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Address:
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria,
Alexandria 21521, Egypt.
Tel. Univ. +20-3-4871317, Home +20-3-3082926 ,Fax +20-3-4873273
Date & Place of Birth: December 23, 1960, Alexandria, Egypt.
Education:
• 1993, Ph.D. in Pharmaceutical Chemistry, Thesis entitled “ Synthesis of some quinazoline derivatives of potential therapeutic activity ”. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Egypt. Major advisor: Prof. Dr. A. M. Farghaly
• 1989, M. Pharm. in Pharmaceutical Chemistry, Thesis entitled “ Synthesis of some quinazoline derivatives of potential therapeutic activity ” Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Egypt. Major advisor: Prof. Dr. A. M. Farghaly
•1984, B. Pharm. Sci. with general grade distinction honor, Faculty of Pharmacy, University of Alexandria, Egypt.
Post Doctoral Experience:
•May,1993 - present, Faculty member, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Egypt.
• Dec.,1996 - Mar.,1999, Postdoctor Research Fellow, Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan, (Prof. Y. Kiso).
•Jun. - Sept. 1995, Visiting Scientist, SAIC-NCI-FCRDC, Frederick, MD 21702, USA (Dr. John Erickson).
Faculty Appointements:
• 2000 - present, Assistant Professor, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria 21521, Egypt.
• 1993 - 2000, Lecturer, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria 21521, Egypt.
• 1990 - 1993, Assistant Lecturer, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria 21521, Egypt.
• 1984 - 1989, Teaching Assistant, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria 21521, Egypt.
Areas of Expertise and Research Activities:
• Univ. Alex., Design, synthesis and in vitro/in vivo evaluation of new pharmacologically active compounds, e.g. Anti-inflammatory, Antimicrobial, cardiotonic and anticaner. Teaching of Pharmaceutical Organic Chemistry, Pharmaceutical Chemistry, Medicinal Chemistry courses for undergraduate and graduate students as well as continuing education courses for medical professions. Supervision of Master and Ph.D. students. I used to apply and teach multi-step synthesis together with modern synthetic methods and analytical techniques (NMR, HPLC, MS…etc.). Laboratory and research projects management.
•Beirut Arab University, Visiting faculty member, Faculty of Pharmacy, Sept. – Dec., 1999 and Mach – May, 2005.
• NCI-FCRDC, Structure based drug design as C2 symmetry-based, conformationally-constrained HIV protease inhibitors applying modern synthetic methods and analytical techniques. CADD, using SYBYL molecular modeling package.
• Kyoto Pharm. Univ., Design and synthesis of peptidomimetic HIV protease inhibitors applying modern synthetic methods and analytical techniques. A number of highly potent HIV protease inhibitors was developed by the modification of the lead compounds KNI 272 and KNI 764 ( now is AG 1775) which are in clinical trials. Supervision of undergraduate and graduate students.
Awards:
1. 2004, Alexandria University prize for scientific encouragement.
2. 2001, Silver Medal for Merit, General Egyptian Syndicate of Pharmacists.
3. 2000, Medal of Scientific Advances, Alexandrian Syndicate of Pharmacists.
4. 1999, Full Resident Scholarship to the 1999 Residential School on Medicinal Chemistry, Drew University, Madison, NJ 07940-4037.
5. 1992, Arab Scientific Innovation Prize in Chemistry.
6. 1993, Medal for Merit of the General Egyptian Syndicate of Pharmacists.
7. 1984, Faculty of Pharmacy Recognition Award for Social and Scientific Activities.
Professional Socities:
1. Egyptian Pharmaceutical Society.
2. Japanese Peptide Society.
3. American Chemical Society, Division of Medicinal Chemistry.
4. General Egyptian Syndicate of Pharmacists.
5. Scientific Society of The Faculty of Pharmacy, Alexandria University.
6. Scientific Society of Students Hospital, Alexandria University.
Publications:
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Novel 1H-Pyrazole Derivatives as
Anti-inflammatory-Antimicrobial Agents. Bekhit A. A. and
Abdel-Azeim T.,
Bio-Medical Materials and Engineering
(submitted).
