One-pot microwave assisted synthesis and structural elucidation of novel ethyl 3-substituted-7-methylindolizine-1-carboxylates with larvicidal activity against Anopheles arabiensis

Structural investigation of methyl 3-(4-fluorobenzoyl)-7-methyl-2-phenylindolizine-1-carboxylate, an inhibitory drug towards Mycobacterium tuberculosis

“…For instance, indolizines have been found to exhibit analgesic (Vaught et al, 1990), anticancer (Butler, 2008;Sandeep et al, 2016a,b), antidiabetic (Mederski et al, 2012), antihistaminic (Cingolani et al, 1990), anti-microbial (Hazra et al, 2011) and antiviral (Mishra & Tiwari, 2011) activity. It has also been found to act as cyclo-oxygenase (COX-2) inhibitor (Chandrashekharappa et al, 2018b) and to have larvicidal activity against Anopheles arabiensis (Chandrashekharappa et al, 2018a).…”

Anti-Tubercular Activity of Substituted 7-Methyl and 7-Formylindolizines and In Silico Study for Prospective Molecular Target Identification

“…Multicomponent reactions (MCRs) have gained considerable prominence in the drug-discovery process in both academia and industry. MCRs provide medicinal chemists with the opportunity to rapidly access novel scaffolds with a high degree of structural functionality and complexity, accelerating lead compound identification [21]. MCRs are associated with various advantages such as single operation, synthetic efficiency, and a diversity of inputs, both economic and ecological.…”

“…It is a well-known pharmacophore responsible for various promising pharmacological properties. For instance, indolizines were found to exhibit analgesic [8], anticancer [9,10], antidiabetic [11], antihistaminic [12], anti-inflammatory [13,14], antileishmanial [15], antimicrobial [16], antimutagenic [17], antioxidant [18], antiviral [19], larvicidal [20,21], and herbicidal [22] activities. However, the anti-TB activity of indolizine is poorly documented in the literature [23][24][25][26].…”

“…However, the anti-TB activity of indolizine is poorly documented in the literature [23][24][25][26]. Recently, our group started investigating multifunctionalized indolizine pharmacophores for their chemistry, structural elucidation, and pharmacological properties, including their anticancer properties [10], cyclooxygenase-2 (COX-2) inhibition properties [14,27], and larvicidal activity against Anopheles arabiensis [21]. In continuation of our effort to identify novel potent anti-TB agents of cyclic depsipeptides [28] and heterocyclic origin [29][30][31][32][33][34], we previously identified a series of 7-acetyl indolizines exhibiting interesting anti-mycobacterial activity.…”

Larvicidal study of tetrahydropyrimidine scaffolds against Anopheles arabiensis and structural insight by single crystal X‐ray studies

“…HPM is a versatile pharmacophore that has exhibited larvicidal activity against Anopheles arabiensis , Aedesaegypti , and Culex quinquefasciatus . In view of such versatile pharmacological properties of HPM molecules and in continuation of our effort in search of novel heterocyclic larvicidal agents, a new series of methyl/ethyl 4‐(substitutedphenyl/pyridyl)‐6‐methyl‐2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidine‐5‐carboxylate derivatives 4a–g have been designed in Scheme 1. In this series of compound, the presence of hydrogen bond donors like hydroxy (–OH), hydrogen bond acceptor (pyridine –N) and halogen atom (chlorine) is explored to evaluate the potential of larvicidal activity of HPM molecules.…”