79238-14-5Relevant academic research and scientific papers
Structural Modification of Natural Product Ganomycin i Leading to Discovery of a α-Glucosidase and HMG-CoA Reductase Dual Inhibitor Improving Obesity and Metabolic Dysfunction in Vivo
Wang, Kai,Bao, Li,Zhou, Nan,Zhang, Jinjin,Liao, Mingfang,Zheng, Zhongyong,Wang, Yujing,Liu, Chang,Wang, Jun,Wang, Lifeng,Wang, Wenzhao,Liu, Shuangjiang,Liu, Hongwei
, p. 3609 - 3625 (2018/05/01)
It is a great challenge to develop drugs for treatment of metabolic syndrome. With ganomycin I as a leading compound, 14 meroterpene derivatives were synthesized and screened for their α-glucosidase and HMG-CoA reductase inhibitory activities. As a result, a α-glucosidase and HMG-CoA reductase dual inhibitor ((R,E)-5-(4-(tert-butyl)phenyl)-3-(4,8-dimethylnona-3,7-dien-1-yl)furan-2(5H)-one, 7d) with improved chemical stability and long-term safety was obtained. Compound 7d showed multiple and strong in vivo efficacies in reducing weight gain, lowering HbAlc level, and improving insulin resistance and lipid dysfunction in both ob/ob and diet-induced obesity (DIO) mice models. Compound 7d was also found to reduce hepatic steatosis in ob/ob model. 16S rRNA gene sequencing, SCFA, and intestinal mucosal barrier function analysis indicated that gut microbiota plays a central and causative role in mediating the multiple efficacies of 7d. Our results demonstrate that 7d is a promising drug candidate for metabolic syndrome.
2-(3-oxoalk(en)yl)-3-isothiazolones and derivatives as antimicrobial agents
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, (2008/06/13)
Antimicrobial compounds of the formula STR1 wherein R is hydrogen, halogen or (C1 -C4)alkyl group; R1 is hydrogen or halogen; alternatively, R and R1 may be taken together with the carbons to which they are attached to for
EFFECT OF STRUCTURE ON PHOTOALCOHOLYSIS OF AROMATIC α-HALOKETONES
Izawa, Yasuji,Watoh, Yasushi,Tomioka, Hideo
, p. 33 - 36 (2007/10/02)
Desyl halide, α-bromophenylacetate, and 2,5-dimethoxy-α-bromoacetophenones undergo smooth photomethanolysis, whereas simple α-bromoacetophenone undergoes photoreduction to give acetophenone.
PHOTOCHEMISTRY OF 5-ARYL-2(3H)-FURANONES. A NEW ROUTE TO THE SYNTHESIS OF CHROMONES
Martinez-Utrilla, R.,Miranda, M. A.
, p. 2111 - 2114 (2007/10/02)
The photochemistry of 5-phenyl-, 5-(2',5'-dimethoxyphenyl)-, 5-(2'-acetoxy-5'-methoxyphenyl)- and 5-(2',5'-diacetoxyphenyl)-2(3H)-furanone (1a-d) has been investigated.Compound 1a yields pheny vinyl ketone as expected.Similarly, 1b affords the corresponding aryl vinyl ketone but, in this case, photodimerization also occurs.Irradiation of the two o-acetoxyaryl furanones 1c and 1d gives rise to the formation of chromones as the main products.This interesting result can be accounted for in terms of a photochemical opening of the lactonic ring followed by radical addition to the acetoxy group.
