Novel Broad-Spectrum Anthelmintics. Tetramisole1and Related Derivatives of 6-Arylimidazo[2,1-b]thiazole

1966 ◽  
Vol 9 (4) ◽  
pp. 545-551 ◽  
Author(s):  
Alfons H. M. Raeymaekers ◽  
Fernand T. N. Allewijn ◽  
Jan Vandenberk ◽  
Paul J. A. Demoen ◽  
Theo T. T. Van Offenwert ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Derivatives Of

Multiple types of hydroxyl-rich cationic derivatives of PGMA for broad-spectrum antibacterial and antifouling coatings

2016 ◽  
Vol 7 (36) ◽  
pp. 5709-5718 ◽  
Author(s):  
Huimin Yuan ◽  
Bingran Yu ◽  
Li-Hai Fan ◽  
Meng Wang ◽  
Yiwen Zhu ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antifouling Coatings ◽  
Derivatives Of

A series of hydroxyl-rich quaternized polymers with Ag ions have been proposed for broad-spectrum antibacterial and antifouling coatings.

scholarly journals Overproduction of Wild-Type and Bioengineered Derivatives of the Lantibiotic Lacticin 3147

2006 ◽  
Vol 72 (6) ◽  
pp. 4492-4496 ◽  
Author(s):  
Paul D. Cotter ◽  
Lorraine A. Draper ◽  
Elaine M. Lawton ◽  
Olivia McAuliffe ◽  
Colin Hill ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Structural Genes ◽  
Wild Type ◽  
Genetic Determinants ◽  
Lacticin 3147 ◽  
Genes Encoding ◽  
High Level ◽  
Derivatives Of

ABSTRACT Lacticin 3147 is a broad-spectrum two-peptide lantibiotic whose genetic determinants are located on two divergent operons on the lactococcal plasmid pMRC01. Here we introduce each of 14 subclones, containing different combinations of lacticin 3147 genes, into MG1363 (pMRC01) and determine that a number of them can facilitate overproduction of the lantibiotic. Based on these studies it is apparent that while the provision of additional copies of genes encoding the biosynthetic/production machinery and the regulator LtnR is a requirement for high-level overproduction, the presence of additional copies of the structural genes (i.e., ltnA1A2) is not.

Isothiourea derivatives of 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole with broad-spectrum anthelmintic activity

1987 ◽  
Vol 30 (10) ◽  
pp. 1848-1853 ◽  
Author(s):  
Malcolm D. Brewer ◽  
Roderick J. J. Dorgan ◽  
Brian R. Manger ◽  
Patrick Mamalis ◽  
Richard A. B. Webster
Keyword(s):  
Broad Spectrum ◽  
Anthelmintic Activity ◽  
Isothiourea Derivatives ◽  
Derivatives Of

Tissue distribution of 10-methoxycamptothecin and its metabolite 10-hydroxycamptothecin in rats by a RP-HPLC method with fluorescence detection/UV detection

2015 ◽  
Vol 7 (18) ◽  
pp. 7690-7696 ◽  
Author(s):  
Changmin Shao ◽  
Jian Zheng ◽  
Bo Fan ◽  
Shaman Luo ◽  
Jixiang Lin ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Tissue Distribution ◽  
Fluorescence Detection ◽  
Broad Spectrum ◽  
Hplc Method ◽  
Uv Detection ◽  
Camptotheca Acuminata ◽  
Rp Hplc ◽  
Derivatives Of

Both 10-methoxycamptothecin (MCPT) and 10-hydroxycamptothecin (HCPT) are natural derivatives of camptothecin (CPT) isolated from Camptotheca acuminata, possessing broad-spectrum antitumor activity.

scholarly journals 4′-Fluorouridine is an oral antiviral that blocks respiratory syncytial virus and SARS-CoV-2 replication

Science ◽  
2022 ◽  
Vol 375 (6577) ◽  
pp. 161-167
Author(s):  
Julien Sourimant ◽  
Carolin M. Lieber ◽  
Megha Aggarwal ◽  
Robert M. Cox ◽  
Josef D. Wolf ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Severe Acute Respiratory Syndrome ◽  
Broad Spectrum ◽  
Rna Viruses ◽  
Antiviral Drugs ◽  
Emerging Pathogens ◽  
Primary Indication ◽  
Syncytial Virus ◽  
Derivatives Of