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Novel milrinone analogs of pyridine-3-carbonitrile derivatives as
promising cardiotonic agents ,
. Bekhit A. A. and Baraka A. M., Eur. J. Med. Chem.
(in press).
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Synthesis and biological evaluation of some pyridine-3-carbonitrile
derivatives as cardiotonic agents,
Bekhit A. A. and Baraka A. M.,
Boll. Chim. Farmac.
(in press).
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Synthesis of some thiazolidine derivatives of 1,4-benzoquinone as
potential antimicrobial agents, Chaaban I., Bekhit A. A.,
El-Sayed, Aboulmaged E., Assiut Bull.
Pharm. Sci., 28, 1-7 (2005).
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Novel Pyrazole Derivatives as Potential Promising Anti-inflammatory
Antimicrobial Agents, Bekhit A. A., Ashour H. M., Gumei A.
A., Arch. Pharm. Chem. Life Sci., 338, 167- 174 (2005).
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Evaluation of some pyrazoloquinolines as inhibitors of herpes
simplex virus type 1 replication, Bekhit A. A., El-Sayed O.
A., Aboul-Enein H. Y., Siddiqui Y. M., Al-Ahdal M. N, Arch.
Pharm. Chem. Life Sci., 338, 74 – 77 (2005).
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Coupling Reactions of Hydralazine
with Amino Acids and their Adducts for Antihypertensive Activities,
Khattab S. N., El Massry A. M., El-Faham A., Bekhit A. A.,
Amer A., Hetrocyl. Chem., 41, 387 (2004) .
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Synthesis, Characterization and Cytotoxicity Evaluation of Some new
Platinum(II) Complexes of Tetrazolo[1,5-a]quinolines,
Bekhit A. A., El-Sayed O. A., Al-Allaf T. A. K., Abou-Enein H.
Y., Kunhi M., Subramanian M., Al-Hussian K., El-Khodairy F., Arif
J., Eur. J. Med. Chem., 39, 499-505 (2004).
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Synthesis of Some Thiazolyl and Thiadiazolyl Derivatives of
4(3H)-Quinazolinone as Anti-inflammatory-Antimicrobial Agents,
Bekhit A. A., Habib N. S., Park J. Y., Boll. Chim. Farmac.,143,
34-39 (2004).
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Tetrazolo[1,5-a]quinoline as a Potential Promising New Scaffold for
the Synthesis of Novel Anti-inflammatory and Antibacterial Agents,
Bekhit A. A., El-Sayed O. A., Aboulmaged E., Park J. Y.,
Eur. J. Med. Chem. 39, 249-255 (2004)..
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Design, Synthesis and Biological Evaluation of Some Pyrazole
Derivatives as Anti-inflammatory-Antimicrobial Agents, Bekhit A.
A.., Abdel-Azeim T., Bioorg. Med. Chem. 12, 1935-1945
(2004).
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Synthesis of aldehydo-sugar derivatives of pyrazoloquinoline as
inhibitors of herpes simplex virus type 1 replication, Bekhit A.
A., El-Sayed O. A., and Aboul-Enein H. Y.,
Siddiqui Y. M., Al-Ahdal M. N,
J. Enzyme inhib. Med. Chem.
19, 33-38 (2004)..
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Synthesis and Biological Evaluation of Some New Substituted
Naphthoquinones, Habib N. S., Bekhit A. A., Park J. Y.,
Boll. Chim. Farmac. 142, 232 (2003).
