The chemistry of life has been extensively and effectively elaborated by organic chemists. No doubt, all the fields of science are struggling for the benefit of human beings and the chemists are well known in this regard. The organic or medicinal chemists are the main worker of improving the health. A number of compounds have been synthesized in search of new drug candidates by the orgnic chemists and also they have been successful up to much extent in this regard. The importance of this process can be realized from the increasing inactivity of the running drugs against different diseases. Hence the synthesis of new molecules in search of new drug candidates against different diseases is an ever green process. This was the motivating aspect of the literature survey of synthetic chemistry which encouraged us to design new molecules and evaluate their biological potential. The bioactivity potential of some heterocyclic moieties (as discussed in introduction and review of literature) prompted has to design such type of molecules which bear more than one heterocyclic moieties. These considered heterocyclic moieties included piperidine and 1,2,4-triazole. The aim of submerging different heterocyclic functionalities into one core was to boost up their bioactivity potential. Furthermore, the variation in some part of final molecules was also processed in order to acquire new potent drug candidates. The pharmacological evaluation included enzyme inhibition, antioxidant activity and bovine serum albumin (BSA) binding analysis. The enzyme inhibition results were further substantiated through molecular docking analysis. The presented research work has been distributed into eight solid schemes for the synthesis of ninety six compounds. Ethyl isonipecotate (2) was treated with 4methoxybenzene sulfonyl chloride (1) in 5% sodium carbonate at pH of 9-10 to get ethyl-1-[(4-methoxyphenyl)sulfonyl]piperidine-4-carboxylate (3). Compound 3 and hydrazine monohydrate were refluxed in methanol to acquire 1-[(4methoxyphenyl)sulfonyl]piperidine-4-carbohydrazide (4). Compound 4 was refluxed with phenyl isothiocyanate in methanol to acquire an intermediate compound (2-({1[(4-methoxyphenyl)sulfonyl]-4-piperidinyl}carbonyl)-N-phenyl-1-hydrazinecarbothio amide) which was refluxed in basic medium to get 5-{1-[(4-methoxyphenyl)sulfonyl]4-piperidinyl}-4-phenyl-4H-1,2,4-triazole-3-thiol (5). Compound 5 was stirred with xiii different aralkyl halides (6a-j) in the presence of NaH and DMF using conventional and microwave assisted methods. 3-Aralkylthio-5-{1-[(4-methoxyphenyl)sulfonyl]-4piperidinyl}-4-phenyl-4H-1,2,4-triazole (7a-j) were obtained through filtration from aqueous medium. The compound 5 was treated with equimolar N-substituted-2bromoacetamides (10a-t) to acquire N-alkyl/aralkyl/aryl/phenyl-2-[(5-{1-[(4methoxyphenyl) sulfonyl]-4-piperidinyl}-4-phenyl-4H-1,2,4-triazol-3-yl)sulfanyl] acetamide (11a-t). The electrophiles, 10a-t, were synthesized by the reaction of alkyl/aralkyl/aryl/phenyl amines (8a-t) and bromoacetyl bromide (9) in 5% sodium carbonate solution. The compound 5 was treated with equimolar N-substituted-2bromopropanamides (13a-r) to acquire N-alkyl/aralkyl/aryl/phenyl-2-[(5-{1-[(4methoxyphenyl) sulfonyl]-4-piperidinyl}-4-phenyl-4H-1,2,4-triazol-3-yl)sulfanyl] propanamide (14a-r). The electrophiles, 13a-r, were synthesized by the reaction of alkyl/aralkyl/aryl/phenyl amines (8a-i, k, m-t) and 2-bromopropionyl bromide (12) in 5% sodium carbonate solution. Compound 4 was refluxed with methyl isothiocyanate in methanol to acquire an intermediate compound (2-({1-[(4-methoxyphenyl) sulfonyl]-4-piperidinyl}carbonyl)-N-methyl-1-hydrazinecarbothioamide) which was refluxed in basic medium to get 5-{1-[(4-methoxyphenyl)sulfonyl]-4-piperidinyl}-4methyl-4H-1,2,4-triazole-3-thiol (15). Compound 15 was stirred with different aralkyl halides (6a-j) in the presence of NaH and DMF using conventional and microwave assisted methods. 