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A new class of 2‐aryloxy‐N‐phenylacetamide and N′‐(2‐aryloxyoxyacetyl) benzohydrazide derivatives with different active moieties were synthesized and screened for their antibacterial activity. Structural characterization of synthesized compounds was performed using HR‐MS, 1H‐NMR, and 13C‐NMR spectral data. Amongst the synthesized compounds, 4‐{2‐[2‐(2‐chloroacetamido)phenoxy]acetamido}‐3‐nitrobenzoic acid (3h) and 2‐chloro‐N‐(2‐{2‐[2‐(2‐chlorobenzoyl)hydrazinyl]‐2‐oxoethoxy}phenyl)acetamide (3o) have shown good antibacterial activity against a selected panel of bacteria. Besides, compounds also exhibited bactericidal activity against P. aeruginosa (3h, 0.69 μg/mL) and S. aureus (3o, 0.62 μg/mL) as evident by MBC and time‐kill kinetics studies. In silico molecular docking and ADMET properties of newly synthesized compounds revealed that compounds could be considered as promising antibacterial agents.

Diabetic wound (DW) is considered as one of the serious complications associated with diabetes mellitus. Though some pharmacological approaches are available for managing DW, none of them has been reported to be very effective. Widely accepted options for its management include treatment of infection caused by various pathogens, wound debridement, reducing the period of the prolonged inflammatory phase, and supervision of the remodeling phase of wound healing. Satisfactory management of DW thus requires exploring new avenues for finding a potential therapeutic strategy. Literature shows that human beta defensins (HBDs) help in combating the insulin resistance by inhibiting the production of glucocorticoids, reducing chronic inflammation by acting through Toll-like receptor signaling pathway, and provoking cell migration, proliferation, angiogenesis, and stabilization of fibroblasts and keratinocytes, ultimately resulting in wound closure. In the present review, beneficial role of HBDs in the treatment of DW is discussed in detail.

A series of novel aryl/heteroaryl benzohydrazide (3 a–d) and aryl/heteroaryl phenylacetamide derivatives (5 a–g) were designed, synthesized and characterized by spectral techniques. The synthesized compounds were screened against pathogenic bacteria to assess their in vitro antibacterial properties. From the eleven synthesized compounds, 3 b(0.7 μg/mL) and 3 c(0.6 μg/mL) exhibited potent activity against a panel of organisms especially against S. aureus. Further, time‐kill study confirmed the bactericidal activity of 3 b and 3 c against S. aureus, that may be because of conjoined benzothiazole and benzohydrazide moieties in their structures. Extra‐precision docking and binding free energy calculation were also performed for the title compounds, in which 3 c(‐6.23 kcal/mol) exhibited higher binding affinity against S. aureus ParE (SaParE). Molecular dynamic simulation of 50 ns was used to find out the stability of predicted binding conformation of 3 c/SaParE. Besides, assessment of in silico ADMET properties illustrates that the title compounds were in agreement with Lipinski's rule parameters. The study could offer a unique framework that may lead to the discovery of novel antibacterials.

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