Purpose: Clinical trials are advancing the treatment of polycystic ovary syndrome (PCOS), an endocrine disorder affecting 8-13% of women. Lifestyle interventions, including nutritional plans, physical activity, and stress management, can improve reproductive hormones and metabolic health. Novel pharmacotherapies targeting hormonal, metabolic, and reproductive abnormalities are being explored for individualized treatment.
View Article and Find Full Text PDFNew Biginelli adducts were rationalised, the introduction of selected anti-tubercular (TB) pharmacophores into the dihydropyrimidine (DHPM) ring of deoxythymidine monophosphate (dTMP), the natural substrate of thymidine monophosphate kinase (TMPK). Repurposing was one of the design rationale strategies for some selected mimics of the designed compounds. The anti-TB activity was screened against the M HRv strain where was superior to ethambutol (EMB), and was 9-fold more potent than pyrazinamide (PZA).
View Article and Find Full Text PDFAging is an inevitable biological process that significantly impacts human health, leading to a decline in cellular function and an increase in cellular damage. This study elucidates the burgeoning potential of antiaging pharmaceuticals in mitigating the thriving burden of chronic conditions linked to advancing age. It underscores the pivotal role of these pharmacotherapeutic agents in fostering longevity free from debilitating age-related afflictions, notably cardiovascular disorders, neoplastic processes, and neurodegenerative pathologies.
View Article and Find Full Text PDFA simple and effective three-component one-pot green methodology was employed for the synthesis of a new thiazolidine-2,4-dione based bisspirooxindolo-pyrrolidine derivatives using [Bmim]BF ionic liquid via [3 + 2] cycloaddition reaction. It is an environmentally benign, column chromatography-free, shorter reaction time, good yield and easy product isolation method. The synthesized compounds 10a-x, were thoroughly characterized by using various spectroscopic methods like FT-IR, H NMR, C NMR, Mass spectrometry and finally by single crystal X-ray diffraction method.
View Article and Find Full Text PDFIn a quest to discover new antimalarial and antitubercular drugs, we have designed and synthesized a series of novel triazole-quinazolinone hybrids. The in vitro screening of the triazole-quinazolinone hybrid entities against the plasmodium species P. falciparum offered potent antimalarial molecules 6c, 6d, 6f, 6g, 6j & 6k owing comparable activity to the reference drugs.
View Article and Find Full Text PDFAims And Objectives: The purpose of this study was to systematically review studies related to the use of online Team Based Learning (TBL) platforms with a focus on health professional education. The objectives were to identify best practices, highlight what technological platforms are effective for TBL processes and evaluate educational outcomes in terms of student experience, learning and preference.
Design: A systematic review of published TBL research was undertaken between August and October 2021 and supplemented in September 2022.
Mycobacteria regulate the synthesis of mycolic acid through the fatty acid synthase system type 1 (FAS I) and the fatty acid synthase system type-2 (FAS-II). Because mammalian cells exclusively utilize the FAS-I enzyme system for fatty acid production, targeting the FAS-II enzyme system could serve as a specific approach for developing selective antimycobacterial drugs. Enoyl-acyl carrier protein reductase enzyme (InhA), part of the FAS-II enzyme system, contains the NADH cofactor in its active site and reduces the intermediate.
View Article and Find Full Text PDFThe rational design of novel thiazolo[2,3-][1,2,4]triazole derivatives was carried out based on previously identified antitubercular hit molecule H127 for discovering potent compounds showing antimicrobial activity. The designed compounds were screened for their binding efficacies against the antibacterial drug target enoyl-[acyl-carrier-protein] reductase, followed by prediction of drug-likeness and ADME properties. The designed analogues were chemically synthesized, characterized by spectroscopic techniques, followed by evaluation of antimicrobial activity against bacterial and fungal strains, as well as antitubercular activity against and strains.
View Article and Find Full Text PDFObjectives: Current mental health practices for people living in residential aged care (RAC) facilities are poor. In Australia, there are no mechanisms to monitor and promote mental health for people living in RAC, including those who experience changed behaviours and psychological symptoms. The aim of this study is to improve current practices and mental health outcomes for people living in RAC facilities by codesigning a Mental Health benchmarking Industry Tool for residential aged Care (MHICare Tool).
View Article and Find Full Text PDFSeveral facets of the host response to tuberculosis have been tapped for clinical investigation, especially targeting angiogenesis mediated by VEGF signaling from infected macrophages. Herein, we rationalized combining the antiangiogenic effects of VEGFR-2 blockade with direct antitubercular InhA inhibition in single hybrid dual inhibitors as advantageous alternatives to the multidrug regimens. Inspired by expanded triclosans, the ether ligation of triclosan was replaced by rationalized linkers to assemble the VEGFR-2 inhibitors thematic scaffold.
