219 research outputs found
Nonclassical Antifolate Compounds as Dihydrofolate Reductase Inhibitors: Synthesis and Biological Evaluation
No full textPhDDihydrofolate reductase (DHFR) catalyzes the reduction of folate or
dihydrofolate into tetrahydrofolate, which then converted into N5, N10-
methylenetetrahydrofolate. This later compound functions as the source of the methyl
group to convert dUMP into dTMP. Inhibition of DHFR has long been an attractive
goal for the development of chemotherapeutic agents against bacterial and parasitic
infections as well as cancer. The aim of this research study is to locate a novel
synthetic lead compound(s) for future development as DHFR inhibitors. A new series
of quinazoline analogues is designed and fitted with functional groups believed to
enhance the inhibition of the enzyme activity. Thirty seven compounds (including five
unexpected products) belong to the aforementioned nucleus, have been synthesized.
Structure elucidation of the new compounds was fulfilled based on 1H-, 13C-NMR and
Mass spectrometry. The synthesized compounds were evaluated for their in vitro
DHFR inhibition activity at the Department of Pharmacology, College of Pharmacy,
King Saud University and for their in vitro antimicrobial activity at the Department of
Microbiology, Faculty of Pharmacy, University of Mansoura, Egypt.
Compounds 36, 47, 48-51, 53-57, and 59 proved to be the most active
inhibitors of bovine liver DHFR in this investigation with IC50 values of 0.5, 1.0, 0.6,
0.7, 0.9, 0.6, 0.8, 0.4, 1.0, 0.5, 0.6, and 0.5 M, respectively. Structure activity
correlation of the obtained results revealed that, the DHFR inhibition activity is
embedded in the structure core of the investigated compounds. The investigation
findings indicated that the type of substituent at positions 2- and 6- of the studied
quinazolines manipulate the DHFR inhibition activity.
The synthesized compounds (23-59) were also tested for their in vitro
antimicrobial activity against a panel of standard strains of Gram-positive bacteria,
Gram-negative bacteria, and yeast-like pathogenic fungus. The antibacterial
antibiotics Gentamicin, Ciprofloxacin, the DHFR inhibitor Sulphacetamide and the
antifungal drug Clotrimazole were used as positive controls. The results revealed that
compounds 23, 24, 28, 32, 37, 40-42, 44, 47, 49, 51, and 56-59 showed varying
degrees of inhibition against the tested microorganisms. Comparing the potency of the
antibacterial active compounds and their DHFR inhibition results revealed that
compounds 37, 49, and 57-59 might exert their antibacterial activity through DHFR
inhibition. The other compounds 23, 24, 28, 32, 41, 42, and 44 with low DHFR
inhibition might exert their activity through some other mechanism(s).
The synthesized target compounds (23-59) have been comparatively evaluated
in terms of their mode of binding to human dihydrofolate reductase (hDHFR) pocket.
Molecular modeling has been performed for the proposed compounds to evaluate their
recognition profiles at the hDHFR binding-pocket. This study concluded that,
recognition with key amino acid Glu30 is essential for binding and also reflect
promising biological activity. Also, the synthesized target compounds were subjected
to flexible alignment, electrostatic, hydrophobic mappings, and pharmacophore
prediction study. The main pharmacophore groups necessary for activity are: the 4-
carbonyl fragment, the basic nitrogen atom at N-1, and the hydrophobic -system
regions, as well as of their relative distances.
