Development of novel chelating ion-exchangers containing azole ligands
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Tuberculosis (TB) is a global health disaster and is a wide-reaching hitch. The improper use of antibiotics in chemotherapy of TB patients led to the current problem of tuberculosis therapy which gives rise to Multi-Drug Resistant (MDR) strains. Nitrogen heterocycles including azole compounds are an important class of therapeutic agent with electron-rich property. Azole-based derivatives easily bind with the enzymes and receptors in organisms through noncovalent interactions, thereby possessing various applications in medicinal chemistry. Research on azoles derivatives have been expansively carried out and have become one of the extremely active area in recent years and the progress is quite rapid. A genuine attempt to review chemistry of azoles and to describe various azole-based compounds synthesized in the last two decades having promising antitubercular potential is described in the present article. It is hopeful that azole compounds may continue to serve as an important direction for the exploitation of azole-based antitubercular drugs with better curative effect, lower toxicity, less side effects, especially fewer resistances and so on.
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Some chelate surfactants were synthesized which had one or two hydrophobic long chained N-alkyl groups and hydrophilic EDTA-metal chelate ions, and their properties were investigated.Some EDTA, N-alkyl substitution products and EDTA, N, N'-bisalkyl substitution products (alkyl group; decyl, dodecyl, tetradecyl, hexadecyl and octadecyl) were treated with salts of some transitional metals as the chelating agents, and many pure chelates were obtained. Some of those chelate surfactants thus obtained showed good surface activities.
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Naturally occurring azole-enriched cyclic peptides have broad biological and pharmacological activities. Previous synthetic efforts have mainly concentrated on the preparation of individual target molecules in solution phase. A solid-phase-based cyclitive cleavage strategy was deployed here for efficient library synthesis of azole cyclopeptide derivatives, which is part of our continuous efforts for the characterization of potent modulators of multidrug resistance efflux proteins. Procedures were optimized to afford the azole cyclopeptides at high yield and purity, eliminating the need for any chromatographic purification steps. This development is ideal for high throughput library synthesis and screening and will facilitate the ultimate discovery of novel azole cyclopeptides with potent biological activities.
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Cleavage (geology)
Solid-Phase Synthesis
Cyclic peptide
Efflux
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The increased numbers of patients with compromised immune systems in the last three decades have increased the chances of life-threatening fungal infections. Numerous antifungal drugs have been developed in the last 20 years to treat these infections. The largest group, the azoles, inhibits the synthesis of fungal sterols. The use of these fungistatic azoles has subsequently led to the emergence of acquired azole resistance. The most common mechanisms that result in azole resistance include the overexpression or mutation of the azole target enzyme, and overexpression of drug transporters that are responsible for azole efflux from cells. Additional, less-frequent mechanisms have also been identified. Understanding azole resistance mechanisms is crucial for current antifungal treatment and for the future development of new treatment strategies.
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Efflux
Antifungal drugs
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Abstract Ausgehend von (I), (IV) und (V) werden die Benzimidazole (III) und (VI) dargestellt, von denen im Ratten‐ 87 ödemtest der Vertreter (VII) eine rößere antiinflammatorische Wirkung als Phenylbutazon besitzt.
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Abstract Azole compounds are widely used as antifungal agents. They interact with cytochrome P450 14DM (CYP51) via coordination of the nucleophilic nitrogen of their heterocyclic ring to the heme iron in CYP51. In our previous study, we showed that the binding affinity of eighteen azole compounds for rat CYP2B and CYP3A was nicely expressed by the bilinear model of log P. In this study, the same azole compounds were examined as to their inhibitory effect on the substrates for human CYP2B6 and CYP3A4. The inhibitory activity determined was analyzed as to the molecular properties of the azole compounds. A nice correlation was found with the bilinear model of log P. These results suggested that the molecular hydrophobicity of the azole compounds plays a major role in the inhibition as well as in the binding. For the binding, HOMO was significant as an additional descriptor in the correlation equations, whereas the existence of a hydroxyl group was significant for the inhibition.
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CYP2B6
CYP3A
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Abstract Natural metalloenzymes stabilize metal centers by utilizing multiple imidazole moieties. Inspired by nature's design principles, the introduction of multiple azoles into ligands has been an effective method for constructing transition metal complexes. Herein, we describe a post‐synthetic modification of peptoids to incorporate multiple azoles on side chains. A simple substitution reaction between an azole (imidazole, pyrazole, 1,2,3‐triazole, and tetrazole) and a chloroalkyl‐containing peptoid provided access to a variety of azole‐containing peptoids. Ten azole‐containing peptoids were synthesized from a single chloroalkyl‐containing peptoid, and the efficiency of each azole for the substitution reaction was evaluated. We have identified that several of the azole‐containing peptoids are capable of binding with Cu(II) and Fe(III). Our synthetic approach can contribute to the expansion of peptoids' chemical diversity and the development of novel peptoids for metal recognition and catalysis.
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Peptoid
Pyrazole
Imidazole
Tetrazole
Triazole
Side chain
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Azoles are a broad and promising class of five-membered heterocyclic compounds containing from one up to five nitrogen atom(s) that can also contain sulfur or oxygen atoms. Widely used as potent antifungal agents, various azole derivatives have also demonstrated many other promising biological properties. This book covers studies of several types of thiazole-based heterocyclic scaffolds, the development of 4-thiazolidinone and thiazole derivatives with heterocyclic fragments as potential candidates for new drugs against trypanosomiasis, numerous synthetic approaches for the synthesis of 1,2,3-triazoles, the application of N-azole, N,S-azole, and N,O-azole as well as their derivatives as retarders of metallic corrosion, and the integration of azoles in materials used for renewable energy processing and applications and wood treatment.
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Thiazole
Benzimidazole
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