Synthesis, antimicrobial and anti-inflammatory activities of some new N-substituted sulphonyl indole-3-heterocyclic derivatives

A series of I-substituted sulfonyl indole -3-pyrazolines [4a-j and 5-a-j] and isoxazolines [6a-j] were prepared and tested for their antimicrobial and anti-inflammatory activities. The preparation of compounds 4-6a-j was achieved by treatment of the corresponding chalcones 3a-j with hydrazine hydrate in absolute ethanol, hydrazine hydrate in the presence of glacial acetic acid, and with hydroxylamine hydrochloride in absolute ethanol. The purified products were screened for their antimicrobial activity towards Gram positive, Gram negative bacteria and fungi and also for their anti-inflammatory activity using the carrageenan-induced rat paw oedema. Evaluation of the compounds revealed remarkable antibacterial activity reflected by their ability to inhibit Gram positive and Gram negative bacteria, and also revealed remarkable anti-inflammatory activity reflected by their ability to reduce the carrageenan-induced inflammation in rats

Synthesis of some novel phthalazinone, quinazolinone derivatives and screeing antimicrobial activity of selective compounds

4-[1 H-INDOL-3-YL]-1H-2, 3-benzoxazin-1-one [1] aminolysis with some sulfa drugs and 4-amino-acetophenone to give the corresponding sulfonamide and acetyl phenyl derivatives 2a-c and 3, The key intermediate compound 3 condensed with aromatic aldehyde to yield alpha, beta-unsaturated keto compound 4a, b. Compound 1 reacted with sodium azide to give the tetrazol derivative 5. Benzoxazinone derivative 6 was obtained via the interaction of compound 2 with anthranilic acid, which in turn was condensed with hydrazine hydrate, hydroxyl amine hydrochloride/formamide and glutamic acid to yield quinazolinone derivatives 7, 8, 9 and pentandioic acid derivative 10, respectively. Compound 7 reacted with aromatic aldehyde to achieve the Schiff's bases 11a, b, c. Compound [11c] reacted with thioglycolic acid to give thiazole derivative 12. On the other hand, compound 7 reacted with acetic anhdride to give diacetyl derivative 13. Some of the prepared compounds were screened for their antimicrobial activity

Synthesis and antimicrobial activity of some new heterocycles derived from 1-Benzylindole-3-carboxaldehyde

1-BENZYLINDOLE-3-CARBOXALDEYDE [1] reacted with 2- cyanoaceto-hydrazide to give the pyrazoline derivative 3. its reaction with 3-amino-5-pyrazolinone either in acidic or basic medium gave pyrazoline derivatives 10 and 11, respectively. reaction of 3 with phosphorus oxychloride yielded the 5-choloropyrazoline derivative 4 which was heterocylized in the reaction with hydrazine hydrate, phenylhydrazine or thiourea to give the condensed pyrazolopyrazoles 6 and 7 and pyrazolopyrimidine 9, respectively. on the other hand, cyclization of 10 with malononitrile and 11 with arylidenemaio-nonitrile gave the corresponding pyranopyrazole derivatives 12 and 17a,b, respectively. Compound 14 was obtained via the reaction of 12 with benzene-sulphonyl chloride. Moreover, pyrazole 18, 19, pyrimidine 20, 21 and pyridine 22, 23 derivatives were prepared through cyclization of 1-benzyl-3-indolylidene malononitrile 13 with different amino compounds. The newly synthesized compounds 3-17 showed in vitro potent antifungal activity only towards Candida albicans at MIC 20 and 25 micro g compared with the reference drug Nystatin which showed MIC at 0.3 micro g. They showed slight activities towards gram-negative and gram positive bacteria under test

Synthesis of novel 1-[1H-indol-3-yl] phthalazine-4- derivatives with expected antimicrobial activity

