Design, Synthesis and Biological Evaluation of New Substituted Pyrimidine Derivatives / (Record no. 173601)
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| 000 -LEADER | |
|---|---|
| fixed length control field | 05913namaa22004571i 4500 |
| 003 - CONTROL NUMBER IDENTIFIER | |
| control field | OSt |
| 005 - أخر تعامل مع التسجيلة | |
| control field | 20250924135756.0 |
| 008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION | |
| fixed length control field | 250818s2024 |||a|||frm||| 000 0 eng d |
| 040 ## - CATALOGING SOURCE | |
| Original cataloguing agency | EG-GICUC |
| Language of cataloging | eng |
| Transcribing agency | EG-GICUC |
| Modifying agency | EG-GICUC |
| Description conventions | rda |
| 041 0# - LANGUAGE CODE | |
| Language code of text/sound track or separate title | eng |
| Language code of summary or abstract | eng |
| -- | ara |
| 049 ## - Acquisition Source | |
| Acquisition Source | Deposit |
| 082 04 - DEWEY DECIMAL CLASSIFICATION NUMBER | |
| Classification number | 615.2 |
| 092 ## - LOCALLY ASSIGNED DEWEY CALL NUMBER (OCLC) | |
| Classification number | 615.2 |
| Edition number | 21 |
| 097 ## - Degree | |
| Degree | M.Sc |
| 099 ## - LOCAL FREE-TEXT CALL NUMBER (OCLC) | |
| Local Call Number | Cai01.08.05.M.Sc.2024.Ah.D. |
| 100 0# - MAIN ENTRY--PERSONAL NAME | |
| Authority record control number or standard number | Ahmed Mahmoud Salem Soliman, |
| Preparation | preparation. |
| 245 10 - TITLE STATEMENT | |
| Title | Design, Synthesis and Biological Evaluation of New Substituted Pyrimidine Derivatives / |
| Statement of responsibility, etc. | By Ahmed Mahmoud Salem Soliman Under The Supervision Of Dr. Heba Abdelrasheed Abdelkhalek, Dr. Bassem Heshmat Naguib, Dr. Walaa Ramadan Mahmoud. |
| 246 15 - VARYING FORM OF TITLE | |
| Title proper/short title | تصميم وتشييد والتقييم البيولوجى لمستبدلات مشتقات البيريميدين الجديدة / |
| 264 #0 - PRODUCTION, PUBLICATION, DISTRIBUTION, MANUFACTURE, AND COPYRIGHT NOTICE | |
| Date of production, publication, distribution, manufacture, or copyright notice | 2024. |
| 300 ## - PHYSICAL DESCRIPTION | |
| Extent | 133 pages : |
| Other physical details | illustrations ; |
| Dimensions | 25 cm. + |
| Accompanying material | CD. |
| 336 ## - CONTENT TYPE | |
| Content type term | text |
| Source | rda content |
| 337 ## - MEDIA TYPE | |
| Media type term | Unmediated |
| Source | rdamedia |
| 338 ## - CARRIER TYPE | |
| Carrier type term | volume |
| Source | rdacarrier |
| 502 ## - DISSERTATION NOTE | |
| Dissertation note | Thesis (M.Sc.) -Cairo University, 2024. |
| 504 ## - BIBLIOGRAPHY, ETC. NOTE | |
| Bibliography, etc. note | Bibliography: pages 114-133. |
| 520 #3 - SUMMARY, ETC. | |
| Summary, etc. | A series of novel substituted 1,6-dihydropyrimidinone derivatives were designed, synthesized, and biologically evaluated as preclinical antibacterial candidates, β-lactamase enzyme inhibitors and anticancer agents. <br/>All compounds were tested for their antibacterial activity against Staphylococcus aureus, Bacillus subtilis as a gram-positive species whereas Pseudomonas aeruginosa as a gram-negative species, most of the compounds exhibited promising antibacterial activity compared to reference drug amoxicillin. <br/>Furthermore, the clinical antibacterial tests conducted on β-lactamase resistant strains of Acinetobacter baumannii, Bacillus subtilis and Staphylococcus aureus indicated that the compounds synthesized have the potential to inhibit the activity of β-lactamase enzymes. In addition, the in-vitro test performed on β-lactamase enzymes revealed that compounds VIi, VId and VIIIb have a lower IC50 values (0.164, 0.289 and 0.278 µg/mL respectively) compared to the reference clavulanic acid (0.186 µg/mL). <br/>Moreover, NCI 60 cell-line panel screening for the synthesized compounds revealed the moderate antiproliferative activity of the phenyl derivative VIa with the highest growth inhibition percentage of 34.91% on CNS cancer SNB 75 cell lines. VIa and VIg displayed moderate enzymatic inhibition effect against CDK2 (56.57 and 84.68 µM) and EGFR (25.02 and 63.48 respectively) enzymes.<br/>Additionally, molecular docking was carried out predicting the binding mode of VIi, VId and VIIIb and proving its stability in the β-lactamase enzyme-binding pocket. <br/>These findings suggest that compounds VIi, VId and VIIIb are considered a promising hit for further development of potent and selective β-lactamase inhibitors.<br/> |
