a b s t r a c tHepatitis C virus (HCV) mortality and morbidity is a world health misery with an approximate 130e150 million chronically HCV tainted and suffering individuals and it initiate critical liver malfunction like cirrhosis, hepatocellular carcinoma or liver HCV cancer. HCV NS5B protein one of the best studied therapeutic target for the identification of new drug candidates to be added to the combination or multiple combination medication recently approved. During the past few years, NS5B has thus been an important object of attractive medicinal chemistry endeavors, which induced to the surfacing of betrothal preclinical drug molecules. In this scenario, the current review set limit to discuss research published on NS5B and few other therapeutic functional inhibitors concentrating on hit investigation, hit to lead optimization, ADME parameters evaluation, and the SAR data which was out for each compound type and similarity taken into consideration. The discussion outlined in this specific review will surly helpful and vital tool for those medicinal chemists investigators working with HCV research programs mainly pointing on NS5B and set broad spectrum identification of creative anti HCV compounds. This mini review also tells each and every individual compound ability related how much they are active against NS5B and few other targets.
Background:
A series of 2-aminothiazole schiff’s bases (1-24) were synthesized and
screened against a few neglected tropical disorders (NTDs). Compounds 12 and 14 were found to
have antitrypanosidal activity, whereas compound 14 was found to be more effective than standard
benznidazole. The antiplasmodial assay provided three specific and effective compounds (9, 12 and
24) than standard chloroquine. Compound (21) inhibited Leishmania infantum, almost similar to
Miltefosine.
Methods:
All the compounds were subjected to cytotoxicity assay and none of the compounds
were found to be cytotoxicity. Molecular docking simulations revealed that four compounds (1, 9,
12 and 21) were found to similarly occupy the hydrophobic active site of trans-2-enoyl acyl carrier
protein reductase of P. falciparum (PfENR) as triclosan and outcomes were closely related to their
anti-malarial potencies.
Results and Conclusion:
The screening results against T. cruzi, T. brucei, L. donovani, L. infantum,
P. falciferum and cytotoxicity assays provided a few significant to most potent compounds;
two variant class of NTDs.
The Middle East Respiratory Syndrome (MERS) is caused by the novel coronavirus belongs to the family Betacoronaviridae was first identified in Saudi Arabia during 2012. The first epidemic outbreak of the MERS-CoV has been started reporting in the South Korea and other Asian Countries. The disease was transmitted to humans to humans from the Middle East to other countries through travelling history. The MERS-CoV is responsible for the lower acute and severe respiratory disorder causes the shortness of breath along with fever and cough. The treatment for the disease is purely symptomatic and vaccination is not existed. In the present work we are tried to compile the epidemiology, pathogenesis, viral genome and currently available drugs. At the last the promising approaches for the drug design and development process has been presented.
Background:
Cancer caused nearly 8.8 million deaths in 2015. Limited efficacy, selectivity,
drug resistance and toxicity are major complications associated with chemotherapy, potentiating
the discovery of anticancer agents.
Methods:
A new series of N-(7-hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)acetamide/benzamide
analogues (5a-j) was prepared from the precursor, 7-hydroxy-4-methyl-2H-chromen-2-one (3), as
anticancer agent. The structural assignment of quinolone analogues (5a-j) was based on spectroscopic
data analyses. The cytotoxicity was tested on breast cancer cell lines (MCF7 and MDA-MB-
231) by sulforhodamine B (SRB) assay and three dose-related parameters GI50, TGI, and LC50 were
calculated.
Results:
2-(2-chlorophenoxy)-N-(7-hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)acetamide (5a)
showed the most potent cytotoxicity against the MCF7 and MDA-MB-231 cancer cell lines with
GI50 of 18.7 and 48.1 µM respectively. The glide scores of the compounds, 5a-d were found to be
related to the cytotoxicity profile and the emodel scores for ligands, 5a-j were found to be related to
significant cytotoxicity.
Conclusion:
Compound 5a exhibited the most potent cytotoxicity and this report may provide some
predictions to design more potent novel quinolines as cytotoxic agents.
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