For effective drug design and development,
an integrated process utilizing all available information from structural,
thermodynamic, and biological studies plays a very important role.
To understand the energy basis of molecular interactions utilizing
various thermodynamic methods, volumetric and acoustic studies are
vital early in the development process of any drug toward an optimal
energy interaction profile while retaining a good pharmacological
assay. In this article, we are reporting the data of densities (ρ)
and speeds of sound (u) of an antiarrhythmic agent, namely,
procainamide hydrochloride in an aqueous binary and aqueous solution
of amino acids, i.e., l-alanine and l-valine at T = (298.15, 308.15 and 318.15) K. Different thermodynamic
parameters such as the apparent molar volume (V
ϕ) of the solute, the isentropic compressibility (κs) of the solution, and the apparent molar isentropic compressibility
(κϕ) of procainamide hydrochloride in water
and aqueous solutions of l-alanine and l-valine
have been computed using the density and speed of sound data at different
temperatures. The limiting apparent molar volume (V
ϕ
0) of
solute and the limiting apparent molar compressibility (κϕ
0) of solute
in binary and ternary aqueous solutions have been obtained by extrapolating
the plots. The results have been interpreted in light of the competing
solute–solute and solute–solvent interactions.
One‐pot synthesis of 1‐([6‐bromo‐2‐hydroxy‐naphthalen‐1‐yl]‐aryl‐phenyl)methyl)‐3‐chloro‐4‐(aryl‐phenyl)azetidin‐2‐ones has been reported in the present research work via Staudinger [2 + 2] ketene‐imine cycloaddition reaction pathway. The reaction of 1‐((Benzylideneamino)(aryl)methyl)‐6‐bromo‐naphthalen‐2‐ols with chloroacetic acid and triethylamine afforded 1‐([6‐bromo‐2‐hydroxynaphthalen‐1‐yl]aryl‐phenyl)methyl)‐3‐chloro‐4‐(aryl‐phenyl)azetidin‐2‐ones. For the structural elucidation of series of compounds, different analytical and spectroscopic techniques such as elemental analysis, IR spectra, 1H‐NMR spectra and mass spectra were used. All the newly synthesized compounds were tested for their anti‐bacterial activity studies. It revealed that some of the compounds possesses moderate to good activities as compared to standard drugs. The widest spectrum of anti‐bacterial activities against both gram‐positive and gram‐negative bacterial strains among the examined compounds possessed having more hydroxyl group along with β‐lactam ring compared to other substituted azetidinones.
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