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Synthesis, Characterization and Biological Studies of Novel Guanidines and Their Complexes

Thesis Info

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Author

Murtaza, Ghulam

Program

PhD

Institute

Quaid-I-Azam University

City

Islamabad

Province

Islamabad.

Country

Pakistan

Thesis Completing Year

2011

Thesis Completion Status

Completed

Subject

Chemistry

Language

English

Link

http://prr.hec.gov.pk/jspui/handle/123456789/730

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676727514871

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Two series of substituted guanidines (a 1 -a 32 & b 1 -b 32 ) and their copper(II) complexes of general formula [κ 2 (O, N)-C 6 H 5 CONHC(NHR 1 )NR 2 ] 2 Cu(II) where, R 1 = phenyl (A 1 - A 32 ), 2-chlorophenyl (B 1 -B 32 ) and R 2 = alkyl/aryl groups, have been synthesized and characterized by using elemental analysis, FT-IR, multinuclear ( 1 H and 13 C) NMR spectroscopy and magnetic susceptibility measurements. Single crystal XRD was used for structural elucidation of some of the synthesized guanidine ligands and their copper(II) complexes. Based on the single crystal X-ray analysis most of the synthesized guanidine ligands were stabilized by intermolecular as well as intramolecular hydrogen bonding. All the complexes are mononuclear in solid state and copper adopts a regular square planar geometry with slight distortion in few cases, while N,N'',N"-trisubstituted guanidine ligands chelate the Cu(II) atom through oxygen and nitrogen with ligand to metal ratio 2:1. DFT studies have been used to assess the location of the protons in free ligands, however calculations have shown that in all cases, hydrogen bonding from either of the N-H groups gives conformations that are very similar in energy. The synthesized guanidines and their complexes were also screened for urease inhibition, antileishmanial, anticancer and antifungal activities. The complexes exhibited a better usease inhibition activity than the respective guanidines and compound A 7 was found to be the most active with IC 50 = 4.8 ± 0.05 μM (IC 50 for standard thiourea is 21.0 ± 0.1 μM). These compounds were also screened for their brine shrimp lethality assay, a 1 and A 28 were found to be more toxic with the ID 50 value 1.701 ppm. In potato disc antitumour assay guanidines and complexes have shown the excellent activity comparable with the vincristine, used as standard drug while, in vitro cytotoxicity against human cell lines carcinomas A498, EVSAT, H226, IGROV, M19, MCF-7 and WIDR these compounds show moderate cytotoxicity against these cell lines as compared to the standard chemotherapeutic drugs. These compounds were also tested for antifungal and antileishmanial activities and show moderate to good antifungal activity but no significant antileishmanial activity.
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عبداللطیف تپش

عبداللطیف تپش(۱۸۹۵ء ۔۱۹۴۳ء) لاہور میں پیدا ہوئے۔ منشی فاضل اور بی۔اے کے امتحانات پاس کرنے کے بعد کچھ عرصہ پنجاب ہائی کورٹ میں ملازمت کی۔ پھر گورنمنٹ انٹر کالج پسرور ضلع سیالکوٹ میں علومِ شرقیہ کے استاد مقرر ہوئے۔ پسرور میں ملازمت کے دوران مزید تعلیم کے لیے مطالعے کو جاری رکھا اور ایم ۔اے فارسی کا امتحان ۱عزاز کے ساتھ پاس کیا۔اس امتحان میں تپشؔ یونیورسٹی بھر میں اول رہے ۔ (۴۲۷) تپشؔ کو شعرو شاعری سے حد سے زیادہ دلچسپی تھی۔ ان کے اوقاتِ تدریس بڑے دلکشا اور معلومات افزا ہوتے۔ کالج میں بزمِ ادب کی جان ہوا کرتے تھے۔ گورنمنٹ کالج پسرور میں قیام کے دوران متعدد ادبی مجالس اور مشاعروں کا مقصد طلبا کے ذوق کی نشوونما اور فروغ زبان اُردو تھا۔ جو بدرجہ اتم ہوا اور کئی طالب علم شاعر بن گئے۔ گورنمنٹ کالج پسرور میں ۴ مارچ ۱۹۳۲ء کو ابو الاثر حفیظ جالندھری تشریف لائے تو کالج کے وائس پرنسپل پروفیسر سراج الدین آذر نے کالج سٹاف کا تعارف کراتے ہوئے عبداللطیف تپشؔ کے بارے میں کہا :

