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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Paliperidone is the active metabolite of risperidone. Four metabolic pathways have been identified in vivo, none of which accounted for more than 6.5% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Following administration of [14C]-paliperidone, 59% of the dose was excreted unchanged into urine, indicating that paliperidone is not extensively metabolised in the liver. Approximately 80% of the administered radioactivity was recovered in urine and 11% in the faeces.
The pharmacotherapeutic management of pulmonary tuberculosis: an update of the state-of-the-art
Published in Expert Opinion on Pharmacotherapy, 2022
Ginenus Fekadu, Dilys Yan-wing Chow, Joyce H.S. You
To combat the emerging of multi-drug resistance in TB, it is essential to continue the development of anti-TB agents with various mechanisms of action in near future. The upstream research and development of novel anti-TB entities are increasing and a number of promising compounds are in the pipeline. Benzisoxazole-containing compounds, sulfur-based moieties, chlorine-containing heterocyclic compounds, and oxadiazole-based derivatives, in particular, are potential candidates to be further developed into drug entities with potent anti-TB activities in the future [77–80]. Apart from novel drug development, different combinations of novel and repurposed drugs also need to be explored to obtain shorter or better tolerated regimens. Alongside the ongoing development of novel treatment combinations, development and access of technology for rapid detection of TB cases and drug resistance are also much needed in regions with high TB burden. More importantly, proper health economic evaluations of the new and conventional regimens are highly warranted to enable public health policy makers to make informed decisions on the cost-effective implementation of TB management programmes.
Multi-targeted drug design strategies for the treatment of schizophrenia
Published in Expert Opinion on Drug Discovery, 2021
Piotr Stępnicki, Magda Kondej, Oliwia Koszła, Justyna Żuk, Agnieszka A. Kaczor
Chen et al. reported new amide analogues of benzisoxazole as multi-functional antipsychotics. The effect of substitution with chlorine, nitro and amino groups at the 6-position of benzo[d]isothiazole on receptor affinity was also examined. Nitro and amino groups decreased the affinity for D3, D2, 5-HT2A, and 5-HT1A receptors. However, chlorine substitution increased dopamine D3 receptor affinity, and reduced affinity for the serotonin 5-HT1A receptor. Among a number of synthesized compounds, the best compound (17) (Figure 3) showed high affinity for dopamine D2, D3 (Ki = 2.9; 0.13) and serotonin 5-HT1A, 5-HT2A (Ki = 1.3; 0.23) receptors and low affinity for H1 receptors and hERG channels. Moreover, behavioral studies showed that this compound may be used to treat schizophrenia without inducing catalepsy [107].
In silico docking studies and synthesis of new phosphoramidate derivatives of 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole as potential antimicrobial agents
Published in Journal of Receptors and Signal Transduction, 2020
Munichandra Reddy Sivala, Venkataramaiah Chintha, Krishna Murthy Potla, Sampath Chinnam, Naga Raju Chamarthi
Antimicrobial resistance of pathogenic bacteria and fungi as antibiotic drugs for the effective prevention and treatment of an ever-increasing range of infections. There is a necessity to design and develop new antimicrobial agents for the remedy of infectious diseases. Nitrogen containing heterocycles with an oxygen atom are considered as a significant class of compounds in medicinal chemistry owing to broad biological applications [1]. Specifically, benzisoxazole derivatives are extensively used in the production of dyes, synthetic chemistry, etc. Benzisoxazole scaffolds and its analogs have been found to possess a wide range of pharmacological activities such as anti-HIV [2], anti-psychotic [3–5], anti-cancer [6,7], anti-inflammatory [8,9], anti-thrombotic [10], analgesic [11], dopamine and serotonin receptor [12], acetylcholinesterase [13], anti-diabetic [14–16], and antimicrobial agents [17].