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Synthesis of Quinoline, Idane-1, 3-Dione, Urea and Thiourea Derivatives and Their Bioactivities

Thesis Info

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External Link

Author

Bilquees Bano

Program

PhD

Institute

University of Karachi

City

Karachi

Province

Sindh

Country

Pakistan

Thesis Completing Year

2018

Thesis Completion Status

Completed

Subject

Physical Sciences

Language

English

Link

http://prr.hec.gov.pk/jspui/bitstream/123456789/10785/1/Bilquees%20Bano_Chem_2018_UoK_PRR.pdf

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676725065361

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This research work consists of the synthesis of quinoline, indane 1,3 dione and urea and thiourea derivatives by adopting various synthetic chemical transformations and screening of their biological activities. All compounds were fully characterized by various spectroscopic techniques such as 1H-NMR, 13C-NMR, EI-MS/FAB-MS and HRMS. Melting points of all compounds were also recorded. This dissertation consists of three chapters based on the extensive literature and research findings regarding the five libraries of synthetic compounds. Each chapter has its own compounds numbering, tables, figures, schemes and references Chapter-1 composed of the broad literature survey regarding the general introduction of quinoline, its biological background and various synthetic protocols. This chapter is divided into three parts. Synthesis of Quinoline derivatives and their structure-activity relationship studies 30-52 (Part A), benzamide derivatives of quinoline 53-83(Part B), Sulfonamide and Sulfonyl ester deravatives of quinoline 84-133(Part C) and evaluation of their in vitro activities. Compounds 31, 32, 35, 42, 43 and 48 showed good to moderate antiglycation activity. Compound 34 showed moderate leishmanicidal activity. Compound 41 was found to be more potent than standard thiourea. All compounds are non toxic on rat fibroblast 3T3 cell lines. Compounds 30, 41, 42, and 47 were showed good antiinflammatory potential and found to be more potent than standard ibuprofen. Compounds 53-83 were found to be inactive against immunomodulatory, leshminasis, DPPH and dipeptidyl peptidase activity. Compound 84-133 were screened for βGlucuronidase activity. Out of which Compounds 85-91, 93, 95, 97, 98,101-105, 110, 112 and 115 were found to be more potent than standard D-Saccharic acid 1,4 lactone. Their random screening resulted in finding of some lead molecule for further studies. Chapter-2 demonstrated the Synthesis of urea and thiourea analogs and their biological studies 134-175. Compounds 140, 142, 143, 162, 163, 167 and 170 were more potent than standard thiourea.While compounds 141, 144, 145, 150, 164, 166, 172 and 173 were found to be moderate active in urease inhibitory activity. Chapter 3 Comprises the synthesis of Indane 1,3 dione derivatives and their structure activity relationship studies. Biological screening of all compounds showed that compounds 174, 182, 185, 188-191, 194-197 and 199 showed moderate to weakly leishmanicidal activity. Compound 201 was moderately active in antioxidant assay.
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مولانا محمد زکریا[شیخ الحدیث]

حضرت شیخ الحدیث مولانا محمد زکریارحمۃ اﷲ علیہ
حوادث اور تھے پر دل کا جانا
عجب اک سانحہ سا ہوگیا ہے
واحسرتا!آخر۲۴/مئی کوحضرت شیخ الحدیث مولانا محمد زکریا بھی ہم سے جداہوکر قرب وجوار خداوندی کے اپنے اس مسکن حقیقی میں پہنچ گئے جہاں جانے کے لیے جیسا کہ آپ کا ہر ندیم وہم نشین محسوس کرسکتا تھا، برسوں سے آپ کی روح پرفتوح مضطرب وبے قرار تھی اور عالم اسلام گوہر شب چراغ ملّت بیضا سے یکسر محروم ہوگیا۔ اناﷲ واناالیہ راجعون۔
گذشتہ سال حضرت شیخ نے رمضان المبارک کاپورامہینہ جنوبی افریقہ کے ایک مقام اسٹرنگر میں گزارا تھا، حسن اتفاق سے اپنے ایک عزیزدوست مسٹر موسیٰ پارک کی نجی دعوت پر راقم الحروف بھی رمضان کے آخری ہفتہ میں ڈربن پہنچا، ڈربن سے اسٹرنگر کافاصلہ ڈیڑھ سو کلومیٹر ہے جوجنوبی افریقہ کی زندگی میں درحقیقت کوئی فاصلہ ہی نہیں، اس لیے جب تک حضرت کا قیام اسٹرنگر میں رہا تو وہاں اوراس کے بعد جب آپ ڈربن اوراس کے اطراف واکناف میں ایک ایک دودودن کے لیے قیام فرماہوئے توان مقامات پروقتاً وقتاً خدمت سامی میں برابر حاضر ہوتارہا، اس اثنا میں میں نے حضرت کی صحت اور نقل وحرکت سے مجبوری ومعذوری کاجوحال دیکھا اورساتھ ہی یہ بھی دیکھا کہ حضرت کاپروگرام جنوبی افریقہ،مزمبیق اورنیروبی کامکمل دورہ کرنے اور اس کے بعدانگلینڈ جانے کا ہے اورپھریہ مشاہدہ بھی کیا کہ جہاں کہیں پہنچتے ہیں ہرطبقہ اورہرگروہ کے ہزاروں بوڑھے اورجوان پروانوں کی طرح آپ پرگرتے ہیں توان سب چیزوں کے پیش نظر معاً خیال ہوا کہ یہ جوکچھ ہورہاہے کسی غیبی حکم اوراشارہ پرہورہاہے اور ساتھ ہی اندیشہ اس بات کا ہوا کہ غالباً اب وہ وقت قریب ہے جب کہ یاایتھا النفس المطمئنۃ ارجعی الی ربک راضیۃ مرضیۃ صدائے غیب حضرت کے سامعہ نوازہوگی، بعد میں یہ خیال اوراندیشہ دونوں صحیح ثابت ہوئے،...