As can be concluded from the obtained results, compounds 3-Benzyl-2-
cinnamylthio-6-methylquinazolin-4(3H)-one (36), N-(3-Benzyl-2-methylthio-4-oxo-
3,4-di-hydroquinazolin-6-yl)-cinnamamide (48), N-(2-allylthio-3-benzyl-4-oxo-3,4-
dihydro-quinazolin-6-yl)-cinnamamide (49), 6-Allylamino-3-benzyl-2-methylthioquinazolin-
4(3H)-one (51), 2-allylthio-3-benzyl-6-diallylamino-quinazolin-4(3H)-one
(54), 3-Benzyl-6-cinnamylamino-2-methylthio-quinazolin-4(3H)-one (56), 3-benzyl-
6-dicinnamylamino-2-methylthio-quinazolin-4(3H)-one (57), 2-allylthio-3-benzyl-6-
dicinnamylamino-quina-zolin-4(3H)-one (59), are the most active members of this
study as DHFR inhibitors with IC50 values of 0.5, 0.6, 0.7, 0.6, 0.4, 0.5, 0.6, and 0.5
uM, respectively.
These studied quinazoline analogues could be considered as useful templates
for future development and further derivatization or modification to obtain more
potent DHFR inhibitors
Synthesis and Biological Evaluation of Some New Thiazolodiazepine Analogues as CNS Active Agents
No full textPhDThe ultra‐short ac ng ac vity of ethyl 8‐oxo‐5,6,7,8‐tetrahydro‐thiazolo[3,2‐a]
[1,3]diazepin‐3‐carboxylate (HIE‐124, 12), as a member of a novel class, which might overcome
many of the disadvantages and problems that usually associated the use of thiopental or
benzodiazepines as intravenous anesthetic agents has been reported.
The present investigation is directed toward the synthesis of new derivatives of the
parent thiazolo[3,2‐a][1,3]diazepine (HIE‐124, 12), in continuation to the previous patented
efforts in this area. These derivatives possess the potential to exhibit a promising and varying
range of CNS activities, including, among others, hypnotic and anticonvulsant activities.
The proposed compounds were synthesized according to the designed strategy.
Structure elucidation of the synthesized intermediates and final products was attained by the
aid of IR, 1H, 13C NMR, and mass spectrometry. The synthesized compounds were evaluated for
various CNS activities.
The new analogues Ethyl 3‐methyl‐8‐oxo‐5,6,7,8‐tetrahydro‐thiazolo[3,2‐a]
[1,3]diazepine‐2‐carboxylate (35) and 2‐Bromo‐3‐methyl‐6,7‐dihydro‐thiazolo[3,2‐a]
[1,3]diazepin‐8(5H)‐one (40) showed marginal hypnotic potency compared to what was
reported about the parent compound HIE‐124 (12).
Biological screening results allowed the allocation of two potent anticonvulsant agents
worth patency. Compounds 35 and 40 proved to be the most active compounds in the present
inves ga on as an convulsants with remarkable 100% protec on against PTZ induced
convulsions as compared with the standard drug valproic acid. It is worth mentioning that
compounds 35 (0.78 mmole/kg) and 40 (0.39 mmole/kg) proved to be almost two and four fold
more ac ve, respec vely; than the used posi ve control sodium valproate (1.38 mmole/kg).
Structure activity correlation of the obtained results revealed that, CNS activity is
embedded in the structure core (8‐oxo‐5,6,7,8‐tetrahydro‐thiazolo[3,2‐a][1,3]diazepine) of the
investigated compounds. Structure activity relationships (SAR) were deduced from the obtained
data.
These studied 8‐oxo‐5,6,7,8‐tetrahydro‐thiazolo[3,2‐a][1,3]diazepine analogues could be
considered as useful templates for future development and further derivatization or
modification to obtain more potent CNS active compounds
Adapting authoritarianism: institutions and co-optation in Egypt and Syria
No full textThis PhD thesis compares Egypt and Syria’s authoritarian political systems. While the tendency in social science political research treats Egypt and Syria as similarly authoritarian, this research emphasizes differences between the two systems with special reference to institutions and co-optation. Rather than reducibly understanding Egypt and Syria as sharing similar histories, institutional arrangements, or ascribing to the oft-repeated convention that “Syria is Egypt but 10 years behind,” this thesis focuses on how events and individual histories shaped each states current institutional strengthens and weaknesses. Specifically, it explains the how varying institutional politicization or de-politicization affects each state’s capabilities for co-opting elite and non-elite individuals.