3-Aralkylthio-5-{1-[(4-methoxyphenyl)sulfonyl]-4-piperidinyl}-4methyl-4H-1,2,4-triazole (16a-j) were obtained through filtration from aqueous medium. The compound 15 was treated with equimolar N-substituted-2bromoacetamides (10a-t) to acquire N-alkyl/aralkyl/aryl/phenyl-2-[(5-{1-[(4methoxyphenyl) sulfonyl]-4-piperidinyl}-4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl] acetamide (17a-t). The compound 15 was treated with equimolar N-substituted-2bromopropanamides (13a-r) to acquire N-alkyl/aralkyl/aryl/phenyl-2-[(5-{1-[(4methoxyphenyl) sulfonyl]-4-piperidinyl}-4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl] propanamide (18a-r). The synthesized compounds were initially verified through TLC and stored for further analysis. The synthesized compounds were spectroscopically characterized by using IR, 1H-NMR, 13C-NMR, HMQC, HMBC, COSY, NOESY and EIMS spectral information to justify the available main functional groups, hydrogen atoms, carbon atoms and the fragmentation pattern of the structures of synthesized compounds. xiv The synthesized compounds were screened for enzyme inhibition activity against six different enzymes and also for antioxidant activity. The different six enzymes included acetyl cholinesterase (AChE), butyryl cholinesterase (BChE), αglucosidase, urease, lipoxygenase and carbonic anhydrase II enzyme. Almost all the compounds were found to be excellent active agents against these enzymes. Antioxidant activityof all the synthesized molecules wasalso tested in search of some unique drug candidates. The chemistry of active sites and different functionalities responsible for the best pharmacological potential of all the synthesized compounds was verified through docking studies. In addition to it, the evaluation of protein drug interaction assisted us in understanding the various binding sites and binding constant to justify the stay of the drugs in the body, their circulation, metabolism, elimination and pharmacodynamics. The sketched compounds in the eight schemes were synthesized efficiently with high yield and purity through environment friendly protocol with minimum cost and time. The time of synthesis and the yield were compared for two modes of synthetic methods including conventional and microwave assisted ones. The following synthetic as well as biological screening studies resulted into the identification of a numberof compoundsbeing active against the considered enzymes. These enzymes are responsible for different kind of diseases and so the bioactive potent compounds may be considered as new drug candidates for the concerned diseases.
ظاہری طور پر یہودیوں کے پاس ایسا کوئی خاص نظام یا قاعدہ موجود نہیں ہے جس کی رو سے یہ کہا جا سکے کہ وہ کن مخصوص عقائد کی پیروی کرتے ہیں۔ الہامی مذاہب میں خدا پر ایمان لانا ایک بنیادی عقیدہ ہے تاہم "ملحد یہودی" جیسے تصور نے اس عقیدے کو بھی متاثر کیا ہے۔ یہودی خود بھی اس معاملے میں اختلاف کا شکار ہیں کہ کیا رسمی عقیدے جیسی کوئی چیز مذہب میں موجود بھی ہے یا نہیں؟ اس معاملے میں ایک فریق یہ کہتا ہے کہ یہودیت میں عقائد جیسی کوئی چیز نہیں؛ صنہادرین تک نے ایسی کوئی وضاحت پیش نہیں کی جس کی رو سے یہودیت کے بنیادی عقائد کی فہرست مرتب کی جا سکے۔ موسی ابن میمون نے بھی جو تیرہ اساسی اصول مرتب کیے ہیں ان کو تمام یہودی قبول نہیں کرتے۔ اکثر و بیشتر راسخ العقیدہ یہودی ان پر اعتراضات اٹھاتے رہتے ہیں۔ بعض یہ خیال کرتے ہیں کہ وہ اپنے عقائد کی کوئی فہرست مہیا نہیں کر سکتے کیونکہ ان میں عقائد کے معاملات میں کبھی اتفاق رائے نہیں ہو سکا ہے۔ یہاں تک کہ عبرانی بائیبل کے فراہم کردہ مذہب کو بھی وہ متنوع سمجھتے ہیں۔[1] جو فریق یہ سمجھتا ہے کہ یہودیت میں کچھ بنیادی عقائد موجود ہیں وہ یہ دلیل دیتا ہے کہ اگر یہ مان لیا جائے کہ یہودیت میں عقائد کا وجود ہی نہیں...
