Synthesis, spectral analysis and antibacterial activity of some novel 5- substituted-2-[[6-bromo-3,4-methylenedioxybenzyl]thio]-1,3,4- oxadiazole derivatives

A number of novel 5-substituted-2-[[6-bromo-3,4-methylenedioxybenzyl]thio]-1,3,4-Oxadiazole derivatives [6a-l] have been synthesized to evaluate their antibacterial activity. Using aryl/aralkyl carboxylic acids [1a-l] as precursors, 5-substituted-1,3,4-Oxadiazol-2-thiols [4a-l] were yielded in good amounts.The derivatives, 4a-l, were subjected to electrophilic substitution reaction on stirring with 6-bromo-3,4-methylenedioxybenzyl chloride [5] in DMFto synthesize the required compounds. All the synthesized molecules were well characterized by IR, [1]H-NMR, [13]C-NMR and EIMS spectral data and evaluated for antibacterial activity against some bacterial strains of Gram-bacteria. The molecule, 6d, demonstrated the best activity among all the synthesized molecules exhibiting weak to moderate inhibition potential

Synthesis and antibacterial screening of S-substituted derivatives of 5-[3,4-methylenedioxyphenyl]-1,3,4-oxadiazol-2-thiol

The most emerging class among the heterocyclic compounds is 1,3,4-oxadiazoles for their diverse biological activities. In the present research work, piperonylic acid [1] was converted consecutively into corresponding ester [2], hydrazide [3] and 1,3,4-oxadiazole [4] through intermolecular cyclization. The synthesized compound 4 was subjected further to S-alkylation/aralkylation, using alkyl/aralkyl halides [5a-m] and S-substituted-1,3,4-oxadiazole derivatives were synthesized [6a-m]. The structure elucidation of the synthesized molecules was processed through [1]H-NMR, IR and mass spectral data. The antibacterial activity showed these molecules moderately good inhibitors of gram-negative and gram-positive bacteria

Synthesis, spectral analysis and antibacterial evaluation of N'- substituted-2-[5-[3-chlorophenyl]-1,3,4-Oxadiazol-2- ylthio]acetohydrazide derivatives

The biological potential of N'-substituted-2-[5-[3-chlorophenyl]-1,3,4-Oxadiazol-2-ylthio]acetohydrazide [8ap] has been evaluated against bacterial strains of Gram-negative and Gram-positive bacteria. The multistep synthesis involved the conversion of 3-chlorobenzoic acid [1] to ethyl 3-chlorobenzoate [2], 3-chlorobenzohydrazide [3], 5-[3- chlorophenyl]-1,3,4-Oxadiazol-2-thiol [4], ethyl 2-[5-[3-chlorophenyl]-1,3,4-Oxadiazol-2-ylthio] acetate [5] and 2-[5-[3- chlorophenyl]-1,3,4-Oxadiazol-2-ylthio]acetohydrazide [6]. The last step involved the reaction of 6 and aryl aldehydes, 7a-p, in methanol to synthesize the Schiff bases, 8a-p, with better yields. The structures of all the molecules were corroborated by spectral analysis. The Schiff bases were further evaluated for the antibacterial activity and found to be moderately good inhibitors of bacterial strains of Gram-bacteria

Synthesis and screening of some new N-alkyl/aralkyl-N-[3,4-methylenedioxybenzyl]-4-substituted benzenesulfonamides as potential antibacterial agents

The various p-substituted benzenesulfonyl chlorides [2a-e] were treated with [3,4-methylenedioxy] benzylamine [1] in the presence of aqueous Na2CO3 solution to synthesize N-[3,4-methylenedioxybenzyl]-4-substitutedbenzenesulfonamides [3a-e]. The synthesized molecules were further converted into corresponding Nethyl/benzyl/4-flourobenzyl-N-[3,4-methylenedioxybenzyl]-4-substitutedbenzenesulfonamides [7a-e, 8a-e, 9a-e] on reaction with ethyl iodide [4], benzyl chloride [5] and 4-flourobenzyl chloride [6] in the presence of sodium hydride using N,N-dimethylformamide as solvent. The structure elucidation was processed through different spectral techniques including IR, [1]H-NMR and EIMS. The screening of the synthesized molecules against Gram-bacterial strains, to evaluate antibacterial activity, showed them moderately good inhibitors as shown by their low MIC values

Synthesis, characterization and enzyme inhibition study of O-substituted derivatives of chlorinated coumarin

