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Synthetic Approaches to Inhibitors of Isoprenoid Biosynthesis
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Pedro Merino, Loredana Maiuolo, Ignacio Delso, Vincenzo Algieri, Antonio De Nino, Tomas Tejero
A series of spiro[indole-pyrrolizine], spiro[indole-indolizine], and spiro[indole-pyrrolidine] gem-bisphosphonates (67) were synthesized through multicomponent reactions between substituted isatins (65), amino acids (66) and (64) in the presence of montmorillonite (Scheme 2.19) (Li et al., 2015). It is important to note that this synthetic procedure provided a very useful one-pot strategy for the construction of spiro-gem-bisphosphonates. Reagents and conditions: (i) montmorillonite, MeCN, 0.5–2 h, 80°C. (ii) TMSBr, 18 h, rt; then water, 4 h, rt.
Anti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Katharigatta N. Venugopala, Sandeep Chandrashekharappa, Pran Kishore Deb, Christophe Tratrat, Melendhran Pillay, Deepak Chopra, Nizar A. Al-Shar’i, Wafa Hourani, Lina A. Dahabiyeh, Pobitra Borah, Rahul D. Nagdeve, Susanta K. Nayak, Basavaraj Padmashali, Mohamed A. Morsy, Bandar E. Aldhubiab, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Michelyne Haroun, Sheena Shashikanth, Viresh Mohanlall, Raghuprasad Mailavaram
This study stems from our interest in designing new potential anti-TB therapeutics by focussing on structural modifications of the indolizine scaffold which has demonstrated potential anti-mycobacterial activity as previously reported by our group21–23 and other researchers24–27. Previously, we identified a series of poly-substituted indolizine A21, B22, and C23 as promising anti-TB agents against MDR-TB (Figure 2). Based on our previously reported structure-activity relationship (SAR), the nature and the position of substituents on the indolizine scaffold were found to be very sensitive to retain the anti-mycobacterial activity against susceptible MTB strain as well as rifampicin and isoniazid-resistant clinical isolates of MTB. Approximately, two-thirds of the synthesised indolizines A, B, and C displayed moderate to good potency against susceptible H37Rv MTB strain, whilst half of the active derivatives demonstrated good inhibitory activity against MDR-MTB strain. Indolizine represents a privileged scaffold for the development of bioactive compounds. Several synthetic indolizines have also been reported to possess a broad spectrum of pharmacological activities such as analgesic, anti-inflammatory, anticancer, antidiabetic, antihistaminic, COX-2 inhibition, antileishmanic, antimicrobial, antimutagenic, antioxidant, antiviral, larvicidal, herbicidal and α7 nAChR inhibitors, anti-Alzheimer, antischizophrenic, anticonvulsant and inhibitors of various enzymes28–30.
Inhibitory activities of indolizine derivatives: a patent review
Published in Expert Opinion on Therapeutic Patents, 2020
Kamal M. Dawood, Ashraf A. Abbas
Indolizine (1) is a heteroaromatic ring that belongs to a class of bridgehead-N-fused heterocyclic systems. Indolizine is biostere for indole which is widely common in a large number of natural products, pharmaceuticals, and approved commercial drugs. Indolizine containing compounds have pronounced diverse biological properties and also employed in material science [123–4]. Hydrogenated indolizine (indolizidine) is a well-known core nucleus in many natural product alkaloids which are highly potent scaffolds for drug discovery [56789–10]. One of the most common bioactive indolizidine alkaloids is swainsonine (2) that had a potential chemotherapy drug [11] and toxicological properties [12131415–16] as well as therapeutic potentials [17181920–21]