Synthesis, characterization and SAR of novel bezimidazole derivatives as nematicidal agents

Six novel analogues were prepared by reacting benzimidazole molecules [BM and CMB] propiophenone andbenzoyl chlorides respectively. The structures of newly synthesized compounds were determined with the help of spectroscopic techniques. The compounds were subjected to in-vitro screening for their activity against nematodes. It was observed that the benzimidazole [BM] derivatives possessed more nematicidal activity as compared to that of cyanomethyl-benzimidazole [CMB] for Meloidogyne incognita. Among them, the propiophenone substituted benzimidazole derivative B3 was found to be the most active compound and can be further studied as lead molecule for development of anthelmintic drugs

Cytotoxic and acute toxicity studies of isoniazid derivatives

Cancer is ultimately the result of cells that hysterically grow and do not die. Cells can experience uncontrolled growth if there are mutations to DNA, and therefore, alterations to the genes involved in cell division. Cancer occurs when a cell's gene mutations make the cell unable to correct DNA damage and is unable to destroy itself. There are over 100 different types of cancer each classified by the type of initially affected cell. Isoniazid, a well-known antitubercular agent has been reported to exhibit some cytotoxic activity. This finding prompt us to carry out this study where isoniazid and its sixteen derivatives were studied for any possible cytotoxic activity against Human astrocytoma SNB-19 cells, human Dukes' type C colorectal adenocarcinoma HCT-15 cells, human Dukes' type D colorectal adenocarcinoma COLO-205 cells, and human prostate adenocarcinoma [grade IV] PC-3 cells. Among the test compounds, SN-07 [a phenacyl derivative with para phenyl substitution] demonstrated slight cytotoxic effects on two types of human colorectal adenocarcinoma cells HCT-15 and COLO-205. Moreover, the acute toxicity of the compounds was also estimated in which some compounds were evaluated with more LD[50] values than isoniazid

Analgesic activity of alkyl piperidine derivatives

Piperidine is the most significant scaffold which reveals therapeutic potential because of its conformationally flexible nature. During the course of present investigations synthetic quaternary salts of alkyl piperidine with various phenacyl bromides were explored for their possible analgesic activity. Compounds I analogs [1a-1f] and compound II analogs [IIa-IIf] showed varying degree of analgesic activity when compared with pethidine as standard and its duration by tail immersion method

Antimicrobial and antioxidant screening of N'-substituted sulphonyl and benzoyl derivatives of 4-Pyridine carboxylic acid hydrazide

In this research program, the antibacterial, antifungal and antioxidant activities of six N_-substituted sulfonyl and benzoyl derivatives of lead molecule PCH were reported. Out of these compounds, sulphonyl derivatives 2,3 and benzoyl derivative 5 showed moderate to good activity against different strains of gram-positive and gram-negative bacteria including B. cereus, B. subtilis, B. thruingiensis and S. pyogenes, S. fecalis and E. coli ATCC 8739. Moreover, upon antifungal screening, the compound, N?-[[2,4,6-trimethylbenzene] sulfonyl]pyridine-4-carbohydrazide possessed good antifungal activity against Candida species, a causative agent of systemic fungal infections. Antioxidant study demonstrated more than 50% inhibition in DPPH assay for sulphonyl derivative 2 indicating its potential as antioxidant while the other derivatives expressed low level of radical scavenging property

Cervical screening: do gynecologists themselves practice what they preach? a study based in tertiary care hospitals of Lahore

To determine the frequency of self-compliance to cervical screening guidance among the sexually active female gynecologists in tertiary care hospitals. To identify the possible barriers to effective screening in those who do not undergo cervical screening. Cross sectional study. This study was conducted in the obstetrics and Gynecology department of various tertiary care hospitals of Lahore from 1[st] Jun 2012 to 30[th] Nov 2012. Total 157 female gynecologists, serving in various positions in tertiary care hospitals of Lahore were interviewed by using a structured self reporting performa. The performa was designed to find out the number of gynecologists undergoing pap screening, and in those who fail to undergo screening the single most important barrier presumed to be preventing them from undergoing screening was also evaluated. In this study, only 3.1% of the subject population was found to be undergoing pap-screening, which reflects the national level of screening in urban areas,in sharp constrast to the studies being conducted in developed countries, with screening coverage rates of more than 80%. The prevalence of pap screening in the subject population is disappointingly low and drastic steps are needed to bring about a change in attitude of the subject population which cannot be brought about without changing the current culture of self-negligence and least prioritization for self, in the feminine part of our society