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Design and Synthesis of Some Substituted 1H-Pyrazolyl
Oxazolidines or 1H-Pyrazolyl Thiazolidines as
Anti-inflammatory-antimicrobial Agents. Bekhit A. A., Fahmy
H. T. Y., Archiv Pharm. Pharm. Med. Chem. 336, 111 (2003).
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Design and Synthesis of Some Substituted 1H-Pyrazolyl
Thiazolo[4,5-d]Pyrimidines as Anti-inflammatory-antimicrobial
Agents. Bekhit A. A., Fahmy H. T. Y., Rostom S. A. F., Baraka
A. M., Eur. J. Med. Chem. 38. 27 (2003).
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Thioglycolic Acid and Pyrazole Derivatives of 4(3H)-Quinazolinone:
Synthesis and Antimicrobial Evaluation, Farghaly A. M., Soliman R.,
Khalil M. A., Bekhit A. A., Bekhit A. E. A., Boll. Chim.
Farmac, 141, 372 (2002).
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Synthesis of some new Bis-thiazoles as possible anticancer agents.,
FahmyH. T. Y., Bekhit A. A., Pharmazie 57,
800 (2002).
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Synthesis and Antitumor Evaluation of New Polysubstituted Thiazole
and Derived Thiazolo[4,5-d]pyrimidine Systems, Fahmy H. T. Y.,
Rostom S. A. F, Bekhit A. A., Archiv Pharm. Pharm. Med.
Chem. 335, 213 (2002).
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Synthesis and Antimicrobial Evaluation of Chalcone and Sydnone
Derivatives of 4(3H)-Quinazolinone, Bekhit A. A., Habib N.
S., Bekhit A. E. A., Boll. Chim. Farmac., 140, 297 (2001).
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Fused Cinnolines: Synthesis and Biological Activity, Bekhit A. A.,
Boll. Chim. Farmac., 140, 243 (2001).
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Synthesis of 2,5-Disubstituted –1,4-benzoquinone Derivatives as
Potential Antimicrobial Agents, Bekhit A. A., Chaaban I.,
Abdel-Ghany Y. S., Proceedings of Assiut University 2nd
Pharmaceutical Sciences Conference, 8-9 March, 2000, pp.107-114.
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Design and Synthesis of Some Oxadiazolyl, Thiadiazolyl,
Thiazolidinyl and Thiazolyl Derivatives of 1H-Pyrazole as
Anti-inflammatory Antimicrobial Agents, Farghaly A. M., Bekhit
A. A., Park J. Y., Archiv Pharm. Pharm. Med. Chem.,
333,
53 (2000).
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Allophenylnorstatine containing HIV-1 protease inhibitors: design,
synthesis and structure-activity relationships for selected P2 and
P2' ligands, Bekhit A. A., Matsumoto, Abdel-Rahman H. M. M.,
Mimoto T., Nojima S., Takaku H., Kimura T., Akaji K., and Kiso Y.,
Y. Shimonishi (ed): Peptide Science Present and Future, 660-661,
1999, Kluwer Academic Publisher, Great Britain.
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Allophenylnorstatine containing HIV-1 protease inhibitors: design,
synthesis and structure-activity relationships for selected P2
ligands, Abdel-Rahman H. M. M., Matsumoto H., Bekhit A. A.,
Mimoto T., Nojima S., Takaku H., Kimura T., Akaji K., Kiso Y.,
Y. Shimonishi (ed): Peptide Science Present and Future, 662-664,
1999, Kluwer Academic Publisher, Great Britain.
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Synthesis of Novel Benzoquinone and Hydroquinone Derivatives Bearing
Different Heterocyclic Systems as Potential Antimicrobial Agents,
Chaaban I., Bekhit A. A., Abdel-Ghany Y. S..
Egypt. J.
Pharm. Sci., 39, No. 1-3, 91(1998).
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Non-Steroidal anti-inflammatory agents: Synthesis of novel
benzopyrazolyl, benzoxazolyl and quinazolinyl derivatives of
4(3H)-quinazolinones, Bekhit A. A., Khalil M. A.,
Pharmazie 53, 539(1998).
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Novel Thiazolidinyl-4(3H)-quinazolinones as Potential Antimicrobial
Agents, Farghaly A. M., Soliman R., Khalil M. A., Bekhit A. A.,
Alex. J. Pharm. Sci. 11(2), 69(1997).