Preparing antiviral defenses Antiviral drugs are an important tool in the battle against COVID-19. Both remdesivir and molnupiravir, which target the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) polymerase, were first developed against other RNA viruses. This highlights the importance of broad-spectrum antivirals that can be rapidly deployed against related emerging pathogens. Sourimant et al . used respiratory syncytial virus (RSV) as a primary indication in identifying further drugs that target the polymerase enzyme of RNA viruses. The authors explored derivatives of molnupiravir and identified 4′ fluorouridine (EIDD-2749) as an inhibitor of the polymerase of RSV and SARS-CoV-2. This drug can be delivered orally and was effective against RSV in mice and SARS-CoV-2 in ferrets. —VV

scholarly journals Derivatives of the antimalarial drug mefloquine are broad spectrum antifungal molecules with activity against drug-resistant clinical isolates

2019 ◽  
Author(s):  
Marhiah C. Montoya ◽  
Sarah Beattie ◽  
Kathryn M. Alden ◽  
Damian J. Krysan
Keyword(s):  
Antifungal Activity ◽  
Mechanism Of Action ◽  
Broad Spectrum ◽  
Fungal Infections ◽  
Clinical Isolates ◽  
In Vitro Toxicity ◽  
Drug Resistant ◽  
Candida Auris ◽  
Recent Emergence ◽  
Derivatives Of

ABSTRACTThe antifungal pharmacopeia is critically small, particularly in light of the recent emergence of multi-drug-resistant pathogens such as Candida auris. Herein, we report that derivatives of the anti-malarial drug mefloquine have broad spectrum antifungal activity against pathogenic yeasts and molds. In addition, the mefloquine derivatives have activity against clinical isolates that are resistant to one or more of the three classes of drugs currently used to treat invasive fungal infections, indicating that they have a novel mechanism of action. Importantly, the in vitro toxicity profiles using human cell lines indicate that the mefloquine derivatives are very similar to the parent mefloquine despite being up to 64-fold more active against fungal cells. In addition to direct antifungal activity, sub-inhibitory concentrations of the mefloquine derivatives inhibit the expression of virulence traits including filamentation in C. albicans and capsule formation/melanization in C. neoformans. Mode/mechanism of action experiments indicate that the mefloquine derivatives interfere with both mitochondrial and vacuolar function as part of a multi-target mechanism of action. The broad-spectrum scope of activity, blood-brain-barrier penetration, and large number of previously synthesized analogs available combine to support the further optimization and development of the antifungal activity of this general class of drug-like molecules.

Synthetic Methods for Novel Benzofuran Derivatives and their Biological Activities

2017 ◽  
Vol 1 (1) ◽  
Author(s):  
Bidyut Kumar Senapati
Keyword(s):  
Electronic Properties ◽  
Heterocyclic Compound ◽  
Broad Spectrum ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Present Review ◽  
The Past ◽  
Optical And Electronic Properties ◽  
Novel Approaches ◽  
Derivatives Of

Benzofuran is the heterocyclic compound consisting of fused benzene and furan rings. The benzofuran moiety is widely distributed in both natural and artificial molecules. Substituted benzofurans are pharmaceutically important heterocycles that display numerous biological activities such as antimicrobial, antifungal, antiHIV, anticancer, antimalarial, anti-inflammatory activities. Some derivatives of benzofurans are also used as organic materials due to their optical and electronic properties. Owing to their broad spectrum applications, it is of great significance to develop systematic and novel approaches to benzofurans. During the past decades, many synthetic efforts have been devoted so far to the synthesis of benzofuran derivatives. The present review highlights the recently synthesized benzofurans and their biological activities.

ChemInform Abstract: Isothiourea Derivatives of 6-Phenyl-2,3,5,6-tetrahydroimidazo(2,1-b)thiazole with Broad-Spectrum Anthelmintic Activity.

ChemInform ◽  
1988 ◽  
Vol 19 (10) ◽  
Author(s):  
M. D. BREWER ◽  
R. J. J. DORGAN ◽  
B. R. MANGER ◽  
P. MAMALIS ◽  
R. A. B. WEBSTER
Keyword(s):  
Broad Spectrum ◽  
Anthelmintic Activity ◽  
Isothiourea Derivatives ◽  
Derivatives Of

scholarly journals Synthesis, cytotoxic activity and drug combination study of tertiary amine derivatives of 2′,4′-dihydroxyl-6′-methoxyl-3′,5′-dimethylchalcone

RSC Advances ◽  
2017 ◽  
Vol 7 (76) ◽  
pp. 48031-48038 ◽  
Author(s):  
Chen Wang ◽  
Ping Wu ◽  
Xiao-Ling Shen ◽  
Xiao-Yi Wei ◽  
Zi-Hua Jiang
Keyword(s):  
Cytotoxic Activity ◽  
Tertiary Amine ◽  
Broad Spectrum ◽  
Drug Combination ◽  
Amine Derivative ◽  
Combination Study ◽  
Derivatives Of

Tertiary amine derivative of DMC (2b) exhibited broad spectrum of cytotoxicity and strong synergism with Taxol® against HeLa/Tax cells.

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