Impact assessment of educational intervention among private dental practitioners about infection control practices in district Peshawar

Cross infections occur frequently in dental health care personnel therefore, to protect themselves and their patients; they have to strictly follow infection control practices. To assess the impact of educational interventions on knowledge and practices of private dental practitioners. Interventional study, done from March 2012 to June 2013 in private practitioners of Peshawar using convenient sampling technique. After acquiring base line data on the practices, pertaining to prevention of cross infection in dental practitioners, educational knowledge intervention was applied to them on same day and repeated after two months. Post intervention data was collected using same questionnaire. The data was analyzed using Statistical Package for Social Sciences [SPSS] version 16.0. A total of 90 dental practitioners were included, of whom 49 [54.4%] were qualified and 41 [45.6%] unqualified. Their overall mean age was 33.77 +/- 8.97 years. The mean age of qualified practitioners was 36.24 +/- 10.40 years. Their pre and post intervention practices showed significant improvement in various practices like; screening of patients prior to procedure [p <0.043], hepatitis B vaccination [p < 0.000], type of gloves used [p < 0.031], hand washing [P < 0.004] separate instrument processing area [p < 0.004], floor cleansing with disinfectant [p < 0.000] and proper ventilation [p <0.021]. The mean age of unqualified practitioners was 30.80 +/- 5.73 years. Their pre and post intervention change in knowledge and practices showed poor compliance to most interventions. Qualified dental practitioners had a positive attitude towards educational infection as compared to unqualified practitioners. Yearly health education certification should be implemented for all health care professional [qualified and unqualified] to keep them abreast with the infection control practices

Synthesis of novel derivatives of 4-Pyridine carboxylic acid hydrazide and their activity on central nervous system

Six novel derivatives [2-7] of 4-Pyridine carboxylic acid hydrazide [PCH] were synthesized by treating this lead molecule with substituted arylsulphonyl and benzoyl chlorides

The molecular structures of the newly derived products were characterized by the help of UV Visible, IR, FAB, 1HNMR spectroscopy and CHN analysis

During the preliminary pharmacological screening, it was observed that the synthesized compounds induced noticeable changes on motor activity of the animals

Interesting structure activity relationship was also observed among the synthesized molecules. Because of the interesting affect on motor activity, the newly synthesized derivatives can further be evaluated for their effects on CNS

Determination of pKa values of new phenacyl-piperidine derivatives by potentiometric titration method in aqueous medium at room temperature [25 +/- 0.5[degree sign]C]

Dissociation constant [pKa] of ten novel phenacyl derivatives of piperidine were determined by potentiometric titration method in aqueous medium at room temperature [25 +/- 0.5oC]. The sample solutions were prepared in deionized water with ionic strength 0.01M and titrated with 0.1M NaOH solution. In addition, DELTAG values were also calculated. Different prediction software programs were used to calculate pKa values too and compared to the experimentally observed pKa values. The experimental and theoretical values were found in close agreement. The results obtained in this research would help to predict the good absorption of the studied compounds and can be selected as lead molecules for the synthesis of CNS active agents because of their lipophilic nature especially compound VII

Subfertility: the tragedy of military life style

To determine the frequency of subfertility in military couples owing to military deployments and consequent physical separation of couples. Cross-sectional descriptive study. This study was conducted in the department of Obstetrics and Gynecology at CMH Lahore from Jan 2012 to Jun 2012. Total 232 couples being investigated for subfertility were interviewed for the period of living together at a stretch since their marriage. The couples with established male factor infertility, secondary subfertility, and abdomino-pelvic surgery in female partners were excluded to rule out known pathological conditions as an underlying cause. Data was analyzed using MS excel in the form of frequencies, percentages and presented in the form of tables and figures. In our study 232 couples had subfertility. Out of these 96% of the couples could not spend their first year of marital life together due to non-availability of married accommodation. Nearly 50% of the patients looked for other forms of help including household tips, medicines and spiritual help before seeking medical treatment. In 69% of the couples burden of blame was put on the female partner by the in-laws. The tragedy of subfertility was further compounded by the fact that psychological symptoms were admitted by more than 70% females, 44% confessed being a victim of domestic violence, and 54% husbands refused to have their semen analysis done on first request by clinicians, although after counselling only 13% of the husbands still could not make their semen analysis available either due to military deployments or personal reasons. Incidence of subfertility in military couples is alarmingly high and can be largely attributed to military deployments and lifestyle

