Comparison of the application of low concentration and 80% phenol solution in pilonidal sinus disease

Objectives Many conservative methods have been applied in the treatment of pilonidal sinus disease (PSD). The most commonly used conservative treatment is 80% phenol solution. Our observations demonstrated that 80% phenol solution caused much destruction in the sacrococcygeal region. Design In this study low concentrations of phenol were used with the aim of reducing the unwanted side-effects of high-concentration phenol without reducing the therapeutic effects. Participants We treated 112 patients (18 women, 94 men) with PSD using phenol solution. Patients were divided into two groups: Group A was treated with a 40% solution of phenol solution, and Group B was treated with an 80% solution of phenol solution. Setting All patients were treated on an outpatient basis. One mL of low (40%) or high (80%) concentration phenol solution was injected into the main sinus orifice. During the check it was observed and noted whether there was skin necrosis, fatty tissue necrosis or abscesses. Main outcome measures The mean age was 27.4 years (6–44). The median length of symptoms was seven months (0.5–132). In the 2.8 years (1–6) of mean follow-up period, the disease recurred in 13 (11.6%) patients. Results This treatment procedure was well-tolerated by all the patients except for those who had unwanted results. No patients in group A had skin necrosis, and only one had abscesses. In group B two patients had abscesses, and three had skin necrosis. Fatty tissue necrosis was seen in one patient in Group A and in five patients in Group B. Recurrence rates were four (7.4%) cases in Group A and nine (15.5%) cases in Group B. Conclusions It is possible to treat patients in a shorter time with a considerably smaller loss of working time, since the destruction of peripilonidal adipose tissue and skin is less. Therefore, the use of low-concentration phenol solution is an option to be considered in the treatment of PSD.PubMe

Synthesis and anticonvulsant activity of some 2-pyrazolines derived from chalcones

Synthesis of chalcones (1,3-diarylprop-2-en-1-ones) and 2-pyrazoline derivatives has been an active field of research due to their established pharmacological effects. In this study, a series of chalcones were prepared with methyl aryl ketones and substituted aldehydes in the presence of sodium hydroxide and methanol through Claisen-Schmidt condensation. 3,5-Disubstituted-4,5-dihydro-1H-pyrazole-1-carbothioamides were synthesized by refluxing selected chalcones and thiosemicarbazide in alkaline medium. Similarly N-3,5-trisubstituted-4,5-dihydro-1H-pyrazole-1-carboxamides were synthesized by refluxing selected chalcones with N-(4-chlorophenyl)semicarbazide in alkaline medium. Structures of the synthesized compounds were confirmed by elemental analysis and spectral (UV, IR, 1H NMR, 13C NMR, and mass) data, which were in line with the proposed structures. All compounds were tested for their anticonvulsant activity using pentylenetetrazole induced seizure (PTZ) and maximal electroshock seizure (MES) tests in mice at a dose level of 50 mg/kg. Among the 2-pyrazoline-1-carbothioamide derivatives, 5-(2,6-dichlorophenyl)-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (2e) reduced grade-5 seizure activity and also increased survival rate in PTZ test. In MES test, 5-(4-methoxyphenyl)-3-[4-(methylsulphonyl)phenyl]-4,5-dihydro-1H-pyrazole-1-carbothioamide(2g) has not only decreased seizure severity, but also increased survival rate. Among the 2-pyrazoline-1-carboxamide derivatives, 3-(5-bromothiophen-2-yl)-N-(4-chlorophenyl)-5-(2,6-dichlorophenyl)-4,5-dihydro-1H-pyrazole-1-carboxamide (3d) having 5-bromothiophen and 2,6-dichlorophenyl moieties and N-(4-chlorophenyl)-5-(2,6-dichlorophenyl)-3-(5-chlorothiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-carboxamide (3e) having 5-chlorothiophen and 2,6-dichlorophenyl moieties showed remarkable activities in PTZ test. Among all tested derivatives, compound 3d was found to be the most active one and reduced grade-5 seizure severity and also increased survival rate

In vivo metabolism of 2-[1 '-phenyl-3 '-(3chlorophenyl)-2 '-propenylyden]hydrazino-3-methyl-4(3H)-quinazolinone in rats

The aim of this study was to investigate by HPLC the in vivo metabolism of 2-[1'-phenyl-3'-(3-chlorophenyl)-2'propenylyden]hydrazino-3-methyl-4(3H)-quinazolinone as a substrate, and as a model compound in rats. The substrate was dissolved in DMSO/water (1:4) and administered intraperitoneally at a dose of 100 mg/kg in a volume of approximately 0.1 mL. Blood samples were taken before and 30 min, 1.5, 3, 6, 9, 11, 30 and 48 h after i.p. drug administration. The chromatographic separation of the substrate and its metabolites was performed using a stainless steel Novopak C18 column (150 x 4.6 mm i.d., 5-mu m particle size). The optimal composition of the mobile phase was reached by introducing different mixtures of pure acetonitrile and water in a linear gradient system. Following the biotransformation of this compound, 2-hydrazino-3-methyl-4(3H)-quinazolinone (M1) and 3-(3-chlorophenyl)-1-phenylprop-2-en-1-one (M2) derivatives were identified together with substrate by comparing them to reference standards using HPLC-UV/DAD. In addition, the composition of these metabolites and substrate was confirmed by LC-MS in plasma

Synthesis and antinociceptive-antimicrobial activities of some new amide derivatives of 3,5-di/-and 1,3,5-trimethylpyrazoles

Some N-(3,5-di-/1,3,5-trimethylpyrazole-4-yl)-4-substitutedbenzamide derivatives were prepared as possible antiociceptive-antimicrobial agents. New amide derivatives (3-12) were synthesized by reacting 4-amino-3,5-di and 1,3,5-trimethylpyrazoles with 4-substitutedbenzoyl chlorides. Hotplate and tail-immersion tests were used for the determination of the antinociceptive activity. Morphine, was used as a standard test drug. All compounds were administered at a dose of 100 mg/kg ip and some of them had significant antinociceptive activity in both tests. Compound 10 (N-(1,3,5-trimethylpyrazole-4-yl)-4-bromobenzamide), was the most active one in both tests among the compounds. The antinociceptive activity of the compounds 10, 11 (N-(1,3,5-trimethylpyrazole-4-yl)-4-chlorobenzamide), and 12 (N-(1,3,5-trimethylpyrazole-4-yl)-4-fluorobenzamide), started at 30 minutes and continued up to 150 minutes in the hotplate test. Also compounds were tested for their in vitro antimicrobial activity, but exhibited weak antibacterial activity