Democracy in Nigeria is characterised by corruption, irregularities and injustice. The level of political hostility in the country has resulted in loss of lives and properties and as a result, there have been hindrances to peace and national development to prevail in Nigeria. Hence, the ugly political developments have generated a lot of concerns and questions such as what are the causes of the political unrest in Nigeria? Is democracy really paying off as a political system in Nigeria? What has been the result of democracy in Nigeria? Can there be a better political system in Nigeria? If so, can Islamic political system fulfil the longing of Nigerians? Answers to these questions shall form the body of this research. The research discovers the absence of fairness in the electoral process and bad governance in Nigeria. This research reveals the flaws in effectiveness of democracy as a system of government in Nigeria. It proposes adopting an alternative model of governance. Lastly, this research contemplates the Islamic political model for a better Nigeria.
The study reported in this thesis has the following major objectives: (i) to find out effect of emotional
literacy on academic achievement in terms of experimental group and control group (ii) to find out the
difference of treatment effect between the students of low achievers group and high achievers group
(iii) To find out difference regarding treatment effect in terms of students of experimental group and
control group on the basis of variable emotional intelligence. The researcher selected 60 students of
10th class of Government Boys High School, Isa Khel (Mianwali District).
The sample was equally divided into the experimental group and the control group. Both the groups
were equated on the basis of the scores of 9th class in the Board examination (treated as pre-test). A
pre-test for emotional intelligence was also administered to find out emotional quotient (EQ) of the
experimental and the control group. A curriculum of emotional literacy consisted of Chapters 4-9 taken
from Goleman’s book entitled: “Working with Emotional Intelligence” was taught as treatment to the
experimental group. A short syllabus (Appendix-D) from Urdu Book (Part II) for 10th class was taught
to both experimental and control groups in a combined class by the same teacher. The study lasted for
twelve weeks. After twelfth week, two separate post-tests (one for academic achievement and other for
emotional intelligence) were administered to the both experimental and control groups.
Data were collected, tabulated, analyzed, and interpreted in the light of the objectives of study. Data
were analyzed by applying t-test and (2x2) ANOVA. The findings of the study revealed that there is a
considerable effect of emotional literacy on the academic achievement of the students at secondary
level. It was also found that emotional literacy has improved emotional intelligence of the students.
Moreover, it was found that emotional literacy was equally helpful and effective for both high achievers
and the low achievers. Finally, on the basis of the findings of the study, the researcher put forward some
feasible and practicable suggestions/ recommendations in this area.
It is recommended to include emotional literacy in the curriculum as a compulsory subject, particularly
at secondary level. Emotional education may be utilized in solving the issues of problematic behaviors
of the children in the schools. The managers of educational institutions may monitor teaching learning
process with a view to implementing emotional literacy policy. A special curriculum model suitable for
the subject of emotional literacy may be devised. Moreover, public awareness regarding the importance
of emotional literacy should be increased by using mass media. Emotional literacy should be made an
important element of professional training of teachers, managers, curriculum developers. For further
research it is recommended that the present study needs to be replicated with students and schools at
larger scale and context. The association of Emotional Quotient (EQ) with Intelligence Quotient (IQ) is
another aspect which needs to be addressed.