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1.
ACS Omega ; 9(16): 18566-18575, 2024 Apr 23.
Artículo en Inglés | MEDLINE | ID: mdl-38680340

RESUMEN

We generated novel elven 1,2,3,6-tetrahydrophthalimides and tetrahydroquinazoline derivatives from 1,2,3,6-tetrahydrophthalic anhydride (1) in response to our interest in using the anhydrides to produce heterocyclic nitrogen compounds. The elemental and spectral analyses of the produced compounds validated the recommended configurations and MOE 2014.09 (Molecular Operating Environment) computations were used to perform their in silico analysis. The synthesized compounds have been analyzed and put through various experiments, including in vitro and in silico methods to assess their biological activity against Escherichia coli Penicillin-Binding Protein 3 (PBP3) and Staphylococcus aureus Penicillin-Binding Protein 2 (PBP2), among these compounds showing promising data as antibacterial drugs.

2.
Sci Rep ; 14(1): 2548, 2024 Jan 31.
Artículo en Inglés | MEDLINE | ID: mdl-38291193

RESUMEN

In the current report, we have successfully synthesized nanocomposites of PMMA incorporating different doping of CeO2 through a chemical approach. XRD results reflects decent matching for CeO2 nanoparticles with 29 nm crystallite size. FTIR spectroscopy demonstrates the characteristic functional groups validating the successful formation of the composite. The optical study of PMMA and the nanocomposites has proven that the optical properties such as band gap, refractive index, optical permittivity, and loss tangent factor are affected by adding CeO2 to the PMMA matrix.The peak residing around 420 nm by UV measurements is allocated to occurring electrons photoexcitation from the valence to conduction band inherent in CeO2. The dielectric measurements were achieved using broadband dielectric spectroscopy upon a wide span of frequencies (10-1-107 Hz) and within temperatures from - 10 to 80 °C with a step of 10 °C. The permittivity decreases by adding CeO2 and the dielectric parameters are thermally enhanced, however, the temperature influence is based on CeO2 content, the higher the CeO2 amount, the higher the influence of temperature. The results of the nanocomposites revealed antibacterial activity counter to gram-positive bacteria strain (S. aureus, and B. subtilis), and gram-negative bacteria (E. coli, and K. pneumoniae), yeast (C. albicans, as well as fungi (A. niger). Inherently, the change in CeO2 concentration from 0.01 to 0.1 wt% delivers maximum influence against gram-negative bacteria. These PMMA CeO2-doped composites are beneficial for optoelectronic areas and devices.

3.
Expert Opin Pharmacother ; 23(9): 1051-1063, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35400255

RESUMEN

INTRODUCTION: Sexual dysfunction (SD) and depression have a bidirectional relationship. The rising prescription of antidepressants, especially those with a serotonergic effect, is associated with increased SD. Sexual dysfunction reduces compliance and increases risk of recurrence of depressive episodes. Various strategies have been studied to manage antidepressant-induced SD. AREAS COVERED: This review covers the identification of symptoms of antidepressant-induced SD, prevalence of symptoms in association with commonly used antidepressants, and the main lines of management, with a focus on pharmacological strategies. EXPERT OPINION: The management of antidepressant-induced SD aims to reduce the unwanted sexual adverse effects while maintaining an acceptable control of depressive symptoms. It should implicate a multidisciplinary approach and determination of baseline sexual function and SD risk factors. In spite of several methodological issues, antidepressants can be divided into low- and high-risk categories with regard to the possibility of developing SD. In patients interested in sexual activity, it is recommended to start with low-risk antidepressants. Otherwise, encourage the patient to wait for tolerance and then switch to low-risk. In selected cases, dose reduction or a drug holiday may be applied. The adjunctive use of a PDE5i can help in a significant number of patients. Randomized controlled trials are needed to set high-level evidence-based recommendations.