Beginning with a theoretical framework that considers the limited utility of democratization and transition theoretical approaches, the work underscores the persistence and durability of authoritarianism. Chapter two details the politicized institutional divergence between Egypt and Syria that began in the 1970s. Chapter three and four examines how institutional politicization or de-politicization affects elite and non-elite individual co-optation in Egypt and Syria. Chapter five discusses the study’s general conclusions and theoretical implications.
This thesis’s argument is that Egypt and Syria co-opt elites and non-elites differently because of the varying degrees of institutional politicization in each governance system. Rather than view one country as more politically developed than the other, this work argues that Syria’s political institutions are more politicized than their Egyptian counterparts. Syria’s political arena is, thus, described as politicized-patrimonialism. Syria’s politicized-patrimonial arena produces uneven co-optation of elites and non-elites as they are diffused through competing institutions. Conversely, the Egyptian political arena remains highly personalized as weak institutions and individuals are manipulated and molded according to the president’s ruling clique. This is referred to as personalized-patrimonialism. As a consequence, Egypt’s political establishment demonstrates more flexibility in ad hoc altering and adapting its arena depending on the emergence of crises.
This study’s theoretical implications suggest that, contrary to modernization and democratization theory’s adage that institutions lead to a political development, politicized institutions within a patrimonial order actually hinder regime adaptation because consensus is harder to achieve and maintain. It is within this context that Egypt’s de-politicized institutional framework advantages its top political elite. In this reading of Egyptian and Syrian politics, Egypt’s personalized political arena is more adaptable than Syria’s. These conclusions do not indicate that political reform is a process underway in either state
Conservation in an Islamic context a case study of Makkah
No full textThe Holy Qu’ rān contains many injunctions for Muslims to respect and conserve the natural environment but few address the built environment. Habitat at the time of the Prophet (PBOH) was in the vernacular and relatively impermanent. The first habitat was the cave, the second the tent and then simple flat roofed buildings of post and lintel construction made of mud and rubble. Later buildings were not indigenous but reflected the architectural styles and techniques of Muslim pilgrims from beyond the Arabian Peninsula. Permanent exotic buildings were later erected as reminders of holy places and events. This work advances a case to restore and preserve historic and religious sites in Makkah, Saudi Arabia. Makkah is the destination for millions of Muslim pilgrims who annually pay homage to Allah during the occasions of Hajj, Ramadan and Umra. The tranquillity and peaceful ambience that one associates with the holiest of Islamic experiences have, over the years, given way to jostling crowds of people who must be expediently housed, fed, transported, and protected. Due to the lack of planning and the insensitive but profitable development of the city, Makkah is in grave danger of becoming a bustling metropolis instead of a sanctuary where pilgrims gather to perform their religious rites and reaffirm their dedication to Allah. The author calls for professional planning and international cooperation to guide future development for this expanding and sensitive area. The author's ideas are grounded in practical and aesthetic study, therefore, the political, environmental and economic issues are examined in relationship to religious, historic and artistic values. The author makes proposals for a future Makkah that would provide pilgrims with the physical comforts, security, and serene environment they deserve—without destroying the city they came to visit. The author discusses preservation and conservation in the western world and the need for their acceptance in Muslim countries, the former being an aesthetic and intellectual concept sustained by law and the latter being the prescribed free expression of the individual unhindered by material considerations. Both worlds are rapidly being overwhelmed by materialism, but body, mind and spirit combine in making us aware of our surroundings and the way in what we see around us has come into being
UA-R-GC-1914-01-01-1968-04-19_Page-018
No full text,
I
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TELEPHONE NUMBERS
For information or assistance, please call the following:
President's Office:
Dr. Thomas Bartlett
Mrs. Amina el Lozy
Administrative Assistant
Mr. Feridon Fawzi
Administrative Assistant
Special Sequestrator's Office:
Dr. Hussein Said
Home 34467
Office 21830 or 22969 Ext.137
Home 809344
Office 22969 Ext.139
Home 23645
Home 811113
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For physical disorders of" any kind, please call the following:
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UA-R-GC-1914-01-01-1940-11-15_Page-045
No full text15 Mazhar Said
29 Dr. Taha Hussein Bey
TT
TT
Men Total
155 235
175 225
152 219
184 230
140 162
211 231
95 105
130 160
350 400
1592 1967
334 400
390 431
152
220
160
250
53 56
58 65
48 52
60 63
30 32
1345 1509
102
Appendix III
F O R U M S- 1939 - 40.