Coumarins have much importance in dyes, drugs, perfumes and pesticides. In the demonstrated research work, a benignant series of chlorinated coumarins was synthesized and screened against different enzymes. First, 6-Chloro-7-hydroxy-4-methyl-2H-chromen-2-one [3] was geared up by the reaction of 4-chlororesorcinol [1] and ethyl acetoacetate [2] in the presence of concentrated H[2]SO[4]. Second, various O-substituted derivatives of chlorinated coumarins, 5a-j, were set up by pairing different alkyl/aralkyl halides, 4a-j, with 3 in the presence of NaH in DMF as solvent. The structures of all the synthesized compounds were clarified through spectral analysis using EI-MS, IR and [1]H-NMR. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were acetyl cholinesterase [AChE], butyryl cholinesterase [BChE] and lipoxygenase [LOX]. The most proficient activity was shown against both cholinesterase enzymes

Synthesis, spectral characterization and enzyme inhibition studies of different chlorinated sulfonamides

Sulfonamides are adherent to a biologically dynamic category of compounds and are under consideration of many organic synthetic researches to synthesize pharmacologically important compounds. In this demonstrated research work, a benignant series of chlorinated sulfonamides were synthesized and screened against different enzymes. These various chlorinated sulfonamides [3a-i] were set up by pairing of different substituted anilines [2a-i] with 4-chlorobenzenesulfonyl chloride [1] under basic pH in an aqueous media. The structures of the synthesized chlorinated sulfonamides were furnished by [1] H-NMR, IR and EI-MS. The different enzymes used for the evaluation of bioactivity of all the synthesized compounds were urease, butyrylcholinesterase [BChE] and lipoxygenase [LOX]. All the compounds exhibited good inhibitory activities against these enzymes but the strong activity was shown against BChE and hence can be employed for discovery of 'lead' compounds against Alzheimer's disease [AD]

Marsupialization for simple fistula in ano

To compare the post-operative course and the outcome of marsupialized and open wounds in the patients who underwent either fistulotomy or fistulectomy for simple fistula in ano. Comparative study. Department of General Surgery Jinnah Postgraduate Medical Center Karachi, from December 2011 to May 2012. Fifty patients with simple anal fistula were included in this study. They were divided into two groups. Fistulous tracts were managed by using a fistulectomy or fistulotomy alone [group A] while a fistulectomy or fistulotomy with marsupialization was performed in group B. The primary outcome measure was wound healing time while secondary outcome measures were postoperative bleeding, postoperative pain, wound infection, anal incontinence and recurrence. Postoperative wounds in group B healed earlier in comparison to group A wounds [4.85 +/- 1.39 weeks vs. 6.75 +/- 1.83 weeks, p = 0.035]. No significant differences existed between the operating times [28.00 +/- 6.35 minutes vs. 28.20 +/- 6.57 minutes, p = 0.925] and Visual Analogue Scale scores for postoperative pain was 3.3 +/- 1.4 in group A and 3.2 +/- 1.5 in group B. Post operative bleeding was observed for a significantly longer duration in group A than in group B [4.10 +/- 1.91 weeks vs. 2.75 +/- 1.71 weeks, p = 0.035]. No patient developed anal incontinence or recurrence during the follow-up period of twelve weeks. Marsupialization of the wound after either fistulectomy or fistulotomy for simple fistula in ano results in faster healing, less bleeding without lengthening the operative time and without increasing the infection.

comparison of disease caused by Shigella and Campylobacter species: 24 months community based surveillance in 4 slums of Karachi, Pakistan

Despite the efforts of the international community diarrheal diseases still pose a major threat to children in children less than five years of age. Bacterial diarrhea has also emerged as a public health concern due to the proliferation of drug resistant species in many parts of the world. There is a paucity of population-based data about the incidence of shigellosis and Campylobacter infections in Pakistan. We report country specific results for Shigella diarrhea that were derived from a multicenter study conducted in six Asian countries. Disease surveillance was conducted over a 24 month period in urban slums of Karachi, Pakistan, a city with a population of 59,584. Cases were detected through passive detection in study treatment centers. Stool specimens or rectal swabs were collected from all consenting patients. Between January 2002 and December 2003 10,540 enteric infection cases were detected. The incidence rate of treated diarrhea in children under 5 was 488/1000/year. In children, 5 years and older, the diarrhea rate was 22/1000/year. 576 [7%] Campylobacter isolates were detected. The pre-dominant Campylobacter species was C. jenuni with an increase of 29/1000 year in children under 5 years. Shigella species were isolated from 394 of 8032 children under 5 years of age. Shigella flexneri was the dominant species [10/1000/year in children under 5 years] followed by Shigella sonnei [3.9/1000/year], Shigella boydii [2.0/1000/year] and Shigella dysenteriae [1.3/1000/year]. Shigellosis and Campylobacter infection rates peaked during the second year of life. The incidence rate of shigellosis increased in old age but such a trend was not observed in Campylobacter infections. Of 394 shigellosis patients 123 [31%] presented with dysentery in contrast to only 54 [9%] of 576 patients with Campylobacter infections [p < 0.001]. Both Campylobacter infections and shigellosis are common in community settings of Pakistan but shigellosis presented more frequently with abdominal pain and dysentery than Campylobacter infections indicating that shigellosis may be a more severe illness than Campylobacter infections. Due to the increased and disease severity, drug resistant shigella have become a significant health problem; moreover it is a disease of poor and impoverished people who do not have the access to standard water and sanitary conditions, health care services or optimal treatment. In the face of these facts it is empirically important to develop a low cost effective vaccine that can protect these populations for a longer duration

