scholarly journals Scaffold hybridization strategy towards potent hydroxamate-based inhibitors ofFlaviviridaeviruses andTrypanosomaspecies

MedChemComm ◽  
2019 ◽  
Vol 10 (6) ◽  
pp. 991-1006 ◽  
Author(s):  
Erofili Giannakopoulou ◽  
Vasiliki Pardali ◽  
Efseveia Frakolaki ◽  
Vasileios Siozos ◽  
Vassilios Myrianthopoulos ◽  
...  
Keyword(s):  
Chemical Entity ◽  
Design And Synthesis ◽  
Single Chemical

Design and synthesis of potent inhibitors with dual activity by successfully merging two distinct scaffolds into a single chemical entity.

scholarly journals Chiral Polythiophenes: Part I: Syntheses of Monomeric Precursors

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4205
Author(s):  
Dorota Krasowska ◽  
Rafał Karpowicz ◽  
Józef Drabowicz
Keyword(s):  
Thin Layer ◽  
Chemical Entity ◽  
Single Chemical ◽  
Synthetic Approaches

The purpose of this mini-review is to comprehensively present the synthetic approaches used for the preparation of non-racemic mono- and multi-substituted thiophenes, which, in turn, can be applied as precursors for the synthesis of chiral polythiophenes isolated as a single chemical entity or having supramolecular thin-layer architectures.

Endoperoxide Carbonyl Falcipain 2/3 Inhibitor Hybrids: Toward Combination Chemotherapy of Malaria through a Single Chemical Entity

2010 ◽  
Vol 53 (22) ◽  
pp. 8202-8206 ◽  
Author(s):  
Peter Gibbons ◽  
Edite Verissimo ◽  
Nuna C. Araujo ◽  
Victoria Barton ◽  
Gemma L. Nixon ◽  
...  
Keyword(s):  
Combination Chemotherapy ◽  
Chemical Entity ◽  
Single Chemical

Single Chemical Entity Legal Highs: Assessing the Risk for Long Term Harm

2012 ◽  
Vol 5 (4) ◽  
pp. 304-319 ◽  
Author(s):  
Carolyn B. McNabb ◽  
Bruce R. Russell ◽  
Daniele Caprioli ◽  
David J. Nutt ◽  
Simon Gibbons ◽  
...  
Keyword(s):  
Chemical Entity ◽  
Legal Highs ◽  
Single Chemical

scholarly journals Are Antimalarial Hybrid Molecules a Close Reality or a Distant Dream?

2017 ◽  
Vol 61 (5) ◽  
Author(s):  
Drishti Agarwal ◽  
Rinkoo D. Gupta ◽  
Satish K. Awasthi
Keyword(s):  
Multidrug Resistant ◽  
Chemotherapeutic Agents ◽  
Content Type ◽  
Design And Synthesis ◽  
Lead Compounds ◽  
Novel Drugs ◽  
Hybrid Molecules ◽  
Single Chemical ◽  
Late Stages ◽  
Shed Light

ABSTRACT Emergence of drug-resistant Plasmodium falciparum strains has led to a situation of haste in the scientific and pharmaceutical communities. Hence, all their efforts are redirected toward finding alternative chemotherapeutic agents that are capable of combating multidrug-resistant parasite strains. In light of this situation, scientists have come up with the concept of hybridization of two or more active pharmacophores into a single chemical entity, resulting in “antimalarial hybrids.” The approach has been applied widely for generation of lead compounds against deadly diseases such as cancer and AIDS, with a proven potential for use as novel drugs, but is comparatively new in the sphere of antimalarial drug discovery. A sudden surge has been evidenced in the number of studies on the design and synthesis of hybrids for treating malaria and may be regarded as proof of their potential advantages over artemisinin-based combination therapy (ACT). However, it is evident from recent studies that most of the potential advantages of antimalarial hybrids, such as lower toxicity, better pharmacokinetics, and easier formulation, have yet to be realized. A number of questions left unaddressed at present need to be answered before this approach can progress to the late stages of clinical development and prove their worth in the clinic. To the best of our knowledge, this compilation is the first attempt to shed light on the shortcomings that are surfacing as more and more studies on molecular hybridization of the active pharmacophores of known antimalarials are being published.

scholarly journals A divergent route towards single-chemical entity triazine dendrimers with opportunities for structural diversity

