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1.
Int J Surg ; 110(4): 2498-2501, 2024 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-38215252

RESUMEN

The SARS-CoV-2 subvariant BA.2.86 'Pirola', first identified in Denmark in August 2023, has manifested with a significantly mutated spike protein profile, suggesting a heightened ability to evade vaccine-induced and infection-induced antibodies. This article outlines the epidemiological spread, immune response implications, and global responses to BA.2.86. Preliminary observations indicate community transmissions of the subvariant, even among those previously infected or vaccinated. Notably, the BA.2.86 infection has shown a potential to amplify antibody responses. The variant's emergence has evoked memories of the Omicron variant's rise in late 2021, though global immunity levels might modulate the impact of BA.2.86 impact differently. Continuous genomic surveillance, coupled with integrated diagnostic and epidemiological strategies, proves crucial in early detection and management. The emergence of BA.2.86 reaffirms the unpredictable nature of the COVID-19 pandemic, emphasizing the need for ongoing research, adaptability, and global collaboration.


Asunto(s)
COVID-19 , Salud Global , SARS-CoV-2 , Humanos , COVID-19/epidemiología , COVID-19/inmunología , SARS-CoV-2/inmunología , SARS-CoV-2/genética , Glicoproteína de la Espiga del Coronavirus/inmunología , Glicoproteína de la Espiga del Coronavirus/genética , Vacunas contra la COVID-19/inmunología
2.
Assay Drug Dev Technol ; 18(7): 308-317, 2020 10.
Artículo en Inglés | MEDLINE | ID: mdl-32749851

RESUMEN

Naproxen (NAP) is one of the commonly used nonselective Cycloxygenase (COX) inhibitors. It is a choice of drug for anti-inflammatory activity by subsiding the generation of the inflammatory components called prostaglandins. The common problem associated with the NAP is gastrointestinal toxicity. It may cause ulceration or stomach bleeding. In this study, the different derivatives of NAP were designed by using phytophenols with the aim that they exert the antioxidant activity and have the potential to reduce ulcer formation. The lead molecules were designed by molecular docking-based virtual screening against human COX-2 enzyme through AutoDock. Then these derivatives were screened for pharmacokinetic profiling by considering Lipinski's filter. The potent and safe molecule was identified by pharmacokinetics and toxicity evaluation. The potent compound was synthesized in the laboratory, purified, characterized, and its pharmacological activities were evaluated. The resultant compound was found to be equipotent and less toxic than the parent compound.


Asunto(s)
Inhibidores de la Ciclooxigenasa 2/farmacología , Ciclooxigenasa 2/metabolismo , Diseño de Fármacos , Simulación del Acoplamiento Molecular , Naproxeno/farmacología , Inhibidores de la Ciclooxigenasa 2/química , Humanos , Estructura Molecular , Naproxeno/química
3.
Open Med Chem J ; 11: 146-195, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-29387273

RESUMEN

INTORODUCTION: Prodrug approach deals with chemical biotransformation or enzymatic conversion or involves inactive or less active bio-reversible derivatives of active drug molecules. They have to pass through enzymatic or chemical biotransformation before eliciting their pharmacological action. METHODS & MATERIALS: The two different pharmacophores combine to give synergistic activity or may help in targeting the active drug to its target. Prodrug super seeds the problems of prodrug designing, for example solubility enhancement, bioavailability enhancement, chemical stability improvement, presystemic metabolism, site specific delivery, toxicity masking, improving patient acceptance, or eradicating undesirable adverse effects. RESULTS: As an outcome the search for a prodrug or mutual prodrug with reduced toxicity has continued during recent years. This present review emphasizes the common help to revamp physiochemical, pharmaceutical and therapeutic effectiveness of drugs. CONCLUSION: This gives the researcher a common platform where they can find prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation, ulcergenocity and bleeding).

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