Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine

1990 ◽  
Vol 33 (8) ◽  
pp. 2188-2192 ◽  
Author(s):  
C. K. Chu ◽  
V. S. Bhadti ◽  
K. J. Doshi ◽  
J. T. Etse ◽  
J. M. Gallo ◽  
...  
Keyword(s):  
In Vivo Studies ◽  
Brain Targeting ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Dihydropyridine Derivatives

Traditional Medicines, HIV, and Related Infections

2011 ◽  
Vol 23 (1) ◽  
pp. 159-164 ◽  
Author(s):  
M. Patel ◽  
P. Bessong ◽  
H. Liu
Keyword(s):  
Clinical Trials ◽  
Immune System ◽  
Ethical Issues ◽  
Mechanisms Of Action ◽  
Antiretroviral Drugs ◽  
In Vivo Studies ◽  
Traditional Medicines ◽  
Anti Hiv

Traditional medicines are an integral part of health care worldwide, even though their efficacy has not been scientifically proven. HIV-infected individuals may use them singularly or in combination with conventional medicines. Many in vitro studies have proven the anti-HIV, anti- Candida, and anti–herpes simplex virus potential of traditional plants and identified some of the mechanisms of action. Very few in vivo studies are available that involve a small number of participants and show controversial results. In addition, knowledge is limited of the role of traditional medicines in the enhancement of the immune system. The use of traditional medicines with antiretroviral drugs (ARVs) has created a problem because drug interactions compromise the efficacy of ARVs. Several currently popular plants have been studied in the laboratory for their interaction with ARVs, with disadvantageous results. Unfortunately, no clinical trials are available. The science of traditional medicines is relatively new and is at present being modernized worldwide. However, there are still ethical issues regarding traditional medicines that need to be addressed—for example, regulations regarding quality control and standardization of medicines, regulation and education of healers who deliver these medicines, and unregulated clinical trials. The workshop addressed the following questions about traditional medicine and their use in HIV infection: What are the mechanisms of action of anti-HIV traditional medicines? Should traditional medicines be used in conjunction with ARV? Do traditional medicines enhance the immune system? Should medicinal plants be used for the control of oral infections associated with HIV? What are the ethical issues surrounding the use of traditional medicines for the treatment of HIV and associated infections?

Mono and Dually Decorated Nanoliposomes for Brain Targeting, In Vitro and In Vivo Studies

2013 ◽  
Vol 31 (5) ◽  
pp. 1275-1289 ◽  
Author(s):  
E. Markoutsa ◽  
K. Papadia ◽  
A. D. Giannou ◽  
M. Spella ◽  
A. Cagnotto ◽  
...  
Keyword(s):  
In Vivo Studies ◽  
Brain Targeting

Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies

2016 ◽  
Vol 503 (1-2) ◽  
pp. 127-140 ◽  
Author(s):  
Ghada M. El-Zaafarany ◽  
Mahmoud E. Soliman ◽  
Samar Mansour ◽  
Gehanne A.S. Awad
Keyword(s):  
In Vivo Studies ◽  
Brain Targeting

Preparation, characterization, and optimization of asenapine maleate mucoadhesive nanoemulsion using Box-Behnken design: In vitro and in vivo studies for brain targeting

2020 ◽  
Vol 586 ◽  
pp. 119499 ◽  
Author(s):  
Santosh Ashok Kumbhar ◽  
Chandrakant R. Kokare ◽  
Birendra Shrivastava ◽  
Bapi Gorain ◽  
Hira Choudhury
Keyword(s):  
In Vivo Studies ◽  
Brain Targeting ◽  
Box Behnken Design

Synthesis, characterization and 99mTc-radiolabelling of specific derivatives of alpha thymosin peptides for in vitro and in vivo studies

2011 ◽  
Author(s):  
Chrysoula-Evangelia Karachaliou ◽  
Christos Zikos ◽  
Dimitra Benaki ◽  
Maria Pelecanou ◽  
Ourania Tsitsilonis ◽  
...  
Keyword(s):  
In Vivo Studies ◽  
Derivatives Of

Design, Synthesis, Molecular Modeling and Anti-HIV Assay of Novel Quinazolinone Incorporated Coumarin Derivatives

2020 ◽  
Vol 18 (1) ◽  
pp. 41-51 ◽  
Author(s):  
Mahdieh Safakish ◽  
Zahra Hajimahdi ◽  
Mohammad R. Aghasadeghi ◽  
Rouhollah Vahabpour ◽  
Afshin Zarghi
Keyword(s):  
Therapeutic Index ◽  
In Vivo Studies ◽  
One Pot ◽  
Design Synthesis ◽  
Phenyl Derivative ◽  
Hiv Therapy ◽  
Anti Hiv Agents ◽  
Anti Hiv

Background: The emergence of drug-resistant viral strains has created the need for the development of novel anti-HIV agents with a diverse structure that targets key enzymes in the HIV lifecycle. Objective: Considering the pharmacophore of integrase inhibitors, one of the validated targets for anti-HIV therapy, we designed a quinazolinone incorporated coumarin scaffold to affect HIV. Method: Coumarin is a beta enol ester and also a well-known drug scaffold. Designed structures were prepared using a one-pot three-compo Results: In vitro anti-HIV and cytotoxicity assay indicated that more than half of the compounds had EC50 values lower than 50 µM. Unsubstituted phenyl derivative showed the highest activity and selectivity with an EC50 value of 5 µM and a therapeutic index of 7. Compounds were docked into the integrase active site to investigate the probable mechanism of action. Accordingly, the hydroxyl moiety of coumarin along with the carbonyl of the quinazolinone ring could function as the metal chelating group. Quinazolinone and phenyl groups interact with side chains of IN residues, as well. Conclusion: Here, a novel anti-HIV scaffold is represented for further modification and in-vivo studies.

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