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Anticonvulsant and Hypnotic Agents: Novel Thiobarbituric acid
Derivatives of 4(3H)-Quinazolinones, Farghaly A. M., Soliman R.,
Khalil M. A., Bekhit A. A., El-Mallah A. I., Alex. J.
Pharm. Sci. 11(1), 37(1997).
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Synthesis and Antimicrobial Evaluation of Some Quinazolinone
Derivatives, Bekhit A. A., Bull. Pharm. Sci. Assiut
University, 18(2), 107(1995).
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Non-Steroidal Anti-inflammatory Agents: Synthesis of Novel
Pyrazolyl-, 1,2 -Oxazolyl-, and 1,3-Diazinyl Derivatives of
4(3H)-Quinazolinones. Farghaly A. M., Soliman R., Khalil M. A.,
Bekhit A. A., Arch. Pharm. (Weinheim) 327, 27(1994).
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Non-Steroidal Anti-inflammatory Agents. III: Synthesis of Novel
Pyrazole Derivatives of 4(3H)-Quinazolinones, Farghaly A. M.,
Chaaban I., Khalil M. A., Bekhit A. A.,
Alex. J. Pharm.
Sci. 4(1), 52(1990).
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Non-Steroidal Antiinflammatory Agents, Synthesis of Novel
2-Pyrazolyl-4(3H)-Quinazolinones. Farghaly A. M., Chaaban I., Khalil
M. A., Bekhit A. A., Arch. Pharm. (Weinheim) 323,
833(1990).
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Non-Steroidal Antiinflammatory Agents, II: Synthesis of Novel
Pyrazole and Pyrazoline Derivatives of 4(3H)-Quinazolinone, Farghaly
A. M., Chaaban I., Khalil M. A., Bekhit A. A., Arch. Pharm.
(Weinheim) 323, 311(1990).
Patents
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Design, Synthesis and Biological
Evaluation of Some Pyrazole Derivatives as
Anti-inflammatory-Antimicrobial Agents, A. A. Bekhit,
Egyptian Patent, GATT / TRIPS Treaty, Appl. No. 1117 12 2003.
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Design, synthesis and cardiotonic
evaluation of some pyridinone derivatives and their 2-Amino
isosteres, A. A. Bekhit, Egyptian Patent, GATT / TRIPS
Treaty, Appl. No. 289 6 2004.
Participation in National and International Conferences or Symposia
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Novel Pyrazole Derivatives as Anti-inflammatory-Antimicrobial
Agents; Synthesis ans Optimum Dosing in Experimental Animals,
Adnan A. Bekhit, Elsayed Aboulmagd and Azza M. Baraka, World
Conference on Dosing of Antiinfectives, Nürnberg, Germany, Sept.
9-11th, 2004 ( Invited Participant).
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Biovision Alexandria 2004, Bibliotheca Alexandrina, conference
Center, April 3-6th, 2004 ( Invited Participant).
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NOVEL PYRAZOLE DERIVATIVES AS A POTENTIAL PROMISING
ANTI-INFLAMMATORY-ANTIMICROBIAL AGENTS, Adnan A. Bekhit,
Hayam M. A. Ashour, Aida A. Guemei,
Assuit University 3rd
Pharmaceutical Sciences Conference, Faculty of Pharmacy, Assuit,
Egypt, March 6-7th,2004, P 90.
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Synthesis of some thiazolidine derivatives of 1,4-benzoquinone as
potential antimicrobial agents, I. Chaaban, A. A. Bekhit, E.
Aboulmagd,
Assuit
University 3rd Pharmaceutical Sciences Conference,
Faculty of Pharmacy, Assuit, Egypt, March 6-7th,2004, P
91.
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Novel 1H-Pyrazole Derivatives as
Promising Anti-inflammatory-Antimicrobial Agents. Adnan A. Bekhit
and Tarek Abdel-Azeim, Second International Conference on
Chemistry and its Applications, Doha, Qatar, Dec. 6-9th,
2003, Abst. L 471.
