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Syntezy i aktywność biologiczna wybranych zasad Mannicha

Nawrocka W. P., Nowicka A.

Wiadomości Chemiczne

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2014

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[Z] 68, 11-12

981--1008

EN

The Mannich reaction is important for the synthesis and modification of biologically active compounds. Mannich bases – substituted products containing different heterocyclic system in their structures seem to be suitable candidates for further chemical modifications and might be of interest as pharmacologically active compounds. The main goal of this article is to present synthesis and biological activity of selected Mannich bases. Based on a review of the chemical literature, Mannich bases showed a multipharmacological effects. The Mannich bases, containing various heterocyclic systems were identified as potent anticancer agents. Presented compounds exhibit cytotoxic, antiproliferate in vitro, anticonvulsant, antioxidative, antiinflaminatory and analgesic activity. Some of them can be used in a treatment of diabetes and hypertension.

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Syntezy i aktywność biologiczna pochodnych pirydopirydazyny

Nawrocka W. P., Nowicka A.

Wiadomości Chemiczne

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2014

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[Z] 68, 1-2

67--94

EN

For many years all six isomers of pyridopyridazines have been an interesting class of heterocyclic compounds because of their biological and chemical properties. Endralazine is a hypotensive drug, which contain pyrido[4,3-c]pyridazine structure. Presented in this paper selected compounds exhibit antiviral [20] and antibacterial [21, 22] activity. Based on review of the chemical literature, derivatives of pyridopyridazine showed a multipharmacological effects such as analgesic [23–29] and diuretic [33–38] activity. Some chemical compounds, containing pyridopyridazine moiety showed anticancer activity in vitro with different mechanism of action [12, 15, 18, 19]. Novel pyrazolopyridopyridazine derivatives have been identified as more potent and selective phosphodiesterase 5 (PDE5) inhibitors than sildenafil [41]. Pyrido[2,3-d] pyridazine derivatives were synthesized as selective PDE4 inhibitors [44–46], with good selectivity profile and less undesiderable side effects. 2,3,8-Trisubstituted pyrido[ 2,3-d]pyridazines were novel classes of GABA-A receptor benzodiazepine binding site ligands [30, 31]. While pyrido[2,3-c]pyridazine derivatives were selective agonists for the benzodiazepine site of GABA-A receptor [32]. Some of new substituted pyrido[3,2-c]pyridazine derivatives possess molluscicidal activity [54] and can be used as biodegradable agrochemicals.

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Wybrane Metody syntezy 2-amino-1H-benzimidazolu

Nawrocka W. P., Nowicka A.

Wiadomości Chemiczne

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2013

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[Z] 67, 7-8

715--732

EN

2-Amino-1H-benzimidazoles have attracted much attention due to their varied biological activities toward numerous diseases. 2-Amino-1H-benzimidazole core structures can be found in commercial drugs such as astemizole, mizolastine or carbendazime [1, 2]. 2-(N-substituted)-aminobenzimidazoles are widely used chemical substances in medicinal chemistry. Several compounds from this class have been used as anticancer, antihistamine and antiviral agents [3–5]. An efficient practical method for the synthesis of a diverse collection of 2-aminobenzimidazoles would be of great value for drug discovery. Several synthetic methods have been reported in the literature for the synthesis of 2-aminobenzimidazoles [11]. The synthesis of 2-aminobenzimidazole may be carried out in several ways. The most popular and economical method involves the treatment of various 2-substituted anilines with different cyclising agents to yield 2-aminobenzimidazoles. The cyclocondensation of an appropriate o-phenylenediamine with cyanogen bromide affords high yields of 2-aminobenzimidazoles [12]. Hydrogenation of o-cyanaminonitrobenzene over Raney nickel catalyst gives 2-aminobenzimidazole [34, 35]. Substituted 2-aminobenimidazoles have also been prepared by oxidation of the corresponding substituted thioureas with isothiocyanates using desulfurizing agents such as mercury-(II) oxide or methyl iodide [18–21].

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Syntezy wybranych, nowych pochodnych 2-amino-1H-benzimidazolu i ich mechanizmy działania biologicznego

Nowicka A., Nawrocka W. P.

Wiadomości Chemiczne

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2013

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[Z] 67, 3-4

203--225

EN

Many 2-amino-1H-benzimidazole drugs such as antihistaminic mizolastine and norastemizole or antiparasitic mebendazole, albendazole and thiabendazole have been used in clinic [1, 2]. Benomyl and its metabolite Carbendazim are both antifungal and anticancer drugs [4]. Recently, a lot of literature has revealed that 2-amino-1H-benzimidazole derivatives could effectively inhibit the growth of various microorganisms, what suggests that 2-aminobenzimidazole compounds should have large potential as a new type of antibacterial [15] and antifungal [18] agents. A number of 2-aminobenzimidazoles have exhibited antiproliferative in vitro properties [11]. Some new compounds, containing in theirs structures 2-aminobenzimidazole, show interesting and diverse cytotoxic mechanism of action, e.g. induce apoptosis of cancer cells [13]. Some of 2-aminobenzimidazole analogues are histamine and serotonin receptors antagonists [32]. 2-Aminobenzimidazoles derivatives have been frequently found to display a variety of biological activities like anti-inflammatory, antioxidant and anticoagulant [32] properties.

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Syntezy, struktury i aktywność biologiczna pochodnych imidazo[4,5-b] pirydyny. Część II

Liszkiewicz H., Nowicka A., Nawrocka W. P.

Wiadomości Chemiczne

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2013

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[Z] 67, 3-4

227--250

EN

The main goal of this article is to present selected syntheses, structures and a various biological activity of imidazo[4,5-b]pyridine derivatives. During the past 20 years the biological activity of imidazo[4,5-b]pyridine have been intensively studied. Based on the review of the chemical literature, it was shown that derivatives of imidazole[4,5-b]pyridine showed a multipharmacological effects such as antibacterial effect [20–22] and antituberculotic activity [25–33], nonsteroidal antiinflammatory activity [35–43] and analgesic [44, 45] effect. Among compounds of this class antagonists of angiotensin II receptors that exhibit hypotensive activity are also known [9–11]. Compounds containing imidazo[4,5-b]pyridine moiety can be synthesized from different substrates. The most useful starting compounds for the synthesis of imidazo[4,5-b]pyridine are derivatives of 2,3-diaminopyridine [1–3].