یہ شاعر ہی نہیں شاعر گر بھی ہیں۔(۴۲۸)

تپشؔ کا شعر و شاعری کا ذوق جبلی تھا۔ انھیں سر عبدالقادر (مدیر مخزن) جیسی علمی و ادبی شخصیت کی دامادی کا شرف بھی حاصل تھا۔ جس کی وجہ سے آپ کے شعری ذوق کی بہت جلد اصلاح اور ترقی ہو گئی۔ تپش ؔ نے سر عبدالقادر کی علمی صحبتوں سے بصدِ رنگ استفادہ کیا لیکن آپ کی طبیعت نظم کی طرف مائل نہ ہو سکی۔ بلکہ آپ غزل ہی کے شائق و دلدادہ رہے۔ آپ شروع میں بہت پرگو اور مشکل شاعر تھے لیکن کثرتِ مشق سخن سے ان کے کلام میں سادگی و پرکاری آگئی۔ اُن کے کلام ہندوستان کے ممتاز ادبی رسائل و جرائد میں شائع ہوا کر تاتھا۔ (۴۲۹) آپ کی شاعری میں دل کشی اور سادگی...

توہین مذہب و رسالت اور سماجی رویے: اسلامی تناظر میں

Extremism is a challenge facing the societies both on secular and religious level, which has damaged the society with disrupting peace and creating caos in the world. There is a dire need of an academic discussion regarding the various aspects of the issue in Islamic and social perspectives. This is an attempt to realize the sensitivity of the subject and providing a balanced approached in the light of Islamic teachings. This article draws attention of the concerned authorities to play their role for the stoppage of blasphemous activities by implementation of the existing law and its development by determining the punishment against false accusation. The article also explains that what Islam expects from the Muslims and guides them in expressing their feelings and showing their attitudes, behavior and fixing their responsibilities regarding the issue with true Islamic spirit. The article draws the attention of the non-Muslim countries and communities as well to display impartiality, truth and realistic attitude and appropriate legislation by considering the blasphemous activities as a heinous crime.

Non-Target Effects of Insecticides and Genetically Modified Crop on Ecological Role of Collembolans in Cotton Ecosystem of Punjab, Pakistan

