Synthesis, Anti-Hiv Activity, and Biological Properties of 2',3'-Didehydro-2',3'-Dideoxythwidine (d4T)

1989 ◽  
Vol 8 (5) ◽  
pp. 841-844 ◽  
Author(s):  
John Martin ◽  
Muzammia Mansuri ◽  
John Starrett ◽  
Jean-Pierre Sommadossi ◽  
Vera Brankovan ◽  
...  
ChemInform ◽  
2010 ◽  
Vol 31 (14) ◽  
pp. no-no
Author(s):  
Hitoshi Takeuchi ◽  
Naoki Asai ◽  
Kazunori Tanabe ◽  
Teruya Kozaki ◽  
Masanori Fujita ◽  
...  

1999 ◽  
Vol 52 (11) ◽  
pp. 971-982 ◽  
Author(s):  
HITOSHI TAKEUCHI ◽  
NAOKI ASAI ◽  
KAZUNORI TANABE ◽  
TERUYA KOZAKI ◽  
MASANORI FUJITA ◽  
...  

2014 ◽  
Vol 58 (6) ◽  
pp. 3043-3052 ◽  
Author(s):  
Marika Tiberi ◽  
Cristina Tintori ◽  
Elisa Rita Ceresola ◽  
Roberta Fazi ◽  
Claudio Zamperini ◽  
...  

ABSTRACTWe report here the synthesis of 2-aminothiazolones along with their biological properties as novel anti-HIV agents. Such compounds have proven to act through the inhibition of the gp120-CD4 protein-protein interaction that occurs at the very early stage of the HIV-1 entry process. No cytotoxicity was found for these compounds, and broad antiviral activities against laboratory strains and pseudotyped viruses were documented. Docking simulations have also been applied to predict the mechanism, at the molecular level, by which the inhibitors were able to interact within the Phe43 cavity of HIV-1 gp120. Furthermore, a preliminary absorption, distribution, metabolism, and excretion (ADME) evaluation was performed. Overall, this study led the basis for the development of more potent HIV entry inhibitors.


2020 ◽  
Vol 23 (24) ◽  
pp. 2679-2721 ◽  
Author(s):  
Evangelia-Eirini N. Vlachou ◽  
Konstantinos E. Litinas

Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khellactones and calanolides are usually potent and selective in anti-HIV activity. Decursin and decursinol derivatives are effective as anticancer, neuroprotective, antidiabetic, antibacterial, and antifungal agents.


Author(s):  
Jinling Qin ◽  
Weyland Cheng ◽  
Yong-Tao Duan ◽  
Hua Yang ◽  
Yongfang Yao

Background: Heterocyclic compounds, also called heterocycles, are a major class of organic chemicalcompound that plays a vital role in the metabolism of all living cells. The heterocyclic compound, indazole, has attracted more attention in recent years and is widely present in numerous commercially available drugs. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties. Methods: A literature search was conducted in PubMed, Google Scholar and Web of Science regarding articles related to indazole and its therapeutic application. Results: The mechanism and structure-activity relationship of indazole and its derivatives were described. Based on their versatile biological activities, the compounds were divided into six groups: anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour. At least 43 indazole-based therapeutic agents were found to be used in clinical application or clinical trials. Conclusion: This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compoundswhere the progress of approved marketed drugs containing indazole scaffold is examined from 1966 to the present day. Future direction involves more diverse bioactive moieties with indazole scaffold and greater insights into its mechanism.


2008 ◽  
Vol 3 (1) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Yoshinori Asakawa

The Marchantiophyta (liverworts) produce a number of terpenoids, aromatic compounds and acetogenins, several of which show interesting biological properties, such as antimicrobial, antifungal, allergenic contact dermatitis, insecticide, insect antifeedant, cytotoxic, piscicidal, muscle relaxing, plant growth regulatory, anti-HIV and DNA polymerase β inhibitory, anti-obesity and neurotrophic activities. The isolation and chemical structures of the active compounds are discussed.


2013 ◽  
Vol 49 (spe) ◽  
pp. 33-44 ◽  
Author(s):  
Anne-Marie Caminade ◽  
Cédric-Olivier Turrin ◽  
Jean-Pierre Majoral

Dendrimers are hyperbranched and perfectly defined macromolecules, constituted of branches emanating from a central core in an iterative fashion. Phosphorhydrazone dendrimers constitute a special family of dendrimers, possessing one phosphorus atom at each branching point. The internal structure of these dendrimers is hydrophobic, but hydrophilic terminal groups can induce the solubility of the whole structure in water. Indeed, the properties of these compounds are mainly driven by the type of terminal groups their bear; this is especially true for the biological properties. For instance, positively charged terminal groups are efficient for transfection experiments, as drug carriers, as anti-prion agents, and as inhibitor of the aggregation of Alzheimer's peptides, whereas negatively charged dendrimers have anti-HIV properties and can influence the human immune system, leading to anti-inflammatory properties usable against rheumatoid arthritis. This review will give the most representative examples of the biological properties of water-soluble phosphorhydrazone dendrimers, organized depending on the type of terminal groups they bear.


Author(s):  
Keisham S. Singh ◽  
Supriya Tilvi

: The marine sponges of the genus Oceanapia sp. is comprised of more than 50 species and are distributed in the seas around the tropical and subtropical regions. They are mainly found in the northern Indian oceans, Japan, and the south pacific coast. They are highly colored and known to be a rich source of various secondary metabolites, particularly, alkaloids. Several other secondary metabolites were also reported from this genus which include terpenes, sphingolipids, ceramides, cerebrosides, acetylenic acids, and thiocyanatins, etc. Many of these compounds isolated from this genus exhibited various biological properties including anticancer, antimicrobial, anti-HIV, ichthyotoxicity and nematocidal activities. Although several secondary metabolites have been reported from this genus, a dedicated review of the chemicals and biological activities of this genus is so far lacking. Keeping this in mind this review describes the various chemical entities isolated from the sponges of the genus Oceanapia detailing their chemical structures along with their reported biological properties.


1996 ◽  
Vol 61 (s1) ◽  
pp. 16-19 ◽  
Author(s):  
Nicolai E. Poopeiko ◽  
Alicja K. Drabikowska ◽  
Jaroslav Poznanski ◽  
David Shugar ◽  
Tadeusz Kulikowski

1992 ◽  
Vol 11 (2-4) ◽  
pp. 583-594 ◽  
Author(s):  
S. I. Shimizu ◽  
J. Balzarini ◽  
E. De Clercq ◽  
R. T. Walker

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