scholarly journals Prodrugs of Antiinfective Agents: A Review

2016 ◽  
Vol 19 (1) ◽  
pp. 82 ◽  
Author(s):  
Mona Piplani ◽  
Avtar Chand Rana ◽  
Prabodh Chander Sharma
Keyword(s):  
Active Drug ◽  
Therapeutic Effectiveness ◽  
Pharmacological Properties ◽  
Conventional Drug ◽  
Pharmacokinetic Properties ◽  
Antiinfective Agents ◽  
Productive Area ◽  
Human Therapy ◽  
Synthetic Approaches ◽  
Derivatives Of

Prodrugs are the pharmacologically inactive derivatives of active drugs typically intended to optimize the exposure of active drug at target site, through manipulation of its physicochemical, biopharmaceutical or pharmacokinetic properties. This approach has a number of advantages over conventional drug administration. Antiinfective agents are associated with number of limitations, responsible for their reduced bioavailability. Various antiinfective prodrugs have been synthesized with reduced side effects and improved pharmacological properties. The present paper illustrates different vistas of prodrug approach of antiinfective agents describing brief classification, synthetic approaches, pharmacological aspects and recent patents. It is a very productive area of research and its prologue in human therapy has given triumphant outcomes in improving the clinical and therapeutic effectiveness of drugs.This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Building Blocks ◽  
Vital Role ◽  
Review Of Literature ◽  
Drug Discovery Process ◽  
Active Compounds ◽  
Lead Compounds ◽  
Synthetic Approaches ◽  
Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

„IN SILICO“ PREDICTION OF PHARMACOKINETIC PROPERTIES AND DRUGLIKENESS OF NOVEL THIOUREA DERIVATIVES OF NAPROXEN

2021 ◽  
Author(s):  
Nikola V. Nedeljković ◽  
◽  
Vladimir D. Dobričić ◽  
Marina Ž. Mijajlović ◽  
Gordana P. Radić ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Aromatic Amines ◽  
Gastrointestinal Absorption ◽  
Skin Permeability ◽  
Thiourea Derivatives ◽  
Barrier Permeability ◽  
Brain Barrier Permeability ◽  
Pharmacokinetic Properties ◽  
Inhibitory Potential ◽  
Derivatives Of

Masking the carboxyl group of naproxen with other functional groups may be a promising strategy to decrease its gastrointestinal toxicity. Thiourea moiety has been described as an important pharmacophore in a variety of pharmacologically active compounds, including anti-inflammatory, antiviral, anticancer, hypoglycemic and antimicrobial agents. Our research group has previously designed twenty novel thiourea derivatives of naproxen, containing amino acids (glycine, L-alanine, β-alanine, L-valine and L-phenylalanine – compounds 1,2,3,4 and 5, respectively), their methyl (6–10) and ethyl esters (11–15), as well as aromatic amines (16–20). Pharmacokinetic properties and druglikeness of these compounds were predicted using SwissADME web tool (http://www.swissadme.ch/). Predicted pharmacokinetic properties include potential for gastrointestinal absorption, blood-brain barrier permeability, skin permeability, transport mediated by P-glycoproteins and enzyme inhibitory potential. Druglikeness was evaluated using Lipinski’s, Ghose’s, Veber’s, Egan’s and Muegge’s rules, as well as on the basis of bioavailability score. All tested compounds had high-predicted gastrointestinal absorption and low blood-brain barrier permeability. Also, derivatives 2, 4, 7, 9, 10, 12, 14, 15 and 18 were predicted to be substrates for P-glycoprotein. Derivatives with aromatic amines (16–20) showed inhibitory potential against all tested CYP isoforms. Derivative 19 had the highest, while derivative 13 demonstrated the lowest predicted skin permeability. Finally, derivatives 1–12, except 5 and 10, have druglike structures, since they obey to all imposed rules.

scholarly journals Structural-Functional Analysis of 2,1,3-Benzoxadiazoles and Their N-oxides As HIV-1 Integrase Inhibitors

Acta Naturae ◽  
2013 ◽  
Vol 5 (1) ◽  
pp. 63-72 ◽  
Author(s):  
S. P. Korolev ◽  
O. V. Kondrashina ◽  
D. S. Druzhilovsky ◽  
A. M. Starosotnikov ◽  
M. D. Dutov ◽  
...  
Keyword(s):  
Integrase Inhibitor ◽  
Integrase Inhibitors ◽  
Mechanism Of Inhibition ◽  
Immunodeficiency Virus ◽  
Pharmacokinetic Properties ◽  
Nitro Derivatives ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

