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Combinatorial Design, Synthesis, Bioevaluation and Sar Studies on Some Small Drug‐Like Molecular Libraries

Thesis Info

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Author

Nazir, Samina

Program

PhD

Institute

Quaid-I-Azam University

City

Islamabad

Province

Islamabad.

Country

Pakistan

Thesis Completing Year

2009

Thesis Completion Status

Completed

Subject

Chemistry

Language

English

Link

http://prr.hec.gov.pk/jspui/handle/123456789/1449

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676725745596

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A combinatorial synthesis of small libraries of a variety of amino chalcones has been carried out in solution phase under standard Claisen Schmidt conditions. The compounds were tested for their potential as antibacterial and cytotoxic agents as well as phosphatase inhibitors and the leads were identified in each bioassay. Chalcone 7 was found to have strongest potential as cytotoxic agent, while chalcone 11 be the most potent PGM inhibitory agent. Parallel synthesis of a 120 member chalcone library was carried out as mixture synthesis following the positional scanning protocol. The identification of lead in this library was carried out by deconvulution and chalcones 22 and 41 were found to be the most potential candidates to be developed as antibacterial agents. Following the same strategy of mixture synthesis, another 175 member chalcones library was synthesized and most potent anticancer chalcones 31, 61 and 78 were identified by deconvolution through position scanning protocol. Peptidyl α,β- unsaturated ketones were synthesized as novel bis- electrophiles susceptible for 3+2 and 3+4 annulations. As a result, peptidyl oxazoles, pyrazolines, pyrazoles, benzothiazepines and benzodiazepines were synthesized. Potent antidiabetic chalcones were docked into the PGM active site and a rationale was found for greater antidiabetic activity of chalcones over the other. Rational design and synthesis of some cytotoxic chalcones was based on 3DQSAR studies using CoMFA as a tool. 3DQSAR studies were also carried out on a library of 30 chalcones as potential antitumor agents.
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ڈاکٹر محی الدین زورؔ

ڈاکٹرمحی الدین زورؔ
ڈاکٹر محی الدین زورؔدکن کے مولوی عبدالحق تھے، انھوں نے خود بھی بلند پایہ تحقیقی کتابیں لکھیں، اورادارہ ادبیات اُردو کے ذریعہ قدیم مخطوطات کواڈٹ کرکے اور چھاپ کر اور نوجوان نسل میں اُردو ادب کاذوق اور تحقیق کاجذبہ پیدا کرکے اورعوام میں مختلف طریقوں سے اُردو کومقبول بناکر علماً وعملاً زبان اوراُس کے ادب کی وہ شاندار خدمات انجام دی ہیں کہ بابائے اُردو کومستثنیٰ کرکے کوئی دوسرا شخص اُن کے حریف ہونے کا مدعی نہیں ہوسکتا۔ [جون ۱۹۶۳ء]

 

EFFECTS OF MILD, MODERATE AND INTENSE PHYSICAL ACTIVITY ON KNEE JOINT PROPRIOCEPTION IN HEALTHY YOUNG ADULTS

Aim: To evaluate the immediate effects of various activity levels on knee joint position sense. Methodology: Sixty males aged between 19 and 24 years, without any complains of discomfort or pain in the knee joint were selected from Bakhtawar Amin Hospital, Multan using convenience sampling, between April 2nd, 2019 to July 28th, 2019. Group A participants walked on the treadmill at a speed of 4 km/h for 5 min (n = 20). Group B participants ran on a treadmill at 6.4 km per hour for five minutes (n = 20). Group C participants sprinted on a treadmill at 8.5 km per hour for five minutes (n = 20). Results: Mean age of the subjects was 21.18±1.77. In the moderate physical activity group, the difference in the means in passive reproduction of the knee flexion angle of 20o observed was 1.40±2.39, (p-value 0.013), and similarly in intense physical activity was 1.75±3.58 (p-value 0.020). For the knee flexion angle of 40o, the difference in the means for moderate was 1.35±1.84 (p=0.002), and for the intense activity was 2.35±2.27 (p=0.012). However, in the group with mild physical activity, the difference in the means was statistically insignificant. Conclusion: The study indicated that physical activities of moderate level and intense level decrease the joint position sense appreciation at the knee joint in less active healthy individuals.

Bilal

to find out the association between terrorism and different factors affecting learning behavior of secondary school students. . It was found agreed by the respondents that terrorism causes fear among students, affects the learning process, terrorist mostly kidnap the school students and use them as suicide bomber after brainwashing. Military operations in the tribal areas and drone attacks created hatred against America and Pakistani military forces because of the perception to be an allied force which ultimately increased terrorism in Khyber Pakhtunkhwa. Parents remain worried till returning of their children from school and don’t allow them to take part in any co-curricular activity. Media is not performing its due positive role. It was concluded from the study that fear was created among students due to terrorism. Behavior related problems, shortage of attendance, drop out and intolerance increased. Social injustice, religious extremism, false interpretation of Islamic ideas, Interference of foreign intelligence agencies in our country, our weak security network, curriculum in the most deeni madaras, Post Afghan-Russian war groups, Military operations in the tribal areas and drone attacks were the main causes of terrorism. The study suggested that literacy and effective performance of schools, teachers, religious leaders, media, intelligence agencies, foreign ministry, and curriculum wing can eradicate or reduce the terrorism.