T o p i c
First Session
TT
H
Youth & Leisure Time 30
Spiritual & Mental Food
for Youth. 30
355
Second Session
Feb. 12 Saleh Enan Pasha ) First Meeting of Youth
M. Boutros Ghali Bey ) Conference for Social
Mme. Hussein Enan Bey ) Reform
Dr. Hussein Ahmed
19 Dr. Nazmy Bey ) Second Meeting of Youth
Ibnet El-Shati ) Conference for Social
Dr. Ibr. Madkour ) Reform
Galal Hussein )
26 Ahd. Shafik Pasha National Awakening in Egypt
Mar. 4 Fouad Abaza Pasha A Trip to America
Apr. 1 Mazhar Said University & Technical Education
8 Dr. Mohd. Bey Sharaf The Egyptian trace in Relation
to other Races
15 Dr. Aly Bey Hassan Effect of Nutrition on
Improvement of the Race
18 Wahib Bey Doss The Future of the Suez Canal
25 Wahib Bey Doss The Future of the Suez Canal
Average: 1st Session 218
2nd " 168
Date Lecturer
Nov. 27 Miss Asma Fahmy
Dec. 4 Dr. Ahd. Ivlohd. Kamal
11 Mohd. Khalaf Allah
18 Mme. Nazla El-Hakim
Jan. 1 Dr. Ibr.
4 Bahi Ed Din Barakat Pasha
8 Ahd. Mohd. Gad el-Mawla Bey " Youth & Religious Life 10
Problems of Youth: Adolescence 80
IT Puberty 50
Youth & Emotions 67
Youth & Marriage 46
Youth & Reforms 22
Youth & Politics 20
If
It
Women
66
41
8
30
3
7
4
3
2
164
Attendanc
Faculty_1971-75_208
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7
I UNIVERSITY ARCHIVES A. u. C. LIBRARY
HPCQMMPNDAflOHS OP HQMI]WIQHS COMMUTE
At its meeting of October 4, 1971? the Nominations Committee agreed to the- following list for submission to the P'aculty:-Personnel, Policies and procedures Committee
1. hr. Pa^ouk PI-Hitami
2, Dr, Hasan Pl-Shamy 3* Dr. Wadad Said
4. Dr. John Pfdenbeck
5. Dr, Anthony Bryski
6. Dr, Sheila Sl-Mawaziny
Academic Board
1. Dr, Hamdi El-Sakkout
2, Dr. Mahmoud Issa
3« firs . Pnaya Taber
4, Dr, E. H. Yalsan
5. Dr. Pred Hinchey
6, Dr. Kent weeks
7. Dr, Clifford Prator
8. Dr, Hussein fahim
9* Dr. Herbert Aeas
10, Dr . oalah Pi-Din Hami
Safety dissemination messages in VANET and optimized resource management
No full textDr. Ahmad El Hajj, Dr. Hassan ArtailWith the recent technological advancements in vehicular communication, vehicular ad-hoc networks (VANET) have been intensively studied for being a promising approach for reliable dissemination of safety-related messages. VANET who became a key component of the intelligent transportation systems (ITS) will provide a safety environment through early vehicle detection/ collision avoidance systems, cooperative driving and periodic updates on road conditions. The timely exchange of safety information among cars in VANET is of utmost importance. In this context, this thesis provides a mechanism for safety information dissemination that takes into consideration the criticality of the exchanged messages and the optimized usage of uplink and downlink resource in a TDD-LTE framework. vehicle-to-vehicle (V2V), vehicle-to-infrastructure (V2I), and infrastructure-to-infrastructure (I2I) are the main communication techniques deployed in VANET. In this thesis, the main idea is to employ V2V and V2I communications where both systems will cooperate in order to reach the goal which is drivers’ safety. Based on several criteria the communication might be between: (i) I2I communication only, (ii) V2V only, (iii) V2I only, (iv) adaptive V2V-V2I-I2I communication. The main significance of the proposed work is the reconfigurability of the message dissemination architecture based on the actual VANET configuration, traffic conditions, and criticality of messages being relayed. To improve the message delivery process, we used a dynamic LTE resource allocation in which the number of uplink and downlink slots will be set differently every single time based on the joint consideration of traffic volumes and quality of service requirements (delay, rate) in the uplink and downlink. We implemented the proposed work using python and evaluated its performance measuring different parameters. The obtained results are very promising
Els polifenols presents en els aliments com a components funcionals en la prevenció i possible tractament de la hipertensió arterial.
