Abstract：
:Ergosterol, the predominant sterol of fungi, is postulated to have many cellular functions which include a bulk membrane role and a regulatory role. Studies with sterol auxotrophs show that, even in the presence of sterols which can fulfill the bulk membrane requirements, a small concentration of ergosterol is absolutely necessary for growth. The delta 5-double bond appears to be required for the regulatory role of ergosterol; therefore, development of inhibitors of the enzyme that introduce this double bond, delta 7-sterol 5-desaturase (5-desaturase), may lead to effective antifungal agents. Within is the first reported synthesis of inhibitors of fungal 5-desaturase and the development of an in vitro tritium efficacy radioassay. The inhibitors were of the general structure 7,22(E)-ergostadien-3 beta-ol with alpha-face heteroatom substituents in the vicinity of C-5. They exhibited IC50 values of 47-149 microM.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Goldstein AS,Frye LLdoi
10.1021/jm9605851subject
Has Abstractpub_date
1996-12-20 00:00:00pages
5092-9issue
26eissn
0022-2623issn
1520-4804pii
jm9605851journal_volume
39pub_type
杂志文章abstract：:Glucuronidation and transporter-mediated efflux into bile are important in the elimination of xeno- and endobiotics, including the natural biladienone pigment bilirubin. The mechanisms of these processes and the structural factors that dictate whether cholephilic compounds are excreted directly in bile or require prio...
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abstract：:A series of 4-amino[1,2,4]triazolo[4,3-a]quinoxalines has been prepared. Many compounds from this class reduce immobility in Porsolt's behavioral despair model in rats upon acute administration and may therefore have therapeutic potential as novel and rapid acting antidepressant agents. Optimal activity in this test i...
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abstract：:G-protein coupled receptor (GPCR) GPR109a is a molecular target for nicotinic acid and is expressed in adipocytes, spleen, and immune cells. Nicotinic acid has long been used for the treatment of dyslipidemia due to its capacity to positively affect serum lipids to a greater extent than other currently marketed drugs....
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abstract：:A series of 3-substituted [1,2,4]triazino[4,3-c]benzimidazoles V were prepared and tested at the central benzodiazepine receptor (BzR). These compounds were designed as rigid analogues of the previously described N-benzylindolylglyoxylylamide derivatives IV. The title compounds V showed an affinity which depended dire...
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doi：10.1021/jm00139a024
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abstract：:9,11-Secoestradiol (9) and 11-hydroxy-9,11-secoestradiol (12) have been synthesized starting from 17-acetoxyestradiol 3-methyl ether (1) and found to possess significant antifertility activity in rats. 3-Methoxy-9,11-seco-9-oxo-17beta-acetoxyestra-1,3,5(10)-trien-11-oic acid (2), prepared by CrO3 oxidation of 1, on h...
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doi：10.1021/jm00241a026
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更新日期：2004-03-25 00:00:00
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doi：10.1021/jm00356a019
更新日期：1983-02-01 00:00:00
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更新日期：1998-01-01 00:00:00
abstract：:To eliminate an unwarranted metabolic pathway of the quinoline ring, a set of two compounds, where C-2 position of the antimalarial drug primaquine is blocked by metabolically stable bulky alkyl group are synthesized. Compound 2 [R = C(CH(3))(3)] of the series has produced excellent antimalarial efficacy against P. be...
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更新日期：2004-01-15 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
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更新日期：2004-11-04 00:00:00
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doi：10.1021/jm00094a001
更新日期：1992-08-07 00:00:00
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更新日期：2015-12-10 00:00:00
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更新日期：2011-11-10 00:00:00
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更新日期：2003-07-03 00:00:00
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更新日期：2000-06-01 00:00:00
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更新日期：1992-04-03 00:00:00
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更新日期：2004-02-26 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2019-05-09 00:00:00
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pub_type： 杂志文章
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更新日期：1976-06-01 00:00:00
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更新日期：2009-04-09 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
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更新日期：2006-05-04 00:00:00
