SYNTHESIS OF 1233A ANALOGS AND THEIR INHIBITORY ACTIVITY AGAINST HYDROXYMETHYLGLUTARYL COENZYME A SYNTHASE

Simple and efficient syntheses of 1233A analogs were developed and the inhibitory activity of the analogs against hydroxymethylglutaryl coenzyme A (HMG-CoA) synthase was determined. Study of the structure-activity relationships revealed that not only the geometry in β-lactone moiety but also the len...

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Veröffentlicht in:	Journal of antibiotics 1992/07/25, Vol.45(7), pp.1139-1147
Hauptverfasser:	SUNAZUKA, TOSHIAKI, TSUZUKI, KAZUO, KUMAGAI, HIDETOSHI, TOMODA, HIROSHI, TANAKA, HARUO, NAGASHIMA, HAJIME, HASHIZUME, HIROKAZU, OMURA, SATOSHI
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Biotechnology & Applied Microbiology Fatty Acids, Unsaturated - chemical synthesis Fatty Acids, Unsaturated - pharmacology General and cellular metabolism. Vitamins Hydroxymethylglutaryl-CoA Synthase - antagonists & inhibitors Immunology Lactones - chemical synthesis Lactones - pharmacology Life Sciences & Biomedicine Medical sciences Mevalonic Acid - analogs & derivatives Mevalonic Acid - pharmacology Microbial Sensitivity Tests Microbiology Pharmacology & Pharmacy Pharmacology. Drug treatments Science & Technology Vero Cells - drug effects
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Zusammenfassung:	Simple and efficient syntheses of 1233A analogs were developed and the inhibitory activity of the analogs against hydroxymethylglutaryl coenzyme A (HMG-CoA) synthase was determined. Study of the structure-activity relationships revealed that not only the geometry in β-lactone moiety but also the length of the carbon side chain is important for inhibitory activity against HMG-CoA synthase.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.45.1139