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Home > Solution-Phase Synthesis of a Combinatorial N, N′- Disubstituted Thiourea Library: Complexation, Characterization and Biological Studies

Solution-Phase Synthesis of a Combinatorial N, N′- Disubstituted Thiourea Library: Complexation, Characterization and Biological Studies

Thesis Info

Access Option

External Link

Author

Rauf, Muhammad Khawar

Program

PhD

Institute

Quaid-I-Azam University

City

Islamabad

Province

Islamabad.

Country

Pakistan

Thesis Completing Year

2010

Thesis Completion Status

Completed

Subject

Chemistry

Language

English

Link

http://prr.hec.gov.pk/jspui/handle/123456789/1749

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676727189449

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A chemical library of N, N''-Disubstituted thioureas have been derived from substituted aromatic carboxylic acids and two types of combinatorial strategies have been employed for the construction of chemical library. For high throughput screening of components of the chemical library, solution-phase pool syntheses have been exercised, where each pool consists of four components. All the members of chemical library have also been synthesized by using a parallel mode of solution-phase combinatorial synthesis for the purpose of lead screening/identification, testing, characterization and for assembling of Cu(I), Cu(II) & Pd(II) metal complexes. Copper(I) (1A-19A, 1B-19B, 1C-19C& 1F) and palladium(II) [(1E-14E)] complexes of N, N''-disubstituted thioureas have only been synthesized with some selected thioureas from sub-library-1 and Cu(II) complexes (1D-6D) with isoureas (1-6), prepared from the thioureas derived from benzoic acid. All the thioureas (1a-40a, 1b-40b, 1c-40c, 1d-40d, 1e-40e, 1f-40f & 1g-40g) and complexes have been characterized by elemental analyses, FT-IR, 1 H & 13 C NMR spectroscopy, mass spectrometry and single crystal XRD. The stability of the Cu(I) complexes in the test medium has been confirmed by cyclic voltammetric studies. The products of pool syntheses (pools 1-40) have been characterized by mass spectrometry and GC-MS (gas chromatograph coupled with mass spectrometer) techniques. In all the Cu(I) and Pd(II) complexes, neutral N, N′-disubstituted thiourea ligands have been coordinated to the metal atom through the sulphur atom in a terminal mode except (1F), where the deprotonation of NH group of the thiourea ligand has facilitated the bonding of copper atom through N and S. The isoureas (1-6) show bidentate behavior in Cu(II) complexes having square planar geometry (1D-6D). The thioureas have also been examined for their fungicidal properties and these show significant activity against various fungi strains and low phytotoxicity for the representative monocot plant species. The complexes have been screened for their in vitro cytotoxicity in human cell lines carcinomas A498 (renal), EVSA-T (breast), H226 (lung), IGROV (ovarian), M19 (melanoma-skin), MCF-7 (breast) and WIDR (colon). They show a moderate cytotoxicity against these seven human cancer cell lines in comparison to that of the less active standard chemotherapeutic drugs. Biological screening of the synthesized thioureas and their metal complexes for various targets is in progress.
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4 ۔حدِحرابہ

4 ۔حدِحرابہ
لغوی معنی کسی کا مال یا کوئی چیز زبردستی چھین لینا ، جیسا کہ ابن فارس لکھتے ہیں
"الحاء والراء والباء أصولٌ ثلاثة: أحدها السّلْب، والآخر دويْبَّة، والثالث بعضُ المجالس.فالأوَّل: الحَرْب، واشتقاقها من الحَرَب وهو السَّلْب. يقال حَرَبْتُه مالَه، وقد حُرِب مالَه، أي سُلِبَه، حَرَباً. والحريب: المحروب. ورجل مِحْرَابٌ: شجاعٌ قَؤُومٌ بأمر الحرب مباشرٌ لها. وحَريبة الرَّجُل: مالُه الذي يعيش به، فإذا سُلِبَه لم يَقُمْ بعده. ويقال أسَدٌ حَرِبٌ، أي من شدّة غضبِه كأنّه حُرِب شيئاً أي سُلِبه. وكذلك الرجل الحَرِب۔"115
"مادہ " حَرَبَ " ہے اس کے تین معنی ہیں ایک معنی سلب کرنا(چھیننا )دوسرا دویبۃ اور تیسرا بعض المجالساور پس پہلا حرب سے مشتق ہے جس کا مطلب ہے چھیننا جیسے کہا جاتا ہے میں نے اس سے اس کا مال چھین لیا اور رجل محراب ایسے شخص کو کہتے ہیں جو امور حرب میں ماہر ہو اور حریبۃ الرجل سے مراد آدمی کا وہ مال ہے جس پر اس کی گزران ہوتی ہو جب وہ چھین لیا جائے تو اس کی گزران باقی نہ رہ سکے اور" الرجل الحرب "بہادر اور شجاع آدمی کو کہا جاتا ہے۔ "
فساد پھیلانے کے لیے کسی کو قتل کرنا حرابہ کہلاتا ہے ۔ یہ لڑائی دارالاسلام میں بھی ہو سکتی ہے اور دارالحرب میں بھی ، جیسا کہ ابن منظور لکھتے ہیں
"إِنما حَمَله على معنى القَتْل أَو الهَرْج وجمعها حُرُوبٌ ويقال وقَعَتْ بينهم حَرْبٌ الأَزهري أَنَّثُوا الحَرْبَ لأَنهم ذهَبُوا بها إلى المُحارَبةِ وكذلك السِّلْمُ والسَّلْمُ يُذْهَبُ بهما إِلى المُسالمةِ فتؤَنث ودار الحَرْب بلادُ المشركين الذين لا صُلْح بينهم وبين المسلمِين وقد حاربَه مُحارَبةً وحِراباً وتحَارَبُوا واحْترَبُوا وحارَبُوا بمعنى ورجُلٌ حَرْبٌ ومِحْرَبٌ بكسر الميم ومِحْرابٌ شَديدُ الحَرْبِ شُجاعٌ۔" 116
"اس کو محمول کیا ہے قتل کے معنی پر اور اس کی جمع حروب ہے اور کہا جاتا ہے کہ ان کے درمیان لڑائی واقع ہوئی اور دارالحرب ایسے...

