Author
V. I. Shchelokov
Bio: V. I. Shchelokov is an academic researcher from Russian Academy of Sciences. The author has contributed to research in topics: Acylation & Phthalic anhydride. The author has an hindex of 3, co-authored 6 publications receiving 100 citations.
Topics: Acylation, Phthalic anhydride, Amide, Peptide, Ring (chemistry)
Papers
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TL;DR: In this paper, a new reaction, the hydroxy-and aminoacyl incorporation in aliphatic and alicyclic N-hydrox-(amino)acl amides is described in detail.
72 citations
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18 citations
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8 citations
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TL;DR: The complete synthesis of the antibiotic serratamolide has been effected, definitively demonstrating its structure as mentioned in this paper, and it has been shown that it can be synthesized in the laboratory.
Abstract: The complete synthesis of the antibiotic serratamolide has been effected, definitively demonstrating its structure.
1 citations
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1 citations
Cited by
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645 citations
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TL;DR: A convenient synthesis of 4-nitrobenzyl-substituted macrocyclic tetraamines and their conversion to bifunctional poly(amino carboxylate) chelating agents is described and preparation of the isothiocyanate derivatives and 14C labeled che lating agents are described.
116 citations
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94 citations
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TL;DR: This minireview has drawn on recent progress to highlight the key reaction design features that enable successful ‘normal-to-medium’ ring expansion for the synthesis of these medicinally important molecular frameworks.
Abstract: Medium-sized rings have much promise in medicinal chemistry, but are difficult to make using direct cyclisation methods. In this minireview, we highlight the value of ring expansion strategies to address this long-standing synthetic challenge. We have drawn on recent progress (post 2013) to highlight the key reaction design features that enable successful 'normal-to-medium' ring expansion for the synthesis of these medicinally important molecular frameworks, that are currently under-represented in compound screening collections and marketed drugs in view of their challenging syntheses.
94 citations
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TL;DR: Antimalarial properties of purified prodigiosin (I), the cyclotetradepsipeptide serratamolide (II), an ethyl alcoholic extract of Serratia marcescens (III) from which I, II and other metabolites can be derived, and two dipyrrolylmethenes (IV a and b) against Plasmodium berghei in mice are investigated.
Abstract: SINCE Babes in 1885 claimed the complete inhibition of cholera vibrio by an old culture of Micrococcus prodigiosus there have been numerous descriptions1–3 of antibiotic properties associated with the bacterium Chromobacterium prodigiosum (Serratia marcescens) and the bipyrrolylpyrrolylmethene prodigiosin (I), which occurs in the red bacterial pigment. The purity of the metabolite4,5 used in the earlier investigations is suspect and the earlier claims like those for the bacterium lack definition of the true causative factor. In this regard the prodigiosin used has been considered too toxic for therapeutic use, although it has evidently been used in the clinical treatment of some cases of disseminated coccidioidomycosis (San Joaquin Valley fever)6. Goble and Boyd7 examined a number of porphyrins, bilirubinoids, pyrroles and congeners against Trypanosoma congolese in mice and found chlorophyllins, containing either magnesium or copper, and haematoporphyrin to be effective in delaying death and curative with prolonged treatment. We have investigated the antimalarial properties of purified prodigiosin (I), the cyclotetradepsipeptide serratamolide (II)4,8,9, an ethyl alcoholic extract of Serratia marcescens (III) from which I, II and other metabolites can be derived4, and two dipyrrolylmethenes (IV a and b) against Plasmodium berghei in mice. Prodigiosin showed definite activity (Table 1) against the parasite, which took about twice as long to kill the mice as compared with untreated infections, whereas the other materials exhibited only weak activity at the same or comparable concentrations.
90 citations