Abstract:
:Synthesis and biological activity of 17-esters of 6-dehydro-16-methylene-17 alpha-hydroxyprogesterone are presented. A systematic study of the influence of the alteration of halogen at 6 and the acyl group at 17 on the progestational and antiandrogenic activities of the resulting structures is described. A convenient general method for synthesis of all of the members of the generic family from the precursors in common is described. It is believed that 6-chloro-16-methylene-17 alpha-hydroxy-4,6-pregnadiene 17-acetate, because of its structural similarity to chlormadinone acetate and its high progestational potency, will perform as a contraceptive at perhaps a lower dose than that of chlormadinone acetate.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Shapiro EL,Weber L,Harris H,Miskowicz C,Neri R,Herzog HLdoi
10.1021/jm00277a006subject
Has Abstractpub_date
1972-07-01 00:00:00pages
716-20issue
7eissn
0022-2623issn
1520-4804journal_volume
15pub_type
杂志文章abstract::A series of S-alkylated derivatives of 5-mercapto-2'-deoxyuridine have been prepared by alkylation of the preformed nucleoside. Two of these compounds, the S-propargyl and S-allyl derivatives, have shown significant antiviral activity against Herpes simplex type 1 in HeLa TK- cells but appear to be less effective in t...
journal_title:Journal of medicinal chemistry
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journal_title:Journal of medicinal chemistry
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更新日期:2016-05-26 00:00:00
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更新日期:2017-11-09 00:00:00
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更新日期:2008-03-27 00:00:00
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journal_title:Journal of medicinal chemistry
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更新日期:2008-12-25 00:00:00
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journal_title:Journal of medicinal chemistry
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更新日期:2007-01-25 00:00:00
abstract::A series of α-ketooxazoles containing conformational constraints in the C2 acyl side chain of 2 (OL-135) were examined as inhibitors of fatty acid amide hydrolase (FAAH). Only one of the two possible enantiomers displayed potent FAAH inhibition (S vs R enantiomer), and their potency is comparable or improved relative ...
journal_title:Journal of medicinal chemistry
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更新日期:2016-12-22 00:00:00
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journal_title:Journal of medicinal chemistry
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doi:10.1021/jm00175a007
更新日期:1980-01-01 00:00:00
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更新日期:2008-05-22 00:00:00
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abstract::Retinoic acid receptor-related orphan receptor γt (RORγt) is a nuclear receptor associated with the pathogenesis of autoimmune diseases. Allosteric inhibition of RORγt is conceptually new, unique for this specific nuclear receptor, and offers advantages over traditional orthosteric inhibition. Here, we report a highly...
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更新日期:2013-09-26 00:00:00
abstract::Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1,2-dione inhibitors are decidedly hydrophobic, a modified dione scaffold was designed and elaborated into a >3...
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更新日期:2010-12-23 00:00:00
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journal_title:Journal of medicinal chemistry
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abstract::Quantitative structure-activity relationships (QSAR) of a series of 6-anilinouracil derivatives were developed for their inhibitory activity against the wild-type DNA polymerase III (pol III) and a mutant enzyme, pol III/azp-12, derived from Bacillus subtilis. Interaction between inhibitors and both enzymes appears to...
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journal_title:Journal of medicinal chemistry
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