Comparison of Economic Activities: Time Deposits, Investments, Income and Needs

This article aims to discuss the comparison of economic activities including time deposits, investment, income and needs. The advantage of a bank by raising reserves through stores is that the cash put away can take longer, considering that stores have a moderately long period of time and the recurrence of withdrawals is additionally uncommon. Hence the bank can unreservedly utilize the credit of these stores. Income in common is regularly related to the sum of cash an individual gets as a result of something done, done, or contributed. The pay is at that point utilized or went through to meet different needs in life for a certain period of time. It is vital to have Financial Management by giving need scale by prioritizing all things that are vital since the more noteworthy a person's pay more often than not the more he needs. The survey results within the AES business group show a significant comparison of the amount of income derived from investment and sales that generate income, while time deposits are rarely performed as a principal economic activity in generating income.

Facies Distribution, Depositional Environments, Provenance and Reservoir Characters of Upper Cretaceous Succession Kirthar Fold Belt Pakistan

Excellent exposures of Upper Cretaceous succession (Campanian-Maastrichtian; Mughal Kot and Pab formations) in the north-south trending Kirthar Fold Belt, Pakistan are studied in detail. The succession is 7 m to 467 m thick in the study area and is comprised of fine to coarse, thin to thick-bedded sandstone with subordinate mudstones and marls. The succession was deposited on west (northwest)-facing passive margin of the Indian Plate. Twelve facies are identified and grouped into nine facies associations, which exhibit that they were formed in two partly coeval depositional systems: the Northern Depositional System and Southern Depositional System. The Northern Depositional System consists of shoreface (upper shelf), shelfal delta lobes (middle shelf) and outer shelf ramp (lower shelf) facies association, formed on a storm and flood dominated, low gradient clastic shelf of Mutti type shelf delta lobes. The Southern Depositional System is characterized by fluviodeltaic deposits in the southeast (proximal) and deep water turbidite sandstones in the northwest, formed in channel-levee and lobes complex within deep slope and basin floor settings. In the Southern system, the Mughal Kot Formation is comprised of basin floor lobes, channel filled sand bodies and base of slope mud rich lobes, whereas, the Pab Formation is comprised of submarine slope fan, channels and levee deposits. The succession was deposited during regression phase as indicated by shallowing upward trend which is evidenced from thickening upward cycles, grain size, bed thickness increase and shallow marine Ranikot Group deposited over the succession. Physiography and tectonic character of Indian Passive margin during its drifting towards north deduce its regional distribution, vertical & lateral sequences and style of sandstone bodies both in northern and southern depositional systems. Sandstones composition and petrography of these two systems are also significantly different. The sediments were supplied to the shallow marine deposits in Northern Depositional System from thermally uplifted Indian shield in the east as evidenced from persistent westward paleocurrent directions. Deep marine turbidite sands were sourced by north-northwest directed density currents. Uppermost parts of the Upper Cretaceous succession in Southern Depositional System contain an appreciable amount of volcanic fragments, which were most probably caused by Deccan Trap volcanism in south-southeast to the studied area. Low K2O/Al2O3 ratio in mudstones, high values of CIA (Chemical Index of Alteration) and SiO2 – Al2O3+K2O+Na2O diagram suggest the initial feldspar deficiency was caused by intense chemical weathering due to warm humid paleoclimatic conditions in source area. Further reduction of feldspar was caused by long transport distance and most effectively by diagenetic dissolution, alteration and replacement. The sandstones have undergone intense and complex diagenetic changes due to framework composition of sandstones, burial depth and thrusting of Bela Ophiolites. The unstable grains like feldspar and lithic volcanic fragments were dissolved considerably and altered to a variety of clay minerals. Compaction, authigenic cementation, dissolution and grain fracturing are important diagenetic events identified. Calcite, quartz, clay minerals and iron oxide are the common authigenic cements. Dissolution and alteration of feldspar and volcanic lithic fragments and pressure solution were the main sources of quartz cements. Mechanical compaction, authigenic cements like calcite and quartz reduced the primary porosity of the sandstones, whereas, dissolution of feldspar and volcanic grains have enhanced and produced secondary porosity up to 15.53% (average 2.77 to 10.61%). Chlorite coating has prevented the quartz cementation, so some microporosity was preserved. Some microporosity in interbooklets of kaolinite is observed.