An anti-1-adrenoceptor medication called prazosin is used to treat high blood pressure (hypertension). Newer Prazosin analogues were produced in the current investigation employing a bioisosteric method. 190 bioisosteres were produced as a result of substituting the aminoqunazoline group in the prazosin using MolOpt, a web service for in silico drug creation. Utilizing ADMETlab 2.0, pharmacokinetic (absorption, distribution, metabolism, and excretion) and toxicity properties were determined. Results show that the analogues 046 (Hexahydrofuro[3,2-b]furan), 182 (1,3-Oxazolidine), and 187 (Pyrido[3,4-b]Pyrazine)] have lower levels of the human ether-à-go-go-related gene (hERG) (less cardiotoxic), lower levels of human hepatotoxicity (H-HT), and lower levels of drug-induced liver injury (DILI), The computation of drug-likeness and drug score resulted in a quantitative estimate of drug-likeness (QED) value of 0.67. Other analogues were also more potent and less dangerous than the original medication. New 1-adrenoceptor antagonists for the treatment of hypertension will be created as a result of this investigation.
Author(s) Details:
Sunil Sahu,
Department of Pharmacy, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (CG)-495009, India.
Sanmati K. Jain,
Department of Pharmacy, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (CG)-495009, India.
Please see the link here: https://stm.bookpi.org/CAPR-V7/article/view/8365
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