Ethyl 2- [1-[1H-indol-3-yl] phthalazin-4- yloxy] acetate [2] condensed with some aromatic amines and hydrazine hydrate to give the corresponding amides [3a-c] and hydrazide [4] derivatives, respectively. The key intermediate compound [4] was subjected to various reactions to yield the oxadiazoles [5] and [10], triazole [7], thiazolidinone [12] and pyrazole [13] derivatives. Also, the key intermediate thiol derivative [14] was subjected to alkylation reaction to give 15,21 and 22 and to acetylation to yield compound [16]. The latter compound condensed with p- anisaldehyde to yield the alpha, beta unsaturated keto compound [17] which in turn was condensed with hydrazine hydrate to yield pyrazoline [18] and with hydroxyl amine to give the isoxazoline [20]. The antimicrobial activity for some representative samples of the new prepared compounds was studied. The data showed that some of the tested compounds possess moderate activity towards G-positive G-negative bacteria and fungi compared with the reference drugs Ampicillin and Mycostatin. Also, the MIC of these compounds showed activity in the range of 125-250 microg/disk Compared with the reference drugs

Blood pressure and echocardiographic measurement of left ventricular mass in children with nephrotic syndrome

Blood pressure and left ventricular mass index were studied in nephrotic children. The study included 40 nephrotic patients [17 were recently diagnosed, 12 with frequent relapse and 11 with persistent proteinuria]. They were recruited from multiple pediatric nephrology clinics. The study also included 17 healthy children of comparable and sex as a control group. For each child; a medical history, complete clinical examination measurements of weight, height, body surface area and blood pressure were done. Besides, routine urinalysis, proteinuria/24 hours, total plasma proteins and albumin, serum cholesterol, blood urea and creatinine were subjected to electrocardiographic detection of left ventricular hypertrophy and echocardiographic measurements of left ventricular mass. High blood pressure was found in 21.4% of recently diagnosed cases prior to initiation of corticosteroid therapy. The percentage was higher among children with frequent relapses [72.4%] and those with persistent proteinuria [100%]. The study found a significant increase in the mean values of weight, body surface area, LVEDD, PWT, IVS, LVM, LVMI and blood pressure between different groups of cases and controls. A significant correlation was observed between LVMI and age, blood pressure and duration of the disease. Multiple regression analysis in cases to predict LVMI showed that duration of the disease is the most important factor. The results showed that echocardiographically measured LVMI is an important early predictor of left ventricular hypotrophy and creating a cut off value based on the 98th percentile of LVMI among children is needed

Assessment of radiotherapeutic management of primary brain tumors by computerized tomography and electroence phalography

The results of radiotherapy treatment were evaluated in 38 patients with primary brain tumors [32 gliomas and 6 meningiomas]. During the period from January 1990 to December 1992, 21 males and 17 females with histologically verified brain tumor were attended and received radiotherapy at Oncology Unit, Radiology Department, Tanta University Hospitals. In glioblastomas multiforme and astrocytomas whole brain irradiation was given using two parallel opposed lateral fields to a total dose of 4000-5000 cGy in 4-5 weeks. Localized irradiation was given to the small volume in a boost dose of 1500 to 2500 cGy in 1.5 to 2.5 weeks. For meningiomas the selection of the small localized field was based on tumor size and histology with a total tumor dose of 5000 cGy to 5500 cGy in 5.5 to 6 weeks. Following radiotherapy patients were examined by both computed tomography [CT] and electroencephalography [EEG] which were compared with pre- and postoperative results. After radiotherapy CT evidence of brain tumor response to treatment was not marked. EEG showed marked changes compared to CT

Comparative analysis of ascaridial parasitic crude antigen by SDS-page and UV absorbance techniques

Ascaridial nematodes are among the well-known parasites infesting fish, birds and mammals. Crude antigen was extracted from Amplicaecum larvae [AL3], Ascaridia galli [adult worm, AG] and Neoascaris vitulorum [adult worm, AV]. The characterization of these parasitic nematodes revealed relative homologous polypeptide chains [MW 25.5 kDa] common to the three parasitic species, whereas the UV absorbance scan mode wave length [WL 200/550 nm] as related to the absorbance [AB] value 0 - 2 recorded an indicative frequency curve. The protein concentration in Amplicaecum, Ascaridia and Neoascaris figured up to 5.47 g%, 4.93 g% and 2.2 g%, respectively