Diurnal variation in salivary progesterone in fertile Indian women

Patil, Suvarna; Patil, Netaji; Bhat, Rohit; Hardikar-Bhat, Pallavi; Jadhav, Dnyaneshwar; Dervankar, Omkar; Joglekar, Charudatta; Desai, Shradha; Chavan, Dhanashree; Pise, Megha; Nandoskar, Ajit

doi:10.1016/j.heliyon.2022.e12719

Cited by 3 publications

(2 citation statements)

References 31 publications

(39 reference statements)

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“…The pyrimidine ring, resembling both pyridine and benzene chemically, displays an irregular hexagonal structure with aromatic properties akin to benzene, while also exhibiting electron‐deficient characteristics similar to pyridine. A wide range of natural and synthetic pyrimidines have been discovered, exhibiting a variety of pharmacological activities including antioxidant, antibacterial, antiviral, antifungal, antituberculosis, and anti‐inflammatory properties [145–154] …”

Section: Pyrimidinesmentioning

confidence: 99%

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

Li,

Gu,

Nong

et al. 2023

The Chemical Record

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Cancer stands as a serious malady, posing substantial risks to human well‐being and survival. This underscores the paramount necessity to explore and investigate novel antitumor medications. Nitrogen‐containing compounds, especially those derived from natural sources, form a highly significant category of antitumor agents. Among these, antitumor agents with six‐membered aromatic nitrogen heterocycles have consistently attracted the attention of chemists and pharmacologists. Accordingly, we present a comprehensive summary of synthetic strategies and clinical implications of these compounds in this review. This entails an in‐depth analysis of synthesis pathways for pyridine, quinoline, pyrimidine, and quinazoline. Additionally, we explore the historical progression, targets, mechanisms of action, and clinical effectiveness of small molecule inhibitors possessing these structural features.

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Section: Pyrimidinesmentioning

confidence: 99%

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

Li,

Gu,

Nong

et al. 2023

The Chemical Record

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“…The pyran moiety is the core component of many pharmacological agents that have a broad spectrum of biological properties [1–6] . The pyrimidine ring is part of numerous biological compounds showing diverse medicinal properties; [7–9] they also serve as potential inhibitors of kinase activity [10] . Additionally, the pyrazole ring is integral to numerous bioactive species exhibiting activities like antibacterial, [11] anti‐malarial, [12] anti‐viral, [13] anti‐oxidant, [14] anti‐inflammatory, [15] and anticancer agents [16] .…”

Section: Introductionmentioning

confidence: 99%

Facile Synthesis of Pyrazolopyranopyrimidines by Synergism of Ultrasound Irradiation and Biocompatible Inulin Biopolymer as Catalyst

Jain,

Jain

2024

ChemistrySelect

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Inulin, a natural polysaccharide has been utilized as a novel biodegradable, efficient, and environmentally benign catalyst for the ultrasound‐assisted one‐pot, single‐step multicomponent formation of a library of pyrazolopyrano[2,3‐d]pyrimidine‐diones 5(a‐k) from the reaction of ethyl acetoacetate, hydrazine hydrate, aromatic aldehydes, and barbituric/ thiobarbituric acid in aqueous ethanol (1 : 1) at 50 °C. This facile methodology offers a metal‐free, sustainable, selective synthesis of pyrazolopyrano[2,3‐d]pyrimidine‐diones with no by‐product having excellent product yield (≥90 %) in a shorter reaction time. Additionally, the biocompatible inulin is recyclable for up to five consecutive runs without much decrease in its catalytic potential. Inulin has been characterized by spectral techniques such as XRD, FTIR, Raman, and SEM. It shows remarkable stability in the reaction medium as evident from the zeta potential value of −21.39 mV and hydrodynamic diameter of 459.5 nm. Novel pyrazolopyrano[2,3‐d]pyrimidine‐diones (5g, 5h, 5j, and 5k) were also synthesized using this protocol and the synthesized compounds were examined for their antimicrobial activity.

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Replicating clinical placebo effects in computational trials: Bridging the gap between in silico and clinical studies

Dominguez-Gomez,

Butakoff,

Rast

et al. 2024

Preprint

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This study replicates human cardiac safety clinical trials using computational models, which include diurnal hormonal placebo effects, aiming to create fast and efficient drug screening tools to assess QT interval prolongation preclinically. A virtual cardiac population that simulates sex-specific electrophysiological variability influenced by diurnal hormonal cycles was created to closely mirror human physiology. The goal is to assess the impact of these hormone dynamics on placebo-induced responses and evaluate the virtual population's accuracy in reflecting clinical trial outcomes. The study showed that the virtual population model successfully replicated about 50% of the observed QT variability seen in placebo groups. The computational framework facilitated direct comparison with human clinical trials, achieving critical concentrations, i.e., concentrations that cause a mean QTc effect of 10 ms, within a 0.6-fold range of clinical results. Additionally, the exposure-response slopes exhibited relative errors averaging 43%, which translates into mean absolute errors of 6-7 ms in comparison to clinical data. These results highlight its potential to reproduce human physiology and provide results consistent with real-world human clinical trials. Additionally, a comparison with a previously published statistical placebo model further supports this approach. By approximating the diurnal hormonal variations, as a component of the mechanistic basis of placebo, this method offers a robust decision-making tool for early-stage drug safety assessment.

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Diurnal variation in salivary progesterone in fertile Indian women

Cited by 3 publications

References 31 publications

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

Facile Synthesis of Pyrazolopyranopyrimidines by Synergism of Ultrasound Irradiation and Biocompatible Inulin Biopolymer as Catalyst

Replicating clinical placebo effects in computational trials: Bridging the gap between in silico and clinical studies

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