Conventional versus microwave assisted synthesis, molecular docking and enzyme inhibitory activities of new 3,4,5-trisubstituted-1,2,4- triazole analogues

N-[Substituted]-5-[1-[4-methoxyphenylsulfonyl]piperidin-4-yl]-4H-1,2,4-triazol-3-ylthio] acetamide were synthesized by following conventional as well as microwave assisted protocol through five consecutive steps under theimpact of various reaction conditions to control the reaction time and the yield of product. Starting from 4- methoxybenzenesulfonyl chloride and ethyl isonipecotate, product 3 was obtained which was converted into product 4by treating with hydrazine hydrate. In step 3, the product 4 was refluxed with methyl isothiocyanate and KOH to yield compound 5 which was finally treated with variety of N-substituted acetamides to yield an array of different new compounds [8a-k]. These synthesized compounds were evaluated for their inhibition potential against bovine carbonic anhydrase [bCA-II], acetylcholinesterase [AChE] and butyrylcholinesterase [BChE] enzymes. Compound 8g demonstrated good activity against bCA-II, AChE and BChE with IC50 values of 8.69 +/- 0.38 MuM, 11.87+/-0.19 MuM and 26.01+/-0.55 MuM respectively. SAR studies assisted with molecular docking were carried out to explore the mode of binding of the compounds against the studied enzymes

Synthesis of 2-[[5-phenyl-1,3,4-Oxadiazol-2-yl]sulfanyl]-N-substituted acetamides as potential antimicrobial and hemolytic agents

A new series of N-substituted derivatives of 2-[[5-phenyl-1,3,4-Oxadiazol-2-yl]sulfanyl] acetamides was synthesized. The synthesis was carried out by converting benzoic acid [1] into ethyl benzoate [2], benzohydrazide [3] and then 5-pheny-1,3,4-Oxadiazol-2-thiol [4] step by st0ep. The target compounds 6a-p were synthesized by reaction of compound 4 with equimolar ratios of different N-alkyl/aryl substituted 2-bromoacetamide [5a-p] in the presence of DMF and sodium hydride [NaH]. The spectral [EI-MS, IR, 1H-NMR] characterization of all the synthesized compounds reveal their successful synthesis. The compounds were also screened for antimicrobial and hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. But 6h was the most active against the selected panel of microbes. This series showed less toxicity and may be considered for further biological screening and application trial except 6m, possessing higher cytotoxicity

Frequency of hydrocephalus in myelomeningocele patients in a tertiary care hospital

Background: Myelomeningocele is most complex form of spin a bifida and most of the times, it is associated with hydrocephalus

Objective: To find the frequency of hydrocephalus in Myelomeningocele patients

Methodology: Study design: Cross sectional Study. Setting: Department of Neurosurgery, Sheikh Zayed Hospital, Rahim Yar Khan. Study duration: From 1[st] January 2012 to 31[st] December 2013. Study subjects: 52 patients of Myelomeningocele were included in our study and were assessed for different variables like age, sex, site of lesion, presence of hydrocephalus and status of lower limbs [power, sensation and sphincter control]. The data was entered and analyzed by using SPSS version 15

Results: 34 patients [65.38%] were male and 18 patients [34.61%] were female and common site of lesion was lumbar region [48%] followed by thoracolumbar region [42%]. The power of legs was G0-G2 in majority of patients [90%]. 40 patients [76%] had hydrocephalus detected by CT Scan brain

Conclusion: Our study suggests it is better to put VPShunt before going for treatment of Myelomeningocele, as majority of the patients of myelomeningocele have hydrocephalus

Result of surgical decompression and internal fixation with titanium cage in patients with carries spine

The objective of the study is to assess, the postoperative outcome of the intervertebral titanium cage, in patients operated for Caries spine with unstable spine with/without neurological deficits. This is a retrospective study, carried out in department of Neurosurgery Sheikh Zayed Hospital, Rahim Yar Khan, during 2 years, from January 2006 to December 2007. All patients underwent a neurological and radiological assessment. Those patients who had collapse of vertebral body/s, with/without gibbus formation having some neurological deficit were included. Patients fit for surgery, were operated upon, with placement of intervertebral adjustable titanium cage. These patients were followed up for eighteen months. The study comprised of 11 patients, with their age ranging from 20 to 53 years having 7 males and 4 females. The patients were admitted through OPD or the emergency department in neurosurgical ward of Sheikh Zayed hospital, Rahim Yar Khan. The majority of the patients had D10-11 lesion [36.3%] followed by L2 in 18.1%. The neurological status of the patients received showed paraplegia in 27.27% while paraparesis in 72.72% of patients. The neurological outcome of 11 patients, after eighteen months of follow up, showed marked improvement in 72.72% patients of incomplete spinal cord compression [paraparesis]. While some improvement in 27.27% patients of complete spinal cord damage [paraplegia]. All patients with kyphotic lesions had near normalization of the anatomical curve of the spine. All patients were kept on antituberculous chemotherapy for one year. Our experience with usage of the titanium cage for internal fixation in Caries spine showed very promising results, especially in patients of paraperesis with/without gibbus formation. This technique may become a main stay of surgical management in Caries spine for thoracolumber region in our setup

study of complications seen in 300 cases of ventriculo peritoneal shunts managed at Sheikh Zayed Hospital, Rahim Yar Khan

The objective of the study is to assess, the postoperative complications of 300 hydrocephalic patients, operated with ventriculo peritoneal shunting system. This is a retrospective study, carried out in the department of Neurosurgery Sheikh Zayed Hospital, Rahim Yar Khan. 300 patients including both adults [20.3%] and children [79.6%] with various causes of hydrocephalus were operated upon. All patients underwent a neurological and radiological assessment, and all those patients who had clinical and radiological evidence of hydrocephalus and were fit for surgery, were operated. All patients underwent a ventriculo peritoneal shunt placement. The follow up of the patients was for six months and all the complications were noted and dealt with. The common cause of hydrocephalus seen in children was Aequeductal stenosis, followed by post meningitis hydrocephalus, whereas in adults, trauma and tumours were responsible for the disease. Most common complication seen in our study was shunt blockade [33%] followed by wound infection and meningitis [23%].The study was to identify complication rate of ventriculoperitoneal shunt in our setup. Inspite of low socioeconomic setup and poor hygiene our results are still comparable to some foreign studies