Functionality of amidines and amidrazones

Aly, Ashraf A.; El‐Din, Ahmed M. Nour

doi:10.3998/ark.5550190.0009.106

Cited by 74 publications

(30 citation statements)

References 25 publications

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“…The formation of amidines in the presence of transition metals is hardly without precedence, as shown by a recent review. 59 Namely, a direct addition of amine, a nucleophile, to nitrile, is only possible when the C^N carbon atom is made electron-decient. 52 Ordinary nitriles that lack electronwithdrawing substituents, such as acetonitrile, require a presence of a Lewis acid such as AlCl 3 , ZnCl 2 60 or other metal-based activating agents such as lanthanide(iii) triates, 61 CuI, 24 CuCl, 58 SmI 2 62 or ytterbium amides, 63 combined with lengthy reaction times and harsh conditions.…”

Section: Syntheses and Reactivitymentioning

confidence: 99%

From cyclic amines and acetonitrile to amidine zinc(ii) complexes

et al. 2020

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Section: Syntheses and Reactivitymentioning

confidence: 99%

From cyclic amines and acetonitrile to amidine zinc(ii) complexes

et al. 2020

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“…The most venerable method for the nitrile to amidine conversion is known as the Pinner amidine synthesis which was first described by Pinner in 1877 (Pinner and Klein, 1877). This method, which is arguably the most widely used, has been reviewed by several authors (Shriner and Neumann, 1944; Roger and Neilson, 1961; Eloy and Lenaers, 1962; Aly and Nour-El-Din, 2008). Scheme 1 illustrates this 2-step process which was used in the synthesis of furamidine (Fig.…”

Section: Design and Synthesismentioning

confidence: 99%

Novel amidines and analogues as promising agents against intracellular parasites: a systematic review

et al. 2013

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SUMMARY Parasitic protozoa comprise diverse aetiological agents responsible for important diseases in humans and animals including sleeping sickness, Chagas disease, leishmaniasis, malaria, toxoplasmosis and others. They are major causes of mortality and morbidity in tropical and subtropical countries, and are also responsible for important economic losses. However, up to now, for most of these parasitic diseases, effective vaccines are lacking and the approved chemotherapeutic compounds present high toxicity, increasing resistance, limited efficacy and require long periods of treatment. Many of these parasitic illnesses predominantly affect low-income populations of developing countries for which new pharmaceutical alternatives are urgently needed. Thus, very low research funding is available. Amidine-containing compounds such as pentamidine are DNA minor groove binders with a broad spectrum of activities against human and veterinary pathogens. Due to their promising microbicidal activity but their rather poor bioavailability and high toxicity, many analogues and derivatives, including pro-drugs, have been synthesized and screened in vitro and in vivo in order to improve their selectivity and pharmacological properties. This review summarizes the knowledge on amidines and analogues with respect to their synthesis, pharmacological profile, mechanistic and biological effects upon a range of intracellular protozoan parasites. The bulk of these data may contribute to the future design and structure optimization of new aromatic dicationic compounds as novel antiparasitic drug candidates.

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“…14 Opisane su mnoge metode sinteze amidina, a najčešće se sintetiziraju iz amida, 15 karboksilnih kiselina 16 i nitrila. 17 Sve navedene reakcije provode se u više stupnjeva, zahtijevaju bezvodne uvjete i često podrazumijevaju rad s opasnim reagensima uz složene postupke izolacije.…”

Section: Trokomponentne Cu(i) Katalizirane Reakcijeunclassified