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  • 1
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2021
    In:  Current Computer-Aided Drug Design Vol. 17, No. 7 ( 2021-12), p. 850-864
    In: Current Computer-Aided Drug Design, Bentham Science Publishers Ltd., Vol. 17, No. 7 ( 2021-12), p. 850-864
    Abstract: The HIV-1 pandemic is undoubtedly the major public-health crisis of our time. The extensive research on HIV has deepen ed our understanding of its pathogenesis and transmission dynamics. Some new entity molecules have been approved by the FDA for HIV treatment but till now protective vaccine remains elusive. Scientists are targeting many important proteins of HIV-1; gp41, gp120, CCR5 coreceptor, integrase, reverse transcriptase and protease. Few compounds are used as nucleotide analogues to stop HIV replication. Altogether, these compounds and their derivatives specifically block HIV entry and DNA replication. Using ADMET studies, people are working on these compounds to reduce toxicity and increase potency. Objective: Our main aim is to discuss the Pharmacokinetics properties of 23 important FDA antiretroviral drugs used for the treatment of HIV-1 infections. Methods: We have searched literature related to pharmacokinetics properties in PubMed, Google Scholar search engine. Conclusion: Here, we have reviewed the pharmacokinetic properties such as absorption, bioavailability, distribution, metabolism, and excretion, of important 23 FDA approved drugs. The drugs namely Fuzeon, Selzentry, Complera, Epivir, Retrovir, Emtriva, Ziagen, Edurant, Intelence, Pifeltro, Sustiva, Viramune, Isentress, Genvoya, Tivicay, Reyataz, Prezista, Lexiva, Invirase, Aptivus etc. are classified into five major classes: fusion inhibitors, Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs), Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs), Integrase Strand transfer inhibitors (INSTIs) and Protease inhibitors (PIs). This Review may helpful for the future development of potent antiretroviral drugs with improved pharmacokinetic properties.
    Type of Medium: Online Resource
    ISSN: 1573-4099
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
    SSG: 15,3
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  • 2
    In: Phytotherapy Research, Wiley, ( 2010-06-07), p. n/a-n/a
    Type of Medium: Online Resource
    ISSN: 0951-418X , 1099-1573
    Language: English
    Publisher: Wiley
    Publication Date: 2010
    detail.hit.zdb_id: 1493490-5
    SSG: 15,3
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  • 3
    Online Resource
    Online Resource
    American Chemical Society (ACS) ; 2012
    In:  Journal of Medicinal Chemistry Vol. 55, No. 23 ( 2012-12-13), p. 10662-10673
    In: Journal of Medicinal Chemistry, American Chemical Society (ACS), Vol. 55, No. 23 ( 2012-12-13), p. 10662-10673
    Type of Medium: Online Resource
    ISSN: 0022-2623 , 1520-4804
    Language: English
    Publisher: American Chemical Society (ACS)
    Publication Date: 2012
    detail.hit.zdb_id: 1491411-6
    SSG: 15,3
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  • 4
    Online Resource
    Online Resource
    Bentham Science Publishers Ltd. ; 2023
    In:  Letters in Drug Design & Discovery Vol. 20, No. 4 ( 2023-04), p. 469-478
    In: Letters in Drug Design & Discovery, Bentham Science Publishers Ltd., Vol. 20, No. 4 ( 2023-04), p. 469-478
    Abstract: Ursolic acid (UA, 3β-hydroxy-urs-12-en-28-oic acid), a pentacyclic triterpenoid from various medicinal plants, has been blessed with proven biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial, but its bioavailability and solubility limit its clinical application. Objective: Synthesis of UA-based hybrid molecules to explore their antibacterial and synergy potential in combination with azithromycin (AZT) for the treatment of multidrug-resistant (MDR) bacterial infections. Methods: Hybrid molecules of UA with menthol, eugenol, and nalidixic acid (NAL) along with some other ester derivatives were synthesized, and evaluated for their antibacterial and synergy potential in combination with AZT against the clinical isolate of Escherichia coli in terms of their minimum inhibitory concentration (MIC), fold reduction in MIC, fractional inhibitory concentration index (FICI) and type of interaction. In silico screening of pharmacokinetic parameters, docking affinity against efflux pump proteins AcrA, AcrB, and TolC was performed on the most potent derivative 7 (3-O-nalidixoyl UA). Results: Derivative 7 showed MIC of 62.5 µg/mL and a strong synergistic effect with AZT reducing the MIC of AZT from 100 to 0.19 µg/mL (512-fold reduction) against E. coli at a concentration of 12.5 µg/mL. Other derivatives neither showed antibacterial activity of their own (MIC 〉 1000 µg/mL) nor any significant synergistic interaction in combination with AZT. The in silico studies on 7 revealed improved druggability parameters over the parent UA and NAL. Conclusion: The findings highlight derivative 7 as strong synergistic agent in combination with AZT which may be further investigated to render its efficient use for the treatment of MDR bacterial infections.
    Type of Medium: Online Resource
    ISSN: 1570-1808
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2023
    SSG: 15,3
    Location Call Number Limitation Availability
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