Reconciliation Process in Afghanistan and Pakistan as Cardinal Player

Afghanistan is in state of war for almost 40 long years but the political dynamics got changed after 9/11. Since the war on terror started facets of peace talks launched without meaningful end. The reconciliation process in Afghanistan had immediately started after establishment of Afghan interim government in 2001. Till 2016 mid, four different reconciliation /reintegration processes were launched by the USA and Hamid Karzai government with Afghan Taliban. The new elected president Ashraf Ghani ended all such processes in 2016 but showed willingness again in 2018 for direct peace talks between USA and Taliban clerics. In the current political scenario, Afghan reconciliation process is back on track with direct peace talks between USA, Taliban and Afghan Government along other international actors. However, Taliban were not ready to sit with the Afghan Government and this is where the Pakistan played as key to Afghan peace process. The focus of this research article is to find the challenges and opportunities of this peace process; Pakistan’s role as cardinal player can consolidate the peace process in Afghanistan. Furthermore, this research will give future recommendations for the peace process in Afghanistan.

Date Palm Diversity in Pakistan and its Relationship With World Dates Germplasm for Exploring the Center of Origin of Phoenix Dactylifera L.

Date Palm, (Phoenix dactylifera L.) often called ‘nakhl’, ‘khajor’, or ‘khaji’ belonging to the family Arcaceae (Dransfield et al., 2008) is an evergreen tree. It is the hardiest among tropical fruit trees and exceeds most other fruit crops in productivity and adaptability. The characterization of date palm at the genetic level supplemented with phenotypic character is of great concern as an important step towards efficient conservation, maintenance and utilization of the existing genetic diversity. The present research work was carried out to investigate the phenotypic variability and genetic diversity of the date palm germplasm present in the 16 districts of Pakistan. A planned survey of date palm growing regions of Pakistan in 4 provinces (Punjab, Sindh, Khyber Pakhtunkhwa and Balochistan) and Azad Jammu and Kashmir was conducted for collecting leaf and fruit samples of date palm. Young and healthy leaves were used to extract DNA whereas seeds were extracted from fruit for recording qualitative and quantitative morphometric diversity. In total, 2460 seeds of 82 accessions were included in morphometric study. About 139 date palm accessions were evaluated for genetic variability and population structure. The recorded data were analyzed using a set of different statistical tools for making significant interpretation. A total of 19 traits (5 quantitative and 14 qualitative) enabled an assessment of phenotypic diversity and structure. The measured traits: dorsal area, lateral area, embryo to apex length, embryo to base length and their percentage, seed base, micropyle position, seed wings and frequency of wings were more variable. PCA grouped all the accessions according to their phenotypic relations and morphometric characteristics. Cluster analysis distributed all the 82 Pakistani date palm accessions into their three original groups. The results reflect huge seed morphometric variation and presented seeds as a powerful tool for phenotyping. Furthermore, our study also exhibited strong resemblance and possible relationship between some groups of accessions. All 18 SSR primer pairs successfully analyzed molecular genetic variation and produced multiple fragments in the Pakistani collection as well as in date palm germplasm representing 10 different date palm growing regions of the eastern and western world. These set of markers proved themselves as highly polymorphic for genetic diversity estimation and population structure within and among all the geographically spaced population of xvii worldwide accessions. The findings of implemented markers revealed 2-23 alleles per locus with high level of expected heterozygosity in the accessions collected from Pakistan. The most informative SSR marker in this study was mPdCIT078. In addition, cultivar identification key were established. It allowed resolving the difference and constructs the relationships of the same name or vice versa. Our results also suggested the existence of population subdivision at the regional level. Population from semi arid – monsoonal or canal irrigated (seasonal or perennial) belt of Punjab (Bhakkar, Muzafargarh and Rahim Yar Khan) and dry arid ecological zones of Balochistan (Kech, Gwadar) are stable in their structure whereas DAPC distributed 342 accessions of 10 date palm growing countries into two major geographical groups (eastern and western). It is concluded that Pakistani germplasm has huge diversity and genetic pool were close to the eastern world especially Iraq and Oman.