SYNTHESIS OF NEW SUBSTITUTED PROCAINE HYDROCHLORIDE COMPOUNDS AND THEIR USE IN SPECTROPHOTOMETRIC DETERMINATION OF TETRACYCLINE HYDROCHLORIDE THROUGH DIAZOTIZATION-COUPLING REACTIONS

Background: Tetracycline is one of the most important antibiotics. It is used to treat many different bacterial infections. It is often used in treating severe acne, or sexually transmitted diseases such as syphilis, gonorrhea, or chlamydia. In some cases, tetracycline is used when penicillin or another antibiotic cannot be used to treat serious infections such as the ones caused by Bacillus anthracis, Listeria, Clostridium, Actinomyces. Aim: synthesized a new novel reagent used to determine TCH spectrophotometrically by using diazonium and coupling reaction. Methods: Four new substituted procaine derivatives were prepared by simple organic methods using aniline derivatives. A spectrophotometric approach was established for the micro-determination of TCH. The stoichiometry was investigated using mole ratio and continuous variation methods, and the stability constant was also estimated. The ΔG, ΔH, and ΔS were determined as thermodynamic parameters for evaluating the effect of temperature on the reaction. Results: Substituted procaine derivatives were prepared, and o-hydroxy procaine seems to be the best reagent used to determine TCH by diazotization and coupling reaction. The result was a yellow water-soluble dye with a maximum absorbance of 380 nm. The reaction conditions were studied and optimized. Beers law was obeyed over a concentration range (2.5–50) μg.mL-1 for TCH. The molar absorptivity was (14.4669.103) L.mol-1.cm-1, and the detection limit was (0.5052) μg.mL-1. The stoichiometry of the formed product was found 1:1 (o-hydroxyprocaine: TCH). The stability constant indicated that the product formed was stable, and the thermodynamic parameters showed that the diazonium salt reaction was preferred to occur at a low temperature. Conclusions: a simple, accurate, and fast method was developed to determine TCH in pure form and pharmaceuticals by coupling the TCH with a newly synthesized procaine derivative reagent (o-hydroxy procaine) in a basic medium.

Preparation, analytical Studies and application of a New Azodye Derived from Pharmaceutical Materials (Procaine Hydrochloride & Salicylic acid)

Procaine hydrochloride was used as an aromatic amine, and salicylic acid (5-[2-(diethylamino)-4-benzoateazo]-2-hydroxybenzoic acid) was used to make a new azodye derived from pharmaceutical materials ( PS ).C.H.N., H1-NMR, I.R., and visible spectroscopic techniques have also been used to characterize dye. At different pH values ( 2 - 12 ), the electronic spectra of this azo dye was investigated in terms of acid-base properties, which included defining isobestic points and determining protonation and ionization constants. The effect of different polarities of solvents on the electronic spectra was the subject of another study. The dye has been used in a variety of applications, including as an indicator for strong acid with strong base and for nitrite determination.

The local anaesthetic procaine prodrugs ProcCluster® and Procaine-hydrochloride impair SARS-CoV-2 replication in vitro

The SARS-CoV-2 pandemic has had the world in suspense for more than a year. Even if more and more vaccines are approved there is still an urgent need for efficient antiviral treatment strategies. Here, we present data on the inhibitory effect of the local anaesthetic procaine, especially the prodrugs ProcCluster® and Procaine-hydrochloride on SARS-CoV-2 infection in vitro. Remarkably, similar effects could be shown on the replication of influenza A viruses in cell culture systems. Since the active ingredient procaine is well-tolerated and already used in the clinics for anaesthetic purposes, the further investigation of this substance could enable its reuse in antiviral therapy, including SARS-CoV-2.

Quantitative sperm characteristics of Tankwa goats with special reference to hyperactivated motility

Computer-assisted semen analysis (CASA) is an automated and objective method of evaluating structural (e.g. morphology) and functional sperm parameters (e.g. motility and hyperactivation). Sperm hyperactivation is essential for successful fertilization and is thus an important aspect in determining the fertility potential of a male. In the current study, CASA was used for standard semen analysis and for comparison of the ability of phosphate buffered saline (PBS), BO sperm wash (10 mM caffeine), 4% lignocaine, and 5 mM procaine hydrochloride to induce hyperactivation in Tankwa goat spermatozoa. Twenty-nine ejaculates were collected from randomly selected male goats by electroejaculation. Although none of the four media affected percentage total sperm motility, lignocaine caused a significant decrease (P >0.05) in percentage progressive motility. Exposure to procaine resulted in an increase in swimming speed (P ≤0.05) and star-spin motility tracks, which are typical of sperm hyperactivation. Using PBS and procaine motility data from individually selected spermatozoa, receiver operator characteristic curves were constructed to distinguish the kinematic parameters employed as cut-off values for sperm hyperactivation. PBS and BO sperm wash did not induce hyperactivation (0.1 + 0.2% and 0.04  0.2% respectively), while lignocaine induced little hyperactivation (3.4 + 3.0%) and procaine hydrochloride had the highest percentage hyperactivation (25.3 + 13.6%). The large variation in hyperactivation (0–54.5%) may reflect inter-individual differences in sperm quality among these males. This study indicated procaine hydrochloride was the most promising hyperactivation-inducing medium for Tankwa goat spermatozoa and should be considered for similar assessments in other animal species Keywords: computer-aided sperm analysis, procaine hydrochloride, sperm kinematics, sperm morphometry, sperm motility