Evaluation of quality and patient satisfaction during endoscopic procedure: a cross sectional study from South Asian country

To assess the quality of gastrointestinal [Gl] endoscopic procedures and patient satisfaction in endoscopy suite of South Asian country. Patients coming to the endoscopic suite of Aga Khan University Hospital [AKUH] were interviewed and assessed in this cross-sectional study. Quality of Gl endoscopic procedures was evaluated using assessment tools as suggested by The American Society of Gastroenterology. Patient satisfaction after the procedure was assessed using a modified GHAA-9 questionnaire. The questionnaire was statistically evaluated using Pareto analysis and Spearman rank correlation. In this study, 323 patients were evaluated with a mean age of 43 +/- 14.36 years. Out of all the procedures 251 [77.7%] were gastroscopies while 72[22.3%] were colonbscopies. Patients undergoing different therapeautic procedures were 121 in number [37.46%]. Pre-procedure education was rated as excellent or very good by 91.3% of the patients. Midazolam was used for sedation with an average dose of 3 mg. Technically successful procedures included 99.2% gastroscopies and 98.6% colonoscopies. Mean score of patients regarding satisfaction on mGHAA-9 questionnaire was 30 +/- 3.965. Patient dissatisfaction calculated In our study was 3.6% with the length of time spent waiting before procedure and length of time waiting to get an appointment for the procedure contributing to 90% of dissatisfaction. Quality of endoscopic procedures at our centre is at par with international standards with acceptable complication rate and good patient satisfaction

phase II study of gemcitabine concurrent with radiation in locally advanced squamous cell carcinoma of head and neck: a trial of the cancer research group Pakistan

To evaluate the efficacy and toxicity of weekly gemcitabine as a radiosensitizer concurrent with radical radiotherapy in locally advanced carcinoma of head and neck. From August 2001 to January 2002, thirty-nine patients with stage III or IV B inoperable carcinoma of head and neck were enrolled. Patients with histopathologically confirmed squamous cell carcinoma with at least one bidimensionally measurable lesion, no prior chemotherapy or radiotherapy, and a KPS of 60 or above were included. Patients with nasopharyngeal, glottic or sub-glottic cancer were excluded. Gemcitabine 150mg/m2 or a total dose not exceeding 200 mg was given on day 1, 8, 15, 22, 29, and 36 during radiation treatment. Radiation was delivered with conventional fractionation to a total dose of 66-70Gy. Miller's criteria was used for response evaluation. RTOG/EORTC acute radiation [and chemotherapy] morbidity scoring system and WHO grading of acute and sub acute toxicity criteria were used for documentation of toxicity. All 39 patients were evaluable for toxicity but only 35 patients were evaluable for response. An overall response rate of 94.3% [95% CI; 80.8-99.3] was seen with a partial response rate of 71.4% and complete response rate of 22.9% [95%CI; 10.4-40.1]. Grade 3 mucositis was seen in 28 patients [71.8%]. Grade 4 mucositis was seen in 2 patients [5.1%]. Pharyngeal toxicity was the second-most common toxicity. Grade 2 toxicity was seen in 12 patients [30.8%] and grade 3 in 6 patients [15.4%]. Despite vigorous symptomatic and supportive care acute toxicities led to treatment interruption in 40% of patients. A high overall response rate and a high rate of acute toxicity are seen at a weekly gemcitabine dose of 150mg/m2 concurrent with radiation. This shows that gemcitabine is a potent radiosensitizer with a marked tumor and normal tissue radio sensitization

Presentation, management and outcome of mastalgia

To find out the causes of mastalgia in females of various age groups, its management and outcome. Descriptive study. The study was carried out in the breast clinic of Surgical Unit-I, Ward-3 of Jinnah Postgraduate Medical Centre, Karachi. From January 2001 to December 2001. The study included 100 consecutive patients diagnosed as a case of mastalgia on the basis of history and clinical examination. Out of 100 patients, 56 presented with cyclical mastalgia, 28 non-cyclical mastalgia, 13 associated withfibroadenoma and 3 had carcinoma. Cyclical mastalgia is commonest in pre-menopausal women whereas noncyclical mastalgia is common in post-menopausal women. Reassurance and good analgesia can cure more than 50% of patients presenting with mastalgia. Almost all patients of cyclical mastalgia were cured by evening primrose oil. Some of the cases may have other associated lesions which must be excluded carefully