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Nucleic Acids as Therapeutic Targets and Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
A substituted benzoquinone ring has been employed as an “anchor” for aziridine rings in the experimental agents AZQ and BZQ. The aziridine moieties are deactivated by the withdrawal of electrons from their nitrogens into the quinone carbonyl groups via the six-membered ring. These molecules have been employed as experimental bioreductive prodrugs because reduction of the quinone ring to either the semiquinone or the hydroxyquinone species reverses the electron flow, thus increasing the basicity of the aziridine nitrogens which allows them to become activated via protonation. No benzoquinone agents of this type have yet been approved for clinical use.
Identification of proper herbs
Published in C. P. Khare, Evidence-based Ayurveda, 2019
Taalisha still remains a drug of disputed source. Abies webbiana and Taxus wallichiana both are known as Taalisha patra. Two samples of needles and twigs from two different locations of central Nepal gave alpha-pinene 3.0, 10.3; fascile 3.5, 9.3; beta-pinene 5.1, 3.3; limonene 6.1, 2.3; bornyl acetate 4.2, 15.5; and carvone 5.8, 0.75%, respectively. Leaves obtained from Sikkim-Himalayan region gave a bioflavonoid, abiesin; two glycosides, methylbetuloside, and betuloside; n-triacontanol and beta-sitosterol. A new alkaloid, 1-(4’ methoxyphenyl)-aziridine was isolated.
Immunotherapy of Graves’ Eye Disease
Published in George S. Eisenbarth, Immunotherapy of Diabetes and Selected Autoimmune Diseases, 2019
N. R. Farid, G. Kahaly, J. Beyer
The aziridine derivative ciamexon is being tried out at present in autoimmune diseases. This agent has immunomodulatory properties and inhibits antibody production in experimental animals. It also appears to modify autoaggression in animal models of autoimmune disease, e.g., in insulin-dependent diabetes mellitus and myasthenia gravis.16
Aromatic sulphonamides of aziridine-2-carboxylic acid derivatives as novel PDIA1 and PDIA3 inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
D. Zelencova-Gopejenko, V. Andrianov, I. Domracheva, I. Kanepe-Lapsa, M. Milczarek, M. Stojak, K. Przyborowski, F. A. Fedak, M. Walczak, K. Kramkowski, J. Wietrzyk, S. Chlopicki, I. Kalvins
Activated aziridines, such as aziridine-2-carboxylic acid (Az-COOH), have been suggested as promising cysteine protease inhibitors. It was found that the aziridine moiety of Az-COOH is substantially more reactive towards cysteine’s thiol groups than activated double bonds (e.g. N-ethylmaleimide, or halides such as alpha-iodopropionic acid or chloroacetic acid). Markedly, the amide of Az-COOH (Az-CONH2) as a cysteine proteinase inhibitor is magnitudes of order less potent than Az-COOH4. This observation reflects the lower reactivity of Az-CONH2 towards the thiol group of cysteine compared to the methyl ester of Az-COOH (Az-COOMe). Surprisingly, among a number of known cytostatic derivatives of Az-COOH, Az-CONH2 was selected and approved in the USSR as an active pharmaceutical ingredient (API) of an anti-cancer immunomodulator with the brand name Leakadine®5.
Significant role of cationic polymers in drug delivery systems
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Masoud Farshbaf, Soodabeh Davaran, Amir Zarebkohan, Nasim Annabi, Abolfazl Akbarzadeh, Roya Salehi
Poly(ethyleneeimine) (PEI), a none-degradable polymer comprising primary, secondary and tertiary amino groups which is one of the most commonly employed cationic polymers in various industries. PEI can be obtained in two various structures: (i) linear PEI (LPEI) is a solid form of PEI and (ii) branched PEI (BPEI) is a highly viscous liquid at the room temperature. LPEI contains primary and secondary amino groups, while BPEI, in addition to primary and secondary groups, also possesses tertiary amino groups (with ratio of 1:2:1) which makes BPEI more stable and suitable transfection vector [107]. It is worth noting that, at physiological conditions 25% of these amino groups are protonated which gives PEI high buffer capability that could be beneficial in endosomal escape mechanisms. Brissault et al. [108] synthesized LPEI by hydrolysis and/or reduction of poly(2-ethyl-2-oxazoline) (PEtOXZ) (Figure 12(A)). A mixture of PEtOXZ (1 g), hydrochloric acid (11 ml, 37%) and 8 ml water was heated at 110 °C for 3 h. After solvent evaporation, the obtained mixture was dissolved in water and pH was adjusted to 9–10 by adding a proper amount of NaOH. Then the aqueous phase was vaporized, the residue washed with methylene chloride and consequently, the organic layer (Na2SO4) dried and vaporized. Based on results, yield of the polymer was 320 mg (71%) [108]. In another study, Harpe et al. [109] used acid-catalyzed polymerization of aziridine for the synthesis of BPEI (Figure 12(B)). First, aziridine (5 ml) were dissolved in 50 ml distilled water and 0.5 ml of 32% (w/v) hydrochloric acid (HCl) were added to the solution, then the flask was sealed and submerged in oil bath in 65 °C and kept for 24 h. NaOH was added to the mixture in order to neutralization process and then water was vaporized and the obtained polymer was dried under vacuum for 24 h [109].