| 520 #3 - SUMMARY, ETC. | |
| Summary, etc. | تم تصميم سلسلة من مشتقات البيرميدين الجديدة ، وتحضيرها، وتقييمها بيولوجيًا كمضادات البكتريا، ومثبطات لانزيم β-lactamase و كمضادات للسرطان. كشف فحص الخلوي (NCI ) للمركبات المركبة عن النشاط المتوسط المضاد للتكاثر للمستبدل VIa مع أعلى نسبة تثبيط نمو قدرها34.91٪ على خطوط خلايا سرطان الجهاز العصبي المركزي (SNB 75). أظهر VIa وVIg تأثير تثبيط إنزيمي متوسط ضد إنزيمات EGFR وCDK2.<br/>من ناحية أخرى، تم اختبار جميع المركبات لنشاطها المضاد للبكتيريا ضد Staphylococcus aureus ، Bacillus subtilis باعتبارها gram-positive في حين أن Pseudomonas aeruginosa باعتبارها gram-negative، أظهرت معظم المركبات نشاط واعد كمضادات للبكتريا مقارنة مع الدواء المرجعي أموكسيسيلين. <br/>بالإضافة لذلك، أشارت الاختبارات المضادة للبكتيريا التي أجريت على سلالات مقاومة β-lactamase من Acinetobacter baumannii وBacillus subtilis وStaphylococcus aureus إلى أن المركبات المصنعة لديها القدرة على تثبيط نشاط إنزيمات β-lactamase. بالإضافة إلى ذلك، كشف الاختبار المختبري الذي تم إجراؤه على إنزيمات β-lactamase أن المركبات VIdوVIIIb وVIi لهما قيمة IC50 أقل مقارنة مع الدواء المرجعي acid clavulanic.<br/>علاوة على ذلك، تم إجراء الالتحام الجزيئي للتنبؤ بنمط الارتباط لـ VIdوVIIIb وVIi وإثبات ثباته في الموقع النشط لإنزيم β-lactamase. <br/>تشير هذه النتائج إلى أن المركبات VIdوVIIIb وVIi تعتبر بمثابة مركبات واعدة لمزيد من التطوير لمثبطات β-lactamase المؤثرة والانتقائية.<br/> |
| 530 ## - ADDITIONAL PHYSICAL FORM AVAILABLE NOTE | |
| Issues CD | Issued also as CD |
| 546 ## - LANGUAGE NOTE | |
| Text Language | Text in English and abstract in Arabic & English. |
| 650 #7 - SUBJECT ADDED ENTRY--TOPICAL TERM | |
| Topical term or geographic name entry element | Pharmaceutical Chemistry |
| 651 #7 - SUBJECT ADDED ENTRY--GEOGRAPHIC NAME | |
| Geographic name | الكيمياء الصيدلانية |
| 653 #1 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | Dihydropyrimidinone derivatives |
| -- | antibacterial |
| -- | β-lactamase inhibitor |
| 653 #1 - INDEX TERM--UNCONTROLLED | |
| Uncontrolled term | مشتقات Dihydropyrimidinone |
| -- | مضاد للبكتيريا |
| -- | مثبطات B- |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Heba Abdelrasheed Abdelkhalek |
| Relator term | thesis advisor. |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Bassem Heshmat Naguib |
| Relator term | thesis advisor. |
| 700 0# - ADDED ENTRY--PERSONAL NAME | |
| Personal name | Walaa Ramadan Mahmoud |
| Relator term | thesis advisor. |
| 900 ## - Thesis Information | |
| Grant date | 01-01-2024 |
| Supervisory body | Heba Abdelrasheed Abdelkhalek |
| -- | Bassem Heshmat Naguib |
| -- | Walaa Ramadan Mahmoud |
| Universities | Cairo University |
| Faculties | Faculty of Pharmacy |
| Department | Department of Pharmaceutical Chemistry |
| 905 ## - Cataloger and Reviser Names | |
| Cataloger Name | Eman El gebaly |
| 942 ## - ADDED ENTRY ELEMENTS (KOHA) | |
| Source of classification or shelving scheme | Dewey Decimal Classification |
| Koha item type | Thesis |
| Edition | 21 |
| Suppress in OPAC | No |
| Source of classification or shelving scheme | Home library | Current library | Date acquired | Inventory number | Full call number | Barcode | Date last seen | Koha item type |
|---|---|---|---|---|---|---|---|---|
| Dewey Decimal Classification | المكتبة المركزبة الجديدة - جامعة القاهرة | قاعة الرسائل الجامعية - الدور الاول | 23.09.2025 | 91631 | Cai01.08.05.M.Sc.2024.Ah.D | 01010110091631000 | 23.09.2025 | Thesis |