2-Azetidinone – A new profile of various pharmacological activities

Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe

“…Reported heterocyclic CA-4 analogues include imidazole 8,[9] tetrazole 9 [10] and benzoxepin 10 [11] (Figure 2). The azetidin-2-one (β-lactam) ring [12] is an alternative scaffold for potent non-isomerisable combretastatin analogues (11 -13, Figure 2) [13][14][15][16]. Having previously investigated comprehensive structure-activity relationships of these series with a phenyl-substituted ring at the 3-position of the azetidinone ring, it was of importance to extend the SAR by investigating a range of aryl substituents at the 4-position.…”

1-(Morpholin-4-yl)-4-(2-nitrophenyl)spiro[azetidine-3,9′-xanthen]-2-one

“…(Arya et al, 2014;Singh & Sudheesh, 2014;Zeng et al, 2014;Zarei et al, 2013). In addition to their well recognized antibiotic activity, β-lactams exhibit various other biological activities such as thrombin, human, HIV-1 protease, human leukocyte elastase, cholesterol absorption inhibition and antifungal, anticancer, antidiabetic and potential antimalarial properties (Mehta et al, 2010;Singh et al, 2011;Ebrahimi & Jarrahpour, 2014). The synthesis and chemistry of spiro-fused 2-azetidinones has grown steadily over the years and many newly synthesized spiro-fused 2-azetidinones have been reported in the literature (Jarrahpour & Ebrahimi, 2010;Singh et al, 2011).…”

“…For general background to -lactams, see: Arya et al (2014); Ebrahimi & Jarrahpour (2014); Singh & Sudheesh (2014); Zeng et al (2014); Zarei et al (2013); Jarrahpour & Ebrahimi (2010); Mehta et al (2010); Singh et al (2011). For geometric analysis, see : Cremer & Pople (1975); Nardelli (1995).…”

Advances in synthesis of monocyclic beta-lactams

“…Over the years, monocyclic β-lactams have also emerged as powerful synthons and their reactivity has been exploited in synthesis of diverse type of acyclic and cyclic compounds including complex heterocyclic compounds of natural origin and of potential biological interest. Accordingly, the researches on synthesis, 1 biological activity, [2][3][4][5] and applications of β-lactams in organic synthesis, 6-13, have been reviewed from time to time. 1, [14][15][16][17][18][19] This article aims to update the reports on synthesis of monocyclic β-lactams during last five years.…”