- Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors
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A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds 8u and 8v exhibited selective and potent DGAT-1 inhibitory activities. In addition, compound 8u dose-dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound 8u for an oral lipid tolerance test showed a significant decrease in plasma triglyceride levels compared with vehicle-treated control animals, indicating delayed absorption of triglyceride after an acute lipid challenge.
- Kim, Minkyoung,Kwon, Jinsun,Kim, Mun Ock,Singh, Sarbjit,Kim, Sang Kyum,Lee, Kyeong,Lee, Kiho,Lee, Hyun Sun,Choi, Yongseok
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p. 628 - 635
(2015/05/04)
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- Synthesis and in vitro antimicrobial and antitumoral screening of novel lipophilic isoniazid analogues. VI
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Various kinds of lipophilic analogues of isonicotinic acid hydrazide (Isoniazid) were synthesized and in vitro explored in a search for antimycobacterial agents with extended activity spectrum against pathogens responsible for the AIDS-associated diseases. The primary in vitro screening showed that a) isonicotinoylhydrazones 1a, 1b, 1d, 1e are more active than the parent drug against non-tubercular mycobacteria (MIC ranging between 0.5 and 4 μg/ml), b) isonicotinohydrazides 6b and 6e display interesting antibacterial activity on some Gram + and Gram - strains, and c) trifluoromethyl-containing compounds 1a and 2c inhibit the growth of several human tumor cell lines at doses between 10-5 and 10-6 M. On the contrary, none of the tested analogues significantly counteracts the cytopathogenicity induced by HIV and HSV viruses.
- Vigorita,Ottana,Maccari,Monforte,Bisignano,Pizzimenti
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p. 267 - 276
(2007/10/03)
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