Synthesis and cytotoxic activity of some derivatives of alkyl piperidine

Synthesis of novel phenacyl derivatives of alkyl piperidine as cytotoxic agents via simple and single step reaction procedure is going to be reported here. Twelve new compounds were successfully synthesized in moderate yield and in solid form. Their synthesis was confirmed by TLC, melting point, CHN analysis and through different spectral studies such as UV, IR, Mass and proton NMR. The advantages of this synthetic route are simple operation, mild reaction conditions and good yields. These newly synthesized derivatives were extensively explored for their cytotoxicity by brine shrimp lethality assay

Behavioral and neurochemical profile of some novel phenacyl based isonipecotamide derivatives

Study of natural products led to the development of new molecules of potential biological activity. Piperidine nucleus constitutes one of the components of various alkaloids and drugs. During the course of our project regarding the synthesis of derivatives of piperidine carboxamide to study the effects of these compounds as anti-depressive agents, some of the compounds exhibited significant effects at all three doses, through open field activity thus establishing a direct relationship between dose and locomotion. Moreover, these compounds have also shown the decreased level of 5-HT alone with increased level of dopamine as an indication of their antagonism towards 5-HT receptor

Problems faced by lady health workers [LHWs] in Punjab province

Objective: to assess the problems faced by Lady Health Workers in Punjab province

Material and Methods: this cross-sectional study was conducted in 9 union councils of Punjab province. All 111 Lady Health Workers working in these nine union councils were included in the study and were interviewed on a structured questionnaire

Results: ninety two percent of the LHWs faced problems while providing services. Ninety five percent had salary related problems, seventy four percent had problems with supplies, and thirty two percent faced problems in community services, 44.1 % had difficulties with health facility liaison, 56.7% faced problems due to workload, 44.1 % had problems in traveling, 8.8% in supervision, 20.6% in monitoring, 9.8% in reporting, 29.4% in feedback, 36.3% in security; 14.7% faced problems due to harassment, 18.6% due to training deficiency and 32.4 % faced other problems

Conclusion: efforts must be focused to strengthen the program and increase the LHWs capacity as efficient health care workers by involvement of LHWs' own views and addressing the problems faced by them

Scurvy as a predisposing factor in gingival disease - a case report

Scurvy is a vitamin C deficiency disease which mainly occurs in teenagers. Vitamin C plays a vital role in the synthesis of collagen, the deficiency of which leads to a widespread pathology of supporting tissues of blood vessels, bone and teeth. There is an increased permeability of the capillaries to red blood cells causing hemorrhage. The bone becomes friable at the growing end. There is interference with timely collagen formation which causes delayed wound healing. In addition to other symptoms, there are bleeding gums, loose teeth plus swollen and stiff joints. A case report of a 13 years old girl is presented with gingival swelling and bleeding since last 4 years. The case was thoroughly investigated, oral prophylaxis along with vitamin C was prescribed and the patient became normal within one week time

Synthesis of some novel analogues of 4-[l-pyrrolidinyl] piperidine and their effect on plasma glucose level

In the present study some compounds of 4-[1-Pyrrolidinyl] Piperidine [I] have been synthesized. Structures of compounds were confirmed by using HNMR, IR, Mass and UV spectrophotometer techniques. All the derivatives [II, III, IV and V] and the parent compound [I] at the dose of 100 mg/kg were evaluated for their effect on plasma glucose level. Compound [II] was the only derivative which showed effect on plasma glucose level

Synthesis and evaluation of novel phenacyl based carboxamide derivatives of piperidine as antihypertensive agents

The research in the field of piperidine has generally been related to the synthesis of useful medicinal drugs. In view of the pharmacological and medicinal importance of piperidine derivatives in different disciplines of medicines the present study has been carried out. A series of newly synthesized N-substituted phenacyl piperidine derivatives [II-VII and XIII-XIV] has been evaluated for hypotensive activity in normotensive anesthetized rats at the doses of 0.5 micro g/kg taking acetylcholine and noradrenaline [1 micro g/kg] as control. Mean arterial blood pressure and heart rate were compared to its respective control values obtained immediately before the administration of test compounds and expressed as percent change. The compounds II, III and XIV showed mild hypertensive activity while compound V, VII and XIII were found inactive at that dose level. However, compound IV showed more hypotensive effect than the starting molecule [I]. None of these derivatives affected the heart rate at the same dose. It was also revealed that the carboxamide group has no considerable effects on arterial blood pressure and plays no important role in the increase or decrease of blood pressure

