98155-23-8Relevant articles and documents
Structure-Activity Studies of Truncated Latrunculin Analogues with Antimalarial Activity
Varghese, Swapna,Rahmani, Rapha?l,Drew, Damien R.,Beeson, James G.,Baum, Jake,Smith, Brian J.,Baell, Jonathan B.
, p. 679 - 693 (2020/11/30)
Malarial parasites employ actin dynamics for motility, and any disruption to these dynamics renders the parasites unable to effectively establish infection. Therefore, actin presents a potential target for malarial drug discovery, and naturally occurring actin inhibitors such as latrunculins are a promising starting point. However, the limited availability of the natural product and the laborious route for synthesis of latrunculins have hindered their potential development as drug candidates. In this regard, we recently described novel truncated latrunculins, with superior actin binding potency and selectivity towards P. falciparum actin than the canonical latrunculin B. In this paper, we further explore the truncated latrunculin core to summarize the SAR for inhibition of malaria motility. This study helps further understand the binding pattern of these analogues in order to develop them as drug candidates for malaria.
INTERMEDIATE FOR BIOTIN AND PROCESS FOR PRODUCING THE SAME
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Page 23, (2008/06/13)
The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I) : ???wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a) : ???wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.
Latrunculins: NMR study, two new toxins and a synthetic approach
Kashman,Groweiss,Lidor,et al.
, p. 1905 - 1914 (2007/10/02)
A complete 1H and 13C NMR assignment of one of the latrunculins (B) was accomplished with the aid of 2D NMR COSY and CH shift-correlation experiments. The various H-H coupling constants have been determined and a conformation of the macrolide and the tetrahydropyran (THP) ring suggested on basis of the J-values and measured NOE's. The absolute configuration of latrunculin-A(1) was determined on the grounds of its earlier X-ray analysis, and a chemical degradation to a known compound. Two novel latrunculins, -C(3) and -D(4), were isolated from the Red Sea sponge L. magnifica and their structures elucidated. Starting with L-cysteine a synthon for the latrunculins has been synthesized.
