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A Study of the Mutual Interaction of Some Antibiotics and Non-Steroidal Anti- Inflammatory Drugs in Vitro

Thesis Info

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External Link

Author

Amina Asghar

Program

PhD

Institute

Government College University

City

Lahore

Province

Punjab

Country

Pakistan

Thesis Completing Year

2014

Thesis Completion Status

Completed

Subject

Chemistry

Language

English

Link

http://prr.hec.gov.pk/jspui/handle/123456789/800

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676725419639

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This work aimed at improving efficacy and reducing toxicity of non-steroidal anti- inflammatory (NSAIDs) and anti-bacterial drugs by designing and synthesizing mutual prodrugs with dual activities. The NSAIDs were ibuprofen, flurbiprofen and aspirin, which contained a carboxylic group as part of their structure. The antibacterial included ampicillin, metronidazole, isoniazid, sulfamethoxazole, sulfamerazine, sulfamethazine, sulfanilamide, 7- ADCA and 7-AVCA, which contained an amino group as part of their structure. In the prodrugs of these compounds the two drugs were covalently linked together forming an amide linkage. In addition to these a prodrug from benzydamine, containing amino group, and cefazoline, containing carboxylic group was synthesized, in which the two drugs formed a quaternary ammonium salt. All the synthesized compounds were characterized by use of diverse analytical techniques including elemental analysis, FT-IR, electronic spectra, 1H and 13 C NMR, ESI-MS and single crystal XRD techniques. The new compounds were subjected to anti-bacterial, anti-inflammatory, enzyme inhibition and toxicity tests in order to evaluate them as more effective and safe drugs with dual activities. Some of the activity related properties, which could not be determined experimentally, were determined through computational analysis. The results showed that aspirin, flurbiprofen and ibuprofen prodrugs perform better (having moderate to significant difference) than the parent drugs in anti-bacterial and anti-inflammatory tests. The computational analysis also suggests that the prodrugs possess better druglike properties and bioavailability with slight variations. Thus this study clearly indicates that mutual prodrug is an advantageous option where a concomitant treatment is required.
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اسلام زندہ ہوتا ہے ہر کربلا کے بعد

اسلام زندہ ہوتا ہے ہر کربلا کے بعد
نحمدہ ونصلی علی رسولہ الکریم امّا بعد فاعوذ بااللہ من الشیطن الرجیم
بسم اللہ الرحمن الرحیم
صدر بزم و معزز اساتذہ کرام اور میرے ہم مکتب ساتھیو!
آج مجھے جس موضوع پرلب کشائی کا موقع فراہم کیا گیا ہے ،وہ کچھ یوں ہے:
’’اسلام زندہ ہوتا ہے ہر کربلا کے بعد ‘‘
معزز سامعین!
تاریخ حق و باطل میں خیر و شر کے لاکھوں معرکے ہوئے، ہزاروں شہادتیں ہوئیں۔ اسلام کا اوّلین دور لاتعداد شہادتوں سے لبریز ہے مگر جو شہرت حضرت امام حسین ؓ کو حاصل ہوئی وہ کسی اور کو نصیب نہ ہو سکی۔ آج تک کسی شہادت کو اس قدر شہرت، قبول عام اور ہمہ تذکرہ نصیب نہ ہو سکا جتنا امام حسین ؓ کو ہوا ہے۔ تقریباً ساڑھے تیرہ سو سال گزرنے کے باوجودبھی شہادت امام حسین ؓکا ذکر زندہ و تابندہ ہے۔ حسینیت ہر طبقے میں حق اور یزید یت ہر طبقے میں فتنہ و فساد کی علامت بن گئی ہے۔
حاضرین محفل!
جب یزید تخت نشین ہوا تو اس نے اپنے اقتدار کی راہ میں حائل ہر رکاوٹ کو بڑی بے دردی اورسختی سے دور کرنا شروع کر دیا۔ اسے اپنی راہ میں سب سے بڑی رکاوٹ حضرت امام حسینؓ محسوس ہوئے تھے تو اس نے گورنر مد ینہ کو حکم دیا کہ امام حسین ؓکے پاس جا کر میری بیعت طلب کرو۔ گورنر مدینہ نے حضرت امام حسین ؓکو یزید کا پیغام پہنچایا تو آپ ؓنے صاف انکار کر دیا۔ یہ آپ ؓنے اس لیے کیا کہ آپ ؓ کو اپنے نانا جان حضوراکرمؐ کا فرمان یاد تھا ’’کہ ظالم جابر حکمران کے سامنے کلمہ حق کہنا سب سے بڑا جہاد ہے۔‘‘ تاریخ کے غائر مطالعہ سے جو چیز واضح طور پر ہمارے سامنے آتی ہے وہ یہ ہے...