Neurochemical estimations of some new quaternary phenacyl- bromopiperidinium compounds

Considering the fact that N-alkyl substituted quaternary ammonium salts of piperidinium bromide induce brain catecholamine and indoleamine metabolism, we thought it may he valuable to investigate the effects of three selected phenacyl derivatives [I, V and VIII] of piperidine on brain monoamines metabolism in mice [100mg/kg body weight] assuming that these derivatives might alter the brain indoleamine and catecholamine levels differently. Studies are carried out by using HPLC technique. It was found that compound VIII possessed greater neuroleptic activity as compared to compounds I and V

Antibacterial activity of 1-methyl-7-methoxy-B-carboline and its phenacyl and coumarine analogues

Antibacterial activity of 1-methyl-7-methoxy-pound]-carboline [harmaline] and its phenacyl and coumarine analogues 1-[3-nitro-phenyl]-[2-[7-Methoxy-1-methyl-1,3,4,9-tetrahydro-pound]-carbolin-2-yl]-ethanone[II], 1-[3,4-Dihydroxy-phe-nyl]-2-[7-methoxy-1-methyl-1,3,4,9-tetrahydro-pound]-carbolin-2-yl]-ethanone[III] 7-[methoxy-pound]-carboline],15-24, de-hydro[19,20-dimethoxy]coumarine [IV], 7-[methoxy-pound]-carboline]15-24,dehydro[20-methoxy]coumarine [V] were studied by disc diffusion method. All compounds were tested against three Gram positive and four Gram-negative bacteria. Parent compound showed good activity. All compounds revealed better results against Gram positive as compared to Gram-negative bacteria. 1-[3,4-dihydroxy-phenyl]-2-[7-methoxy-1-methyl-1,3,4,9-tetrahydro-pound]-carbolin-2-yl]-ethanone [III] was found most potent compound showing broad spectrum activity when compared with all synthesized analogues. Coumarine analogues showed more or less same activity indicating that number and position of methoxy groups are not important regarding antimicrobial activity

Effect of diazepam on the CNS excitation and behavioural changes induced by harmdline and its newly synthesized analogues

The neuropharmacologic profile of harmala alkaloids has been studied and found to have central effects like convulsions, catalepsy, or altered startle response. In number of studies the effects of diazepam, on harmaline and other beta carboline containing compounds-induced tremors were investigated. The present study was undertaken to examine the effect of diazepam on pretreated animals with harmaline and its synthesized phenacyl and coumarine analogues. Diazepam successfully inhibited the tremor and convulsions and attenuated the other behavioural response produced by Harmaline and its derivatives

Economic and dietary relation to dental caries incidence in rural and urban school girls, Peshawar district

Investigation of economic and dietary relation to dental caries incidence in 200, 12-14 years old rural and urban school girls s was carried out in Peshawar District during November, 1988-89. The girls belonged to low and lower middle income families. The results have shown that all the subjects under study, both from rural and urban areas, had dental caries [Mean 9.13 +/- 2.35], with various degrees of severity. For girls from the rural area, dental caries indices ranged 5.49 +/- 1.88 - 8.66 +/- 1.87 and for girls from the urban area, the range was 9.89 +/- 1.62 - 13.18 +/- 2.59. The dental caries indices [mean: 11.11 +/- 2.60] in urban school girls was significantly [P < 0.05] higher than the rural school girls [mean: 7.16 +/- 2.10] in each income group which shows that income variable, is not an independent indicator but is accompanied by other factors which influences dental caries incidence and severity. The subjects who consumed milk and milk products, fresh fruits and vegetables regularly, had lower dental caries indices than those who did not. The reverse was found in the subjects who consumed bakery/refined carbohydrates and high sugar content foods. The subjects who consumed bakery products at breakfast and between meals more frequently, had higher dental caries indices than those who took sugar rich foods

Acute necrotizing ulcerative gingivitis in Peshawar [NWFP] Pakistan

This study analyze 54 cases of acute necrotizing ulcerative gingivitis among 4446 patients who were treated at the periodontal department of oral and dental hospital of Khyber College of Dentistry, Peshawar over two years period. There was not a single case of cancrum oris either in adults or in children. The peak occurrence of ANUG was among 8-9 years old children and 76% of them were in the 5-12 years age range. Recent febrile illness was present in 17 cases out of 54. Other predisposing factors which are discussed were poor hygiene, low socio-economic factors and malnutrition. Good oral hygiene, proper medical care, and adequate nutrition are recommended for the risky children