2007 ◽  
Vol 31 (7) ◽  
pp. 1283 ◽  
Author(s):  
Hannah Crampton ◽  
Emily Hollink ◽  
Lisa M. Perez ◽  
Eric E. Simanek
Keyword(s):  
Structural Diversity ◽  
Chemical Entity ◽  
Single Chemical

Multitargeted drugs discovery: Balancing anti-amyloid and anticholinesterase capacity in a single chemical entity

2011 ◽  
Vol 21 (9) ◽  
pp. 2655-2658 ◽  
Author(s):  
Maria Laura Bolognesi ◽  
Manuela Bartolini ◽  
Andrea Tarozzi ◽  
Fabiana Morroni ◽  
Federica Lizzi ◽  
...  
Keyword(s):  
Chemical Entity ◽  
Single Chemical

Prostatic Acid Phosphatase (PAP) Differentiated Ultracytochemically from Lysosomal Acid Phosphate in the Rat with a PAP/Specific Substrate, Phosphorylcholine

1975 ◽  
Vol 33 ◽  
pp. 450-451
Author(s):  
W. Allen Shannon ◽  
José A. Serrano ◽  
Hannah L. Wasserkrug ◽  
Anna A. Serrano ◽  
Arnold M. Seligman
Keyword(s):  
Acid Phosphatase ◽  
Phosphate Buffer ◽  
Prostatic Carcinoma ◽  
Prostatic Acid Phosphatase ◽  
Chemotherapeutic Agents ◽  
Specific Substrate ◽  
Acid Phosphate ◽  
Lysosomal Acid ◽  
Design And Synthesis ◽  
New Chemotherapeutic Agents

During the design and synthesis of new chemotherapeutic agents for prostatic carcinoma based on phosphorylated agents which might be enzyme-activated to cytotoxicity, phosphorylcholine, [(CH3)3+NCH2CH2OPO3Ca]Cl-, has been indicated to be a very specific substrate for prostatic acid phosphatase (PAP). This phenomenon has led to the development of specific histochemical and ultracytochemical methods for PAP using modifications of the Gomori lead method for acid phosphatase. Comparative histochemical results in prostate and kidney of the rat have been published earlier with phosphorylcholine (PC) and β-glycerophosphate (βGP). We now report the ultracytochemical results.Minced tissues were fixed in 3% glutaraldehyde-0.1 M phosphate buffered (pH 7.4) for 1.5 hr and rinsed overnight in several changes of 0.05 M phosphate buffer (pH 7.0) containing 7.5% sucrose. Tissues were incubated 30 min to 2 hr in Gomori acid phosphatase medium (2) containing 0.1 M substrate, either PC or βGP.

Tailoring microstructures of materials through biomimetics

1993 ◽  
Vol 51 ◽  
pp. 500-501
Author(s):  
Mehmet Sarikaya ◽  
Ilhan A. Aksay
Keyword(s):  
Chemical Properties ◽  
Design And Synthesis ◽  
Structure Sensitive ◽  
Macro Scale ◽  
Methods Of Synthesis ◽  
Successive Level ◽  
Engineering Materials ◽  
Physical And Chemical ◽  
And Chemical Properties ◽  
Synthesis Of Materials

Biomimetics involves investigation of structure, function, and methods of synthesis of biological composite materials. The goal is to apply this information to the design and synthesis of materials for engineering applications.Properties of engineering materials are structure sensitive through the whole spectrum of dimensions from nanometer to macro scale. The goal in designing and processing of technological materials, therefore, is to control microstructural evolution at each of these dimensions so as to achieve predictable physical and chemical properties. Control at each successive level of dimension, however, is a major challenge as is the retention of integrity between successive levels. Engineering materials are rarely fabricated to achieve more than a few of the desired properties and the synthesis techniques usually involve high temperature or low pressure conditions that are energy inefficient and environmentally damaging.In contrast to human-made materials, organisms synthesize composites whose intricate structures are more controlled at each scale and hierarchical order.

Design and synthesis of azaisoflavones

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
B Kang ◽  
YJ Jung ◽  
R Jeon
Keyword(s):  
Design And Synthesis

Computer Modeling-Assisted Design And Synthesis Of Flavonols Derivatives As Proteasome Inhibitors

Planta Medica ◽  
2016 ◽  
Vol 82 (05) ◽  
Author(s):  
KY Orabi ◽  
MS Abaza ◽  
KA ElSayed ◽  
AY Elnagar ◽  
SI Faggal ◽  
...  
Keyword(s):  
Computer Modeling ◽  
Proteasome Inhibitors ◽  
Design And Synthesis
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