The present research was planned to determine the effects of insecticides and genetically modified cotton on the abundance of Collembola and on their ecological role as these are the most abundant group of organisms and also used as bio-indicators in disturbed soil habitats. Base line data of Collembola demography were determined in four different crops i.e. sugarcane, cotton, clover (Trifolium alexandrinum) and wheat under conventional agronomic practices. The results revealed that maximum mean abundance of Collembola was found in clover (T. alexandrinum) (36.74) followed by sugarcane (29.15), cotton (20.79) and wheat (16.52). Four species of Collembola (Isotoma decorata, Xenylla indus, Seira indra and Sminthurus mime) were abundant in cotton followed by three (Xenylla indus, Seira indra and Sminthurus mime) in sugarcane and two (Xenylla indus and Seira indra) each in cotton and wheat. The proportionate percentage of the abundance of Xenylla indus was 65% followed by 20% of Seira indra, 13% of Isotoma decorata and 2% of Sminthurus mime throughout the sampling period. The principal component analysis revealed significant effect of soil moisture and soil pH on the abundance of Collembola while the effect of soil temperature, relative humidity and organic matter was non-significant. The abundance of Collembola was positively correlated with soil moisture and organic matter in all the crops, soil temperature in wheat, relative humidity in sugarcane and cotton, soil pH in cotton while negatively correlated with soil temperature in sugarcane, cotton and clover (T. alexandrinum), relative humidity in clover (T. alexandrinum) and wheat, soil pH in sugarcane, clover (T. alexandrinum) and wheat. A laboratory test was conducted to determine the effect of different insecticides on the survival rate of Isotoma decorata after exposure to various doses for the period of eight weeks. Endosulfan, chlorpyrifos, chlorfenapyr and acetamiprid were the highly toxic, imidacloprid, bifenthrin and pyriproxifen were moderately toxic while emamectin benzoate, spinosad and cypermethrin were the least toxic at their recommended doses against I. decorata. No individual of I. decorata was alive when they were exposed to recommended doses of endosulfan and chlorpyrifos for two weeks, acetamiprid for three weeks, chlorfenapyr for four weeks, imidacloprid for five weeks and bifenthrin for eight weeks while mortality of all the released individuals during the period of study, was not observed for pyriproxifen, emamectin benzoate, spnisoad, and cypermethrin. Field experiments consisting of 3 field trials were conducted for two consecutive years (2012 and 2013) at Faisalabad and Multan to determine the effects of insecticides and Bt cotton on the population abundance of Collembola. In the first field trial, the repeated applications of acetamiprid followed by imidacloprid were found the highly toxic while spinosad was the least toxic insecticide against the Collembola. At Faisalabad, the population means of Collembola in the plots that received five applications of acetamiprid reduced to 0.22 and 0.33 individuals per trap during 2012 and 0.33 individuals per trap during 2013 as compared to the control treatments in which means of population were 21.55 and 21.77 individuals per trap during 2012 and 18.55 and 19.11 individuals per trap during 2013 in Bt and non-Bt varieties, respectively. At Multan, the population means of Collembola in the plots that received five applications of acetamiprid reduced to 0.11 and 0.22 individuals per trap during 2012 and 0.11 individuals per trap xiv during 2013 as compared to control treatments in which means of population were 15.33 and 15.88 individuals per trap during 2012 and 13.11 and 13.55 individuals per trap during 2013 in Bt and non-Bt varieties, respectively. No recovery of Collembola population was observed during this study. In the second field trial, the applications of different insecticides in the sequence also caused the significant reduction in the abundance of Collembola. A reduction in the population was observed after 7 and 15 days of treatments while slight increase or recovery in the population was observed after the 30 days of treatments. The abundance of Collembola was reduced significantly in T3 that was consisted of two applications of acetamiprid followed by one application of bifenthrin. After 30 days of treatments at Faisalabad, the population means in T3 were 1.33 and 3.77 individuals per trap during 2012 and 1.88 and 3.00 individuals per trap during 2013 as compared to the T10 (control) in which means of population were 20.33 and 21.33 individuals per trap during 2012 and 19.88 and 19.00 individuals per trap during 2013 in Bt and non-Bt varieties, respectively. After 30 days of treatments at Multan, the population means in T3 were 3.00 and 3.66 individuals per trap during 2012 and 2.33 and 3.77 individuals per trap during 2013 as compared to the T10 (control) in which means of population were 14.55 and 14.66 individuals per trap during 2012 and 13.66 and 13.11 individuals per trap during 2013 in Bt and non-Bt varieties, respectively. In the third field trial, the high doses of different insecticides caused more reduction in the abundance of Collembola as compared to the applications on the recommended dose. A recovery in the population was observed after the 25 days of treatments and onward as the period of study progressed. Fast recovery of population to control level was observed in those plots that were treated with the recommended doses while slow rate of recovery was observed in the plots that were treated with the high doses of insecticides. It is also clear from the results of field trials that there was no adverse effect of Bt cotton on the abundance of Collembola. Litterbag experiment was conducted to determine the effects of insecticides and Bt toxin on the rate of decomposition of litter by Collembola. The results showed significant effects of the mesh size of bags and treated litter on the decomposition rate, while non-significant effect of the litter type from Bt and non-Bt cotton after 60, 120 and 180 days of incubation in the soil was observed. Litter from insecticide treated Bt and non-Bt cotton fields decomposed at slower rate as compared to the untreated litter in both large and small mesh size bags. The percent mass loss of treated litter after 60, 120 and 180 days was 11.97%, 32.28% and 43.73% while mass loss of untreated litter was 16.54%, 41.15% and 56.67%. The litter of Bt and non-Bt cotton was decomposed identically and thus disapprove level of toxin in the litter which can influence Collembola.