Pharmacologic properties and inhibitory activity of 6-azasteroids against Mycobacterium leprae in vivo and in vitro [PDF]
Microbiology SpectrumAlthough the current multidrug therapy (MDT) for leprosy is very successful, the long treatment duration and the emergence of antibiotic-resistant strains demand for new alternative drugs.
Ramanuj Lahiri +2 more
exaly +5 more sources
Fluorescent Azasteroids through Ultrasound Assisted Cycloaddition Reactions [PDF]
Molecules, 2021 We report here the synthesis and optical spectral properties of several new azasteroid derivatives. The formation of these compounds was explained based on the most probable mechanism.
Costel Moldoveanu +2 more
doaj +3 more sources
A Chemoproteomic Approach to Elucidate the Mechanism of Action of 6-Azasteroids with Unique Activity in Mycobacteria. [PDF]
ACS Infect Dis, 2023 By illuminating key 6-azasteroid–protein interactions in both Mycobacterium tuberculosis (Mtb) and the closely related model organism Mycobacterium marinum (Mm), we sought to improve the antimycobacterial potency of 6-azasteroids and further our ...
Werman JM +4 more
europepmc +2 more sources
Novel 4-Azapregnene Derivatives as Potential Anticancer Agents: Synthesis, Antiproliferative Activity and Molecular Docking Studies [PDF]
Molecules, 2022 A series of novel 21E-arylidene-4-azapregn-5-ene steroids has been successfully designed, synthesized and structurally characterized, and their antiproliferative activity was evaluated in four different cell lines.
Vanessa Brito +4 more
doaj +2 more sources
Inhibition of Phytosterol Biosynthesis by Azasterols [PDF]
Molecules, 2020 Inhibitors of enzymes in essential cellular pathways are potent probes to decipher intricate physiological functions of biomolecules. The analysis of Arabidopsis thaliana sterol profiles upon treatment with a series of azasterols reveals a specific in ...
Sylvain Darnet +5 more
doaj +2 more sources
Inhibition of the M. tuberculosis 3β-hydroxysteroid dehydrogenase by azasteroids. [PDF]
Bioorg Med Chem Lett, 2011 The cholesterol metabolism pathway in Mycobacterium tuberculosis (M. tb) is a potential source of energy as well as secondary metabolite production that is important for survival of M. tb in the host macrophage.
Thomas ST, Yang X, Sampson NS.
europepmc +2 more sources
19-nor-10-azasteroids, a new class of steroid 5 alpha-reductase inhibitors. 2. X-ray structure, molecular modeling, conformational analysis of 19-nor-10-azasteroids and comparison with 4-azasteroids and 6-azasteroids. [PDF]
Journal of Medicinal Chemistry, 1997 19-Nor-10-azasteroids are a new class of 5 alpha-reductase inhibitors whose activity depends on the presence of the bridgehead N-10 atom conjugated with the 4-en-3-one moiety in the A ring. The X-ray structure of 19-nor-10-azasteroid 1 has been determined and it is compared with the X-ray structure of testosterone. A complete conformational analysis of
A. Guarna +6 more
semanticscholar +5 more sources
5-alpha-reductase type I (SRD5A1) is up-regulated in non-small cell lung cancer but does not impact proliferation, cell cycle distribution or apoptosis [PDF]
Cancer Cell International, 2012 Background Non-small cell lung cancer (NSCLC) is one of the most frequent malignancies and has a high mortality rate due to late detection and lack of efficient treatments.
Kapp Friedrich G +4 more
doaj +2 more sources
Synthesis of 6-azaprogesterone and 19-hydroxy-6-azasteroids
Steroids, 2013 19-Hydroxy-6-azapregnanes were obtained from pregnenolone via a 7-azido-5-oxo-6-nor-5,7-secopregnane intermediate. The 6-azapregnane core was built in good yield in a straightforward way from the secosteroid, by means of a Staudinger (aza-Wittig ...
Pablo Hector Di Chenna +2 more
exaly +2 more sources
Total Synthesis of 8-Azasteroids
Russian Chemical Reviews, 1984 Studies on the total synthesis of 8-azasteroids from the start of investigations in this field (1963) up to 1983 are examined. Earlier studies on the synthesis of compounds formally containing the 8-azasteroid skeleton and those on the synthesis of 8 ...
F. Lakhvich, L. Lis, A. A. Akhrem
semanticscholar +2 more sources