Asunto(s)
Antidepresivos , Disfunciones Sexuales Fisiológicas , Antidepresivos/efectos adversos , Humanos , Masculino , Preparaciones Farmacéuticas , Psicoterapia , Disfunciones Sexuales Fisiológicas/inducido químicamente , Disfunciones Sexuales Fisiológicas/tratamiento farmacológico
4.
Curr Org Synth ; 2022 Jan 04.
Artículo en Inglés | MEDLINE | ID: mdl-34983349

RESUMEN

BACKGROUND: A series of new pyrimidines and thiazoles containing camphor moiety were synthesized under both conventional and microwave irradiation techniques. METHODS: The condensation of camphor either with aminoguanidine or thiosemicarbazide gives the camphor hydrazine carboximidiamide 2 and the camphor thiosemicarbazone 3, respectively. Refluxing of 3 with chloroacetonitrile afforded the camphor thiazol-4-imine 4. Compounds 2 and 4 were used as precursors for the synthesis of target products. RESULTS: The reaction of 2 with different species such as arylidene malononitrile, acetylacetone, and ethyl acetoacetate gave the corresponding camphor pyrimidine derivatives 5a,b-7 while refluxing of compound 4 with different reagents e.g. aldehydes, isatin, ninhydrin, acetic anhydride, benzene sulphonyl chloride, and p-nitro-benzoyl chloride afforded the camphor thiazole derivatives 8a-d-13, respectively. CONCLUSION: A comparison between the conventional way and the eco-friendly microwave irradiation method occurred in the synthesis of the same compounds, which the latter was more efficient. The elemental analysis, FT-IR, 1H NMR, 13C NMR, and Mass spectra confirm the structures of the obtained new compounds. The potential use of some selected derivatives as antimicrobial agents was investigated and gave promising results.

5.
Int J Impot Res ; 34(2): 145-151, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34992226

RESUMEN

COVID-19 pandemic is associated with devastating effects on social, psychological, and economical aspects of survivors. We assume that erectile function (EF) is affected as well. We performed a systematic review of the published articles about the change in EF among patients and health care providers during the COVID-19 pandemic. We searched PubMed and Cochrane databases for English literature using a combination of medical subject headings (MeSH) terms and keywords. We extracted data of erectile dysfunction (ED) rate, international index of erectile function (IIEF), changes related to exposure to the pandemic (Primary objectives), and factors affecting these differences (Secondary objectives). Twenty articles were included in the screening phase. Only 3 articles were eligible for primary objectives, and 2 articles were included for the secondary objective. Three articles revealed an increase in ED cases and a reduction in IIEF-5 scores during the pandemic. Rates of ED have ranged from 32% to 87% of the study populations. Anxiety, depression, and post-traumatic stress disorder (PTSD) were associated with increased ED rates. We conclude that the COVID-19 pandemic is associated with increased rates of ED. Anxiety and depression augment this increase. Health care providers are at higher risk for PTSD, which increases the risk of ED.


Asunto(s)
COVID-19 , Disfunción Eréctil , COVID-19/epidemiología , Disfunción Eréctil/diagnóstico , Disfunción Eréctil/epidemiología , Disfunción Eréctil/etiología , Personal de Salud , Humanos , Masculino , Pandemias , Erección Peniana
6.
J Sex Med ; 18(10): 1705-1714, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34511369

