The biological targets of acivicin inspired 3-chloro- and 3-bromodihydroisoxazole scaffolds.
نویسندگان
چکیده
Target analysis of acivicin derived 3-halodihydroisoxazoles scaffolds in living non-pathogenic and pathogenic bacteria.
منابع مشابه
Synthesis and in vitro/in vivo Evaluation of the Antitrypanosomal Activity of 3-Bromoacivicin, a Potent CTP Synthetase Inhibitor
The first convenient synthesis of enantiomerically pure (αS,5S)-α-amino-3-bromo-4,5-dihydroisoxazol-5-yl acetic acid (3-bromoacivicin) is described. We demonstrate that 3-bromoacivicin is a CTP synthetase inhibitor three times as potent as its 3-chloro analogue, the natural antibiotic acivicin. Because CTP synthetase was suggested to be a potential drug target in African trypanosomes, the in vi...
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Studies of acivicin [(alpha S,5S)-alpha-amino-3-chloro-2-isoxazoline-5-acetic acid, AT-125] plasma levels in ICR, B6D2F1 and CD2F1 mice after single dose i.p. administration showed that total body clearance of drug by male mice was ca. twice the clearance by females of the same strain. Clearance was also greater in older (22-25 g) than in younger (15-18 g) ICR mice. Testosterone pretreatment in...
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Previously we showed that starvation of HL-60 promyelocytic leukemia cells for a single essential amino acid induced irreversible differentiation into more mature monocyte-like cells. Although not an essential amino acid, glutamine is important in the growth of normal and neoplastic cells. The glutamine analogue, alpha S,5S-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid (acivicin) inhi...
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A Phase I trial of acivicin [L-(alpha S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid] has been performed on an escalating-dosage 24-hr continuous i.v. infusion schedule. Thirty-one patients received 77 courses of treatment, and all but one were evaluable for toxicity. Pharmacological monitoring in selected patients demonstrated that peak plasma levels correlated with dose. Postin...
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Tissue-engineering scaffolds provide biological and mechanical frameworks for cell adhesion, growth, and differentiation. Nanofibrous scaffolds mimic the native extracellular matrix (ECM) and play a significant role in formation and remodeling of tissues and/or organs . One way to mimic the desired properties of fibrous ECM is adding nanoparticles into the polymer matrix. In the current study, ...
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عنوان ژورنال:
- Chemical communications
دوره 46 44 شماره
صفحات -
تاریخ انتشار 2010