View Article and Find Full Text PDFAn innovative series of N-substituted piperazine-linked imidazothiazole derivatives 7(a-x) were synthesized, and their antitubercular effectiveness was evaluated. A three-step reaction sequence involving the condensation of 1,3-dichloroacetone and thiourea, coupling with substituted piperazines to give the intermediates 5(a-d) and cyclization with substituted α-bromoacetophenones produced the desired imidazothiazole derivatives 7(a-x) in excellent yields. In vitro screening of new derivatives against Mycobacterium tuberculosis H37Rv resulted in 7k (minimum inhibitory concentration [MIC]: 0.
View Article and Find Full Text PDFThe development of anti-tuberculosis (anti-TB) drugs has become a challenging task in medicinal chemistry. This is because Mycobacterium tuberculosis (TB), the pathogen that causes tuberculosis, has an increasing number of drug-resistant strains, and existing medication therapies are not very effective. This resistance significantly demands new anti-TB drug profiles.
View Article and Find Full Text PDFSerotogenic toxicity is a major hurdle associated with Linezolid in the treatment of drug-resistant tuberculosis (TB) due to the inhibition of monoamine oxidase (MAO) enzymes. Azole compounds demonstrate structural similarities to the recognized anti-TB drug Linezolid, making them intriguing candidates for repurposing. Therefore, we have repurposed azoles (Posaconazole, Itraconazole, Miconazole, and Clotrimazole) for the treatment of drug-resistant TB with the anticipation of their selectivity in sparing the MAO enzyme.
View Article and Find Full Text PDFA new series inspired by combining fragments from nitazoxanide (NTZ) and 4-aminosalicylic acid (4-ASA) was synthesized and screened for antibacterial and antimycobacterial activities. The majority showed higher antibacterial potency than NTZ against all the screened strains, notably, 5f, 5j, 5n and 5o with MICs of 0.87-9.
View Article and Find Full Text PDFIn the present study, we have reported the synthesis of novel isoniazid-triazole derivatives (), the click chemistry approach. The synthesized isoniazid-triazole derivatives have potent antitubercular activity against the (MTB) H37Rv strain. Among these compounds, , , , , , , , , and were found to be the most active ones with a MIC value of 0.
View Article and Find Full Text PDFAntimicrobial resistance (AMR) is a global health threat, progressively emerging as a significant public health issue. Therefore, an antibiotic susceptibility study is a powerful method for combating antimicrobial resistance. Antibiotic susceptibility study collectively helps in evaluating both genotypic and phenotypic resistance.
View Article and Find Full Text PDFA library of 1, 2, 3-triazole incorporated thiazolylcarboxylate derivatives (7a-q) and (8a-j) were synthesized and evaluated for their in-vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The two compounds 7h and 8h have displayed excellent antitubercular activity with MIC values of 3.12 and 1.
View Article and Find Full Text PDFTetrazole-based easily synthesizable fluorogenic probes have been developed that can form self-assembled nanostructures in the aqueous medium. Though the compounds could achieve detection of cyanide ions in apolar solvents, such as, THF, significant interference was observed from other basic anions, such as F, AcO, HPO, etc. On the other hand, a highly specific response was observed for CN ions in the aqueous medium.
View Article and Find Full Text PDFInfusion of fluids and medications is traditionally performed intravenously. However, venous depletion in patients has led to the quest for vessel health preservation. A safe, effective, acceptable, and efficient alternative is the subcutaneous route.
View Article and Find Full Text PDFIn pursuit of new antitubercular agents, we here report the antimycobacterial (HRv) and DNA gyrase inhibitory potential of daidzein and khellin natural products (NPs). We procured a total of 16 NPs based on their pharmacophoric similarities with known antimycobacterial compounds. The HRv strain of was found to be susceptible to only two out of the 16 NPs procured; specifically, daidzein and khellin each exhibited an MIC of 25 μg/mL.
View Article and Find Full Text PDFSodium-glucose transport protein 2 (SGLT-2) inhibitors are approved antidiabetic drugs with a beneficial effect on reducing major adverse cardiac events and heart failure hospitalization. Among them, canagliflozin has the least selectivity toward SGLT-2 over the SGLT-1 isoform. Canagliflozin can inhibit SGLT-1 at therapeutic levels; however, the underlying molecular mechanism is not understood.
View Article and Find Full Text PDFKey Points: Health professionals resisted practice change in environments of low infection where the perception of a need to change is small. Standardizing care of central venous catheters for hemodialysis requires breaking down silos of practice to benefit all patients. Knowledge of and adherence to guidelines, formal change management, and ongoing facilitation are required to implement standardized care.
View Article and Find Full Text PDF