Affiliation:
1. Department of Pharmacy, School of Chemical Sciences and Pharmacy,
Central University of Rajasthan, Bandarsindri, Ajmer, India
Abstract
Background:
Amphotericin B is a gold-standard drug, particularly for the treatment of
systemic fungal infections. However, its low solubility and permeability limit its application. To
improve its bioavailability, AmB may be conjugated with various water-soluble auxiliary groups.
Methods:
Custom R group Enumeration was used at the designated sites of Amphotericin B. The
designated sites taken into consideration are the carboxyl moiety of the aglycone part and the
amine moiety of the glycone part of Amphotericin B for Enumeration purposes. The enumerated
molecules were subjected to QikProp properties.
Results:
We identified fourteen hits with improved predicted aqueous solubility and cell permeability.
Conclusion:
Enumeration might be applicable in improving bioavailability, which could lead to
the oral formulation of the Amphotericin B drug.
Funder
Department of Science and Technology-BRICs
Department of Higher Education, Bhopal, M.P., India
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Molecular Medicine,General Medicine
Cited by
1 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献