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Novel 1H-Pyrazole Derivatives as
Anti-inflammatory-Antimicrobial Agents. Adnan A. Bekhit and Tarek
Abdel-Azeim, Second International Conference on New Biomedical
Materials, Cardiff, Wales, UK, 5-8th April, 2003.
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Synthesis and Biological Evaluation of Some New Substituted
Naphthoquinones, N. S. Habib and A. A. Bekhit,
The First
International Congress of Pharmaceutical and Drug Industries
Division, National Research Center, Cairo, Egypt, March 24-26th,
2003, Abst. P40.
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Design and Synthesis of Some 1H-Pyrazole Derivatives as
Anti-inflammatory-Antimicrobial Agents. Adnan A. Bekhit,
Hesham T. Y. Fahmy, Sherif A. F. Rostom and Tarek Abdel-Aziem,
XXVIII International Conference of Pharmaceutical Sciences, Cairo,
Egypt, Dec. 17-19th, 2002, Abst. P 81.
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New agents for treating contact dermatitis associated with petroleum
industry. Adnan A. Bekhit, Ola A. El-Sayed, Fayrouz K. Badran
and Azza M. Baraka, 5Th International Conference &
Exhibition on Chemistry in Industry, Manama, Bahrain, 14-16th
October, 2002, PP No. WAT-P6.
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Design, synthesis and cardiotonic evaluation of
4-aryl-6-(4-pyridyl)-3-cyano-2(1H)-pyridinones and their 2-imino
isosteres. Adnan A. Bekhit and Azza M. Baraka, 14th
International Conference on Organic Synthesis, Christchurch, New
Zealand, 14-18th July, 2002, Abst. P114.
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Design and Synthesis of Some 1H-pyrazolyl Derivatives of
Thiazolo[4,5-d]pyrimidines as anti-inflammatory Antimicrobial
agents. Adnan A. Bekhit, Hesham T. Y. Fahmy, Sherif A. F.
Rostom and Azza M. Baraka, Assuit University 3rd
Pharmaceutical Sciences Conference, Faculty of Pharmacy, Assuit,
Egypt, March 5-6th,2002, P 60.
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Design, Synthesis and Biological Evaluation of Some Pyrazole
Derivatives as Anti-inflammatory Antimicrobial Agent. Adnan A.
Bekhit, Al-Azhar 2nd International Conference for
Pharmaceutical and Biological Sciences, Cairo, Egypt, 19-21st
Dec. 2001, Abst. P 34.
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Pyrimidyl Derivatives of Tetrazoloquinoline as Promising
Pharmacologically Active agents. OLA. A. EL-SAYED, ADNAN A.
BEKHIT AND YOUSRY M. GOHAR, Al-Azhar 2nd
International Conference for Pharmaceutical and Biological Sciences,
Cairo, Egypt, 19-21st Dec. 2001, Abst. P 44.
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4(3H)-Quinazolinone Derivatives: Synthesisand Antimicrobial
Evaluation. A. A. Bekhit, A. M. Farghaly, R. Soliman
and M. A. Khalil, The Eighth International Kyoto Conference on
New Aspects of Organic Chemistry (IKCOC-8), Kyoto, Japan,
July 11-15th, 2000. Abst. PP 279.
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Design and Synthesis of Some Thienylpyrazole Derivatives as
Anti-inflammatory Antimicrobial Agents. Adnan A. Bekhit, 7th
Ibn Sina International Conference on Pure and Applied Heterocyclic
Chemistry, Alexandria, Egypt, 25-28th March 2000, Abst.
P 350.
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Synthesis of 2,5-Disubstituted –1,4-benzoquinone Derivatives as
Potential Antimicrobial Agents. A. A. Bekhit, I.
Chaaban and Y. S. Abdel-Ghany, Assiut University 2nd
Pharmaceutical Sciences Conference, Assiut, Egypt, 8-9th
March, 2000, Abst. pp 104.
