drug ◽  
Software Development Practices ◽  
Server Architecture

In this work we present a software system that enables antifungal antibiotic drug candidate toxicity and likelihood of drug binding prediction. The system is composed of a number of machine learning models and deterministic algorithms. Its implementation utilizes modern software development practices including a client-server architecture with a thin web-client. Testing showed the models’ accuracy and viability for predicting antifungal antibiotics’ properties.

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