No full text[cat] La hipertensió és un dels principals factors de risc cardiovascular, sent el problema més important de salut pública i la principal causa de mort i discapacitat en els països desenvolupats. El primer pas per a prevenir la hipertensió és seguir una dieta saludable, com és la dieta Mediterrània i millorar l'estil de vida, augmentant l'activitat física o reduint el pes corporal. Diversos estudis epidemiològics relacionen de manera inversa el consum d'aliments rics en polifenols com el cacau, fruites, verdures i hortalisses (F&V), te, oli d'oliva verge, nous o vi, i el risc de mortalitat total o malalties cardiovasculars. L'objectiu principal del present treball ha estat posar a punt i validar la metodologia per a l'anàlisi dels polifenols totals en mostres d'orina i la seva correlació amb la hipertensió i la pressió arterial sistòlica i diastòlica en pacients d'alt risc cardiovascular. S'ha desenvolupat un mètode sensible, específic, ràpid i senzill per a la quantificació de polifenols totals en un gran nombre de mostres d'orina obtinguda de forma puntual, amb un tractament de mostra molt senzill. Aquest mètode és més barat i respectuós amb el medi ambient en utilitzar menys reactius que els mètodes anteriors. La validació del mètode es basa en els resultats obtinguts a partir d'un estudi prospectiu aleatoritzat, creuat, amb diferents períodes d'intervenció i es va corroborar en un estudi transversal amb 60 voluntaris amb una població free-living. En aquests estudis es van trobar associacions positives entre els polifenols totals excretats en l'orina del matí, el consum de polifenols totals i el consum total de F&V; pel que es va poder considerar als polifenols totals excretats en orina com a biomarcador del consum de polifenols totals. S'ha avaluat l'efecte del consum dels polifenols en la hipertensió arterial en 263 homes i 326 dones amb alt risc cardiovascular, amb edats compreses entre 55 i 80 anys, dins d'un sub-estudi transversal amb dades de l'estudi PREDIMED. En els individus en el quartil més alt d'excreció de polifenols totals, el risc d'hipertensió va disminuir en un 36% a comparació amb el quartil més baix d'excreció de polifenols totals. La ingesta de polifenols totals, avaluats a través de la seva excreció en orina, es va associar negativament amb els nivells de pressió arterial sistòlica i diastòlica. En un altre treball es van revisar els principals estudis epidemiològics que relacionen el consum de polifenols totals i la pressió arterial. En l'últim treball es presenta un sub-estudi d'intervenció amb 1139 participants d'alt risc cardiovascular dins de l'estudi PREDIMED. Els participants van ser assignats a una dieta baixa en greix (dieta control), n=379 o a dues dietes estil mediterrània, una suplementada amb oli d'oliva verge, n=394 i l'altra amb fruits secs, n=366. La dieta mediterrània suplementada amb fruits secs o oli d'oliva verge es va correlacionar positivament amb els polifenols totals excretats en les mostres d'orina puntual. Novament els increments estadísticament significatius en l'excreció de polifenols totals, en un estudi d'intervenció, es van associar negativament amb la pressió arterial sistòlica i diastòlica, en una població mediterrània d'avançada edat. Per tant, una intervenció dietètica dirigides a incrementar la ingesta d'aliments rics en polifenols, podria ser eficient en la prevenció i el tractament de la hipertensió, unit a una disminució la pressió arterial, per tal de reduir el seu risc cardiovascular.