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Biotransformation of Sesquiterpenoids, Ionones, Damascones, Adamantanes, and Aromatic Compounds by Green Algae, Fungi, and Mammals
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Yoshinori Asakawa, Yoshiaki Noma
In conclusion, a number of sesquiterpenoids were biotransformed by various fungi and mammals to afford many metabolites, several of which showed antimicrobial and antifungal, antiobesity, cytotoxic, neurotrophic, and enzyme inhibitory activity. Microorganisms introduce oxygen atom at allylic position to give secondary hydroxyl and keto groups. Double bond is also oxidized to give epoxide, followed by hydrolysis to afford a diol. These reactions precede stereo- and regiospecifically. Even at nonactivated carbon atom, oxidation reaction occurs to give primary alcohol. Some fungi like A. niger cleave the cyclopropane ring with a 1,1-dimethyl group. It is noteworthy that A. niger and A. cellulosae produce totally different metabolites from the same substrates. Some fungi occurs reduction of carbonyl group, oxidation of aryl methyl group, phenyl coupling, and cyclization of a 10-membered ring sesquiterpenoids to give C6/C6- and C5/C7-cyclic or spiro compounds. Cytochrome P-450 is responsible for the introduction of oxygen function into the substrates.
Investigation of radiation protective features of azadispiro derivatives and their genotoxic potential with Ames/Salmonella test system
Published in International Journal of Radiation Biology, 2023
Burak Alaylar, Bünyamin Aygün, Kadir Turhan, Mehmet Karadayı, Esra Cinan, Zuhal Turgut, Gökçe Karadayı, Mohammed Ibrahim Abu Al-Sayyed, Medine Güllüce, Abdulhalik Karabulut
Since spiro compounds have many uses, synthesis studies have been continuing recently. Most of the spiro compounds are anticancer (Reddy et al. 2011; Erugu et al. 2014; Das et al. 2020) anticonvulsants (Kesharwani et al. 2009; Zaher et al. 2010), antibacterial (Youssef and Amin 2010) anti-Alzheimer's (Kamiński et al. 2008), antituberculosis (Al Houari et al. 2008), anti-dermatitis (Yoshikawa et al. 2009), analgesic and antimicrobial (Srivastava et al. 2020). In addition, these compounds are also used in industry and agriculture (Thadhaney et al. 2010). On the other hand, the quinoline derivatives were synthesized and their genotoxic potentials in both radiation levels were determined and studies have shown that these syntheses can be used for a protective drug that can be developed for both gamma and neutron radiation (Aygün et al. 2021c; Alaylar et al. 2021).
An updated patent review of monoacylglycerol lipase (MAGL) inhibitors (2018-present)
Published in Expert Opinion on Therapeutic Patents, 2021
Giulia Bononi, Giulio Poli, Flavio Rizzolio, Tiziano Tuccinardi, Marco Macchia, Filippo Minutolo, Carlotta Granchi
Takeda Pharmaceutical Company patented heterocyclic spiro compounds as MAGL inhibitors to treat or prevent neurodegenerative diseases (i.e. ALS, Huntington’s disease, AD, PD), anxiety disorders, pains, epilepsy, depression, glaucoma, migraine, traumatic brain injury, and brain edema [57]. MAGL inhibitory activities were evaluated by using recombinant His-hMAGL enzyme and adopting a high-throughput mass spectrometry technology. Most of the spirocycles completely inhibited MAGL at the concentration of 10 μM. Inhibitors 28–30 (Figure 2), which are characterized by a cyclobutyl 6-oxo-7-oxa-2,5-diazaspiro[3.4]octane-2-carboxylate scaffold, were further tested in vivo in C57BL/6 J mice to measure brain 2-AG and AA concentrations. These compounds, after oral administration by gavage at a concentration of 1 mg/kg body weight, increased 2-AG levels in the brain compared to the control group of mice and they consequently decreased intracerebral AA concentration.
Spiro heterocycles bearing piperidine moiety as potential scaffold for antileishmanial activity: synthesis, biological evaluation, and in silico studies
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Mounir A. A. Mohamed, Asmaa M. Kadry, Salma A. Bekhit, Mohammed A. S. Abourehab, Kikuko Amagase, Tamer M. Ibrahim, Ahmed M. M. El-Saghier, Adnan A. Bekhit
Interestingly, various spiro-compounds were reported to possess antiprotozoal and antileishmanial activities. For instance, compound A (Figure 1) is able to halt the replication of both promastigote and axenic amastigote forms of L. infantum in a dose-dependent manner25. Moreover, the spiro-compound B26 acts as a catalytic inhibitor of the unusual bisubunit DNA topoisomerase IB of L. donovani26. Furthermore, other spiro-compounds were reported to display promising antileishmanial activities, such as C27, as shown in Figure 1.