Revelation in Hinduism: A Muslim Reading

Hinduism has been viewed by Semitic religions as a religion devoid of revelation. Early, Medieval and modem Muslim and Christian writings have often portrayed Hinduism as pagan even satanic while Hindus for millennia have claimed to be divinely revealed. Is Hinduism really a revealed religion and if so, what kind of a revelation does it have? In what manner does the divine reveal himself and who are the recipients of this revelation? To what extent is this concept different from ours? Does the process of revelation continue or has it been discontinued? These are some of the more significant questions that this article shall engage with. It clarifies that Hindus have books which they consider revealed and look upon much as Muslims look upon their Qur’an. The most significant of these among a majority of the Hindus are called the Vedas, literally, knowledge. It goes on to introduce the Vedas with respect to their various parts and content, what Hindus largely believe about it and how they ensured its preservation and safe transmission to later generations through various intricate and elaborate memorization techniques. The article highlights the importance of rishl, the recipients of these revelations, their kinds, characteristics and role in the process of revelation. The article contends that there is much in common between Rishland Semitic prophets with respect to their characteristics but that the similarities do not end here. Rather there is much more common ground to be explored with respect to revelation and its contents and its conveyors than meets the eye.

Synthesis, Characterization and Pharmacological Evaluation of Some 1, 2, 4-Triazole, 1, 3, 4-Oxadiazole, Triazolothiadiazole and Indolinone Derivatives

The work presented in the thesis consists of the synthesis, characterization and pharmacological evaluation of nitrogen-containing heterocyclic compounds. For convenience, the research work presented in this thesis has been divided into four chapters. The first chapter includes, the synthesis, characterization and pharmacological evaluation of 4,5- disubstituted-1,2,4-triazole-3-thiones and 4,5-disubstituted-1,2,4-triazole-3-ones. Both of these target compounds were synthesized by four-step syntheses involving a series of reactions, including esterification of substituted aromatic acids, hydrazide formation and their condensation with substituted isothiocyanates and substituted isocyanates resulting in the formation of thiosemicarbazides and semicarbazides. The former were obtained by refluxing thiosemicarbazides in sodium hydroxide solution (4N) and the latter were formed by refluxing semicarbazides in sodium hydroxide solution (2N). The final products were obtained by neutralizing the reaction mixtures with dilute hydrochloric acid solution. Later on, the synthesized compounds were screened for their antifungal, anti-inflammatory, acetylcholinesterase, alkaline phosphatase and -glucoronidase activities. The second chapter includes the synthesis, characterization and pharmacological evaluation of 1,3,4-oxadiazoles. These compounds were synthesized by refluxing aromatic acid hydrazides with carbon disulfide in ethanolic potassium hydroxide. All of these compounds were checked for their cytotoxic activities using three different cell lines. The third chapter includes the synthesis, characterization and pharmacological evaluation of triazolothiadiazoles-substituted bridged heterocycles. The synthesis involves the formation of 5- substituted-4-amino-1,2,4-triazole-3-thiones by stirring different aromatic hydrazides with carbon disulfide in methanolic potassium hydroxide and resulted in the formation of potassium dithiocarbazinate salts, which on refluxing with hydrazine hydrate, yielded 5-substituted-4- amino-1,2,4-triazoles-3-thiones. Triazolothiadiazoles were formed by refluxing different aromatic acids with 5-substituted-4-amino-1,2,4-triazoles-3-thiones in phosphoryl chloride. All the synthesized compounds were screened for antibacterial, acetylcholinesterase and alkaline phosphatase activities. The fourth chapter addresses the synthesis, characterization and pharmacological evaluation of Schiff bases of isatin, which are known as indolinone derivatives. These compounds were synthesized by the reaction of acid hydrazides with substituted isatins in ethanol. The synthesized compounds were screened for cytotoxic activity.