RESUMEN

BACKGROUND: Peyronie's disease (PD) is associated with penile pain, deviation, and sexual dysfunction. Up till now, there is no conservative standard treatment for PD. However, the role of Extracorporeal Shock Wave Therapy (ESWT) is gaining increasing interest. AIM: To evaluate the effect of ESWT on penile deviation, plaque size, erectile function, pain scale, and the rate of complications in PD patients. METHODS: PubMed database was searched for articles published from January 2000 to November 2020, using related keywords and including randomized controlled trials (RCTs) only. Meta-analysis and forest plots were carried out using RevMan, and outcomes were reviewed by 2 authors independently. PRISMA guidelines were used in this article to achieve the quantitative and qualitative synthesis of data. OUTCOMES: Changes in penile deviation, plaque size, erectile function, pain scale, and the rate of ESWT related complications. RESULTS: The search yielded 73 articles. Three RCTs, including 117 patients in the ESWT group and 121 patients in the placebo group, were reviewed. ESWT is associated with reduction in plaque size (OR = 2.59, 95% CI (1.15-5.85), P= .02). No significant difference in reduction of penile deviation angle or rate of bruises were detected in post ESWT group when compared to placebo. No evidence was found to show an effect of ESWT on erectile function or pain scale. CLINICAL IMPLICATIONS: Based on the available RCTs, ESWT fails to improve penile curvature or pain in men with PD.  Although ESWT may reduce plaque size, this remains of questionable clinical significance. STRENGTHS & LIMITATIONS: RCTs used different metrics to report the same outcome. Missed data were imputed to match the requirements of meta-analysis. However, there is still much data that cannot be estimated. CONCLUSION: The current data suggest that ESWT fails to improve penile curvature or pain in men with PD.  Although ESWT may reduce plaque size, this remains of questionable clinical significance, and further studies are required to confirm findings. Bakr AM, El-Sakka A. Extracorporeal Shockwave Therapy in Peyronie's Disease: Systematic Review and Meta-Analysis. J Sex Med 2021;18:1705-1714.


Asunto(s)
Tratamiento con Ondas de Choque Extracorpóreas , Litotricia , Induración Peniana , Humanos , Masculino , Dolor Pélvico , Erección Peniana , Induración Peniana/terapia , Resultado del Tratamiento
7.
Expert Opin Pharmacother ; 22(7): 821-834, 2021 May.
Artículo en Inglés | MEDLINE | ID: mdl-33275043

RESUMEN

Introduction: The effectiveness of phosphodiesterase type 5 inhibitors (PDE5i) in treating erectile dysfunction (ED) creates a new field of both medical practice and pharmaceutical manufacturing. Both paved the way for emerging minimally invasive therapies to restore male sexual function. However, what is the best drug to achieve the optimum outcome is still a challenging question to be answered.Areas covered: The general viewpoint of matching the pharmacotherapeutic characteristics with the patient's medical, social, and psychological variables, in order to balance between efficacy and safety. Several studies had investigated considerations for preference and long-term adherence for PDE5i. However, a thorough investigation of considerations for prescribing ED pharmacotherapy is still lacking in the literature. This is the aim of this manuscript.Expert opinion: Several issues should be considered in the planning of ED management such as the patient's and partner's expectations, etiologic considerations, performance status, safety, adverse effects, ease of administration, compliance, bad experiences with previous treatment, availability, cost, social factors, satisfaction, and finally, regimen considerations. Addressing the patient's and partner's individual needs help to tailoring treatment in order to minimize compromises and optimize gains.


Asunto(s)
Disfunción Eréctil , Protocolos Clínicos , Disfunción Eréctil/tratamiento farmacológico , Humanos , Masculino , Inhibidores de Fosfodiesterasa 5/uso terapéutico
8.
RSC Adv ; 9(23): 13145-13152, 2019 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-35520793

RESUMEN

In this paper, we present promising results in the green electrochemical oxidation of catechol in the presence of three different thiol nucleophiles at the surface of a glassy carbon electrode in an aqueous solution using cyclic voltammetry (CV). The outcome indicated the synthesis of some new heterocyclic compounds functionalized with phenolic, triazole, triazine and pyrimidine groups. The effects of repetitive cycling, nucleophile concentrations and sweep rates were explored to get more information about the systems. The voltammetric data showed that the electro-generated o-benzoquinone is a quite reactive intermediate, which in aqueous solutions can quickly participate in a Michael-addition reaction with any one of the nucleophiles to form the corresponding products. The structures of all newly electro-synthesized compounds were confirmed by elemental analyses and FT-IR, 1H NMR, 13C-NMR and MS spectra. The one-pot synthesis strategy led to new organics with high purities and good yields under green conditions without harmful reagents.

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