Human immunodeficiency virus type 1 integrase is one of the most attractive targets for the development of anti-HIV-1 inhibitors. The capacity of a series of 2,1,3-benzoxadiazoles (benzofurazans) and their N-oxides (benzofuroxans) selected using the PASS software to inhibit the catalytic activity of HIV-1 integrase was studied in the present work. Only the nitro-derivatives of these compounds were found to display inhibitory activity. The study of the mechanism of inhibition by nitro-benzofurazans/benzofuroxans showed that they impede the substrate DNA binding at the integrase active site. These inhibitors were also active against integrase mutants resistant to raltegravir, which is the first HIV-1 integrase inhibitor approved for clinical use. The comparison of computer-aided estimations of the pharmacodynamic and pharmacokinetic properties of the compounds studied and raltegravir led us to conclude that these compounds show promise and need to be further studied as potential HIV-1 integrase inhibitors.

scholarly journals Bioactive Prenyl- and Terpenyl-Quinones/Hydroquinones of Marine Origin †

Marine Drugs ◽  
2018 ◽  
Vol 16 (9) ◽  
pp. 292 ◽  
Author(s):  
Pablo García ◽  
Ángela Hernández ◽  
Arturo San Feliciano ◽  
Mª Castro
Keyword(s):  
Secondary Metabolites ◽  
Marine Organisms ◽  
Chemical Diversity ◽  
Rich Source ◽  
Pharmacological Properties ◽  
Active Compounds ◽  
Marine Origin ◽  
Synthetic Approaches

The sea is a rich source of biological active compounds, among which terpenyl-quinones/hydroquinones constitute a family of secondary metabolites with diverse pharmacological properties. The chemical diversity and bioactivity of those isolated from marine organisms in the last 10 years are summarized in this review. Aspects related to synthetic approaches towards the preparation of improved bioactive analogues from inactive terpenoids are also outlined.

Azaheterocyclic Derivatives of ortho-Carborane: Synthetic Strategies and Application Opportunities

Synthesis ◽  
2019 ◽  
Vol 52 (03) ◽  
pp. 337-352 ◽  
Author(s):  
Lidiia A. Smyshliaeva ◽  
Mikhail V. Varaksin ◽  
Valery N. Charushin ◽  
Oleg N. Chupakhin
Keyword(s):  
Materials Science ◽  
Cross Coupling ◽  
General Character ◽  
Advanced Technologies ◽  
Substituted Acetylenes ◽  
Synthetic Approaches ◽  
Derivatives Of ◽  
Coupling Strategies

Azaheterocyclic derivatives of 1,2-dicarba-closo-dodeca­borane (ortho-carborane) are known to be of particular interest due to numerous plausible applications, particularly, in medicine, materials science, and advanced technologies. Three principal synthetic strategies resulting in azaheterocyclic carboranes, in which boron-enriched and azaheterocyclic fragments are linked to each other, either directly by means of the C–C bonds or through a short spacer (CH2, CH2S, CH2O, etc.), have been outlined. These synthetic approaches are of general character and can be used both individually and in combination to afford promising organoboron clusters of diverse architectures.1 Introduction2 C–C Cross-Coupling Strategies in the Synthesis of Azahetero­cyclic Carboranes3 Carboryne-Based Transformation Strategies4 Condensation Strategies: Reactions of Decaborane B10H14 with Substituted Acetylenes5 Conclusion and Outlook

Synthesis and pharmacological properties of certain derivatives of octahydroacridines

1968 ◽  
Vol 2 (6) ◽  
pp. 310-312 ◽  
Author(s):  
V. G. Ermolaeva ◽  
V. G. Yashunskii ◽  
A. I. Polezhaeva ◽  
M. D. Mashkovskii
Keyword(s):  
Pharmacological Properties ◽  
Derivatives Of

scholarly journals Synthetic Approaches to Organoselenium Derivatives with Antimicrobial and Anti-Biofilm Activity

2019 ◽  
Vol 16 (6) ◽  
pp. 589-601 ◽  
Author(s):  
Iris Di Leo ◽  
Federica Messina ◽  
Vanessa Nascimento ◽  
Francesca G. Nacca ◽  
Donatella Pietrella ◽  
...  
Keyword(s):  
Glutathione Peroxidase ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Pharmacological Properties ◽  
Organoselenium Compounds ◽  
Synthetic Approaches ◽  
First Time

In the recent years, an increasing attention has been given to the biological activities exerted by organoselenium compounds. In 1984, Sies reported for the first time the ability of ebselen to mimic the activity of glutathione peroxidase. From this milestone, several studies reported the pharmacological properties of selenium-containing compounds including their exploitation as antimicrobials. In this context, this minireview presents the most recent examples of seleno derivatives endowed with antimicrobial activities while discussing the most interesting and recent synthetic procedures used to obtain these compounds.

ChemInform Abstract: SYNTHESIS AND PHARMACOLOGICAL PROPERTIES OF N-AMINOACYL DERIVATIVES OF BETA-PHENYLISOPROPYLAMINE

1975 ◽  
Vol 6 (29) ◽  
pp. no-no
Author(s):  
L. A. DAVANKOVA ◽  
A. D. NEKLYUDOV ◽  
R. A. AL'TSHULER ◽  
N. N. SUVOROV
Keyword(s):  
Pharmacological Properties ◽  
Derivatives Of
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