[eng] "The polyphenols present in food as functional components in the prevention and possible treatment of hypertension". TEXT: Hypertension is a major cardiovascular risk factors, being the most important problem of public health and the leading cause of death and disability in developed countries. The first step to prevent hypertension is to follow a healthy diet as the Mediterranean and improving lifestyle. The main objective of this study was to develop and validate the methodology for the analysis of total polyphenols (TP) in urine samples to evaluate if the TP in urine are correlated with polyphenol intake, to be considered as a marker of intake of these compounds, and its correlation with hypertension and systolic and diastolic blood pressure in patients at high cardiovascular risk. We have developed a sensitive, specific, rapid and simple assay for quantification of polyphenols in a large number of spot urine samples. This method is cheaper and environmentally friendly by using less reactive than previous methods. It was performed a prospective randomized crossover trial and one cross-sectional study with 60 volunteers from the PREDIMED trial. These studies found positive associations between TP excreted in spot urine samples and consumption of TP, and with total fruits and vegetables intake. We evaluated the effect of consumption of polyphenols in arterial hypertension in 589 patients at high cardiovascular risk, within the PREDIMED study. In individuals in the highest quartile of excretion of TP, the risk of hypertension decreased by 36% compared with the lowest quartile. The TP intake assessed by excretion in urine was negatively associated with levels of systolic and diastolic blood pressure. In the sub-intervention study (1139 participants), participants were assigned to a low-fat diet (n=379) or two Mediterranean-style diet. The Mediterranean diet supplemented with nuts (n=366) or virgin olive oil (n=394) were positively correlated with TP content excreted. Statistically significant increases in the excretion of TP were negatively associated with systolic and diastolic blood pressure after the Mediterranean diet supplemented. Therefore, a dietary intervention aimed at increasing the intake of foods rich in polyphenols, may be efficient in the prevention and treatment of hypertension, coupled with a decrease in blood pressure, to reduce their cardiovascular risk
Miscelánea de estudios árabes y hebraicos. Sección Árabe-Islam
No full textNotas bibliográficas contiene: PAREJA, F.M: Islamología. En colaboración con el Dr. Alessandro Bausani y el Dr. Ludwig von Hertling, con un apéndice sobre la Literatura arabigoespañola por el Dr. Elías Terés Sádaba; ABD-EL-JALIL, J: O.F.M: Cristianismo e Islam; IBN SINA, Al-Shifa: La Logique: I. L’Isagoge (al-Madkhal). Préfase de S.E. le Dr. Taha Hussein Pacha. Texte établi par le Dr. Ibrahim Madkour, M. El Khodeiri, G. Anawait, F. El-Ahwani; AL-FARABI: Catálogo de las Ciencias; GUNDISALVO, D: De scientiis. Texto latino establecido por el P. Manuel Alonso, S.J.; IZZEDIN, N: The arab world. Past, present, and future; COON, C.S: Caravan. The Story of the Middle East; THE AMERICAN ANTROPOLOGIST: Studies in Islamic Cultural History; THE AMERICAN ANTROPOLOGIST ISLAM: Essays in the Nature and Growth of a cultural Tradition; RAFAEL CRIADO, S.I: La teología de la historia en el Antiguo Testamento; AUGUSTINUS: Revista trimestral publicada por los PP. Augstinos Recoletos
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