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Allophenylnorstatine containing HIV-1 protease inhibitors: design,
synthesis and structure-activity relationships for selected P2 and
P2' ligands. Adnan A. Bekhit, Hikaru Matsumoto, Hamdy M. M.
Abdel-Rahman, Tsutomu Mimoto, Satoshi Nojima, Harou Takaku, Tooru
Kimura, Kenichi Akaji and Yoshiaki Kiso, First International
Peptide Symposium, Kyoto, Japan, Nov.30 – Dec.5th, 1997,
Abst. P 205.
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Allophenylnorstatine containing HIV-1 protease inhibitors: design,
synthesis and structure-activity relationships for selected P2
ligands. Hamdy M. M. Abdel-Rahman, Hikaru Matsumoto, Adnan A.
Bekhit, Tsutomu Mimoto, Satoshi Nojima, Harou Takaku, Tooru
Kimura, Kenichi Akaji and Yoshiaki Kiso, First International
Peptide Symposium, Kyoto, Japan, Nov.30 – Dec.5th, 1997,
Abst. P 206.
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Small-sized HIV protease inhibitors
containing the hydroxymethylcarbonyl isostere as an ideal
transition-state mimic. Yoshiaki Kiso, Hikaru Matsumoto, Tsutomu
Mimoto, Ryohei Kato, Satoshi Nojima, Haruo Takaku, Tominaga
Fukazawa, Keisuke Terashima, Adnan A. Bekhit, Tooru Kimura,
Kenichi Akaji., International Conference on protease Inhibitors
’97, Kyoto, Japan, 4 Dec. 6th, 1997, Abst. L 12.
Participation in National and International
Seminars or Workshops
1. Pre-Conference
workshops of the ‘World Conference on Dosing of Antiinfectives, Nürnberg,
germany, Sept. 6-8th
2004 (Invited Participant).
2.
The Use of
Crystallography in Genes Drug Design. The Egyptian Society of
Crystallography and Applications,
Ain
Shams University, Jan. 19th, 2003.
3.
“Chemical Diversity”
Generation and Use in Drug Discovery.
Alexandria university, 10/2002, Invited speaker.
4. Small-sized HIV
protease inhibitors containing the hydroxymethylcarbonyl isostere as an
ideal transition-state mimic.
Lincoln
university, Canterbury, New Zealand, 7/2002. Invited speaker.
5. Fused cinnolines:
synthesis and biological activity.
Alexandria university, 4/2002, Invited speaker.
6. Recent advances in the
treatment of AIDS.
Alexandria
university, 2/2002, Invited speaker.
7. Solutions and
Integrated Platforms for Bioinformatics, Cheminformatics and Modeling,
Workshop, Center of Applied Research and Advanced Studies, Faculty of
Pharmacy, Cairo universitry with collaboration with Accelrys.
Jun.
11th, 2001,Cairo, Egypt.
8. Recent Trends in
Developing HIV Inhibitors,
Alexandria
university, 3/2000. Invited speaker.
9. Transponder Technology
and SynPhase crowns, Workshop with the collaboration with Chiron
Technologies, Kyoto Pharmaceutical
University, 5/98.
10.
Small-sized HIV
protease inhibitors containing the hydroxymethylcarbonyl isostere as an
ideal transition-state mimic. Korea Research Institute of Chemical
Technology, Daejon, Korea, 4/98.
Invited Speaker.
11.
Small-sized HIV
protease inhibitors containing the hydroxymethylcarbonyl isostere as an
ideal transition-state mimic. Sookmyung Women’s University,
Seoul, Korea, 4/98. . Invited Speaker.
12.
Quinazoline
Derivatives as Antimicrobial and Anti-inflammatory Agents, , Department
of Medicinal Chemistry,
Kyoto
Pharmaceutical University, 6/96. Invited Speaker.
13.
Design and Screening
of Antimicrobial and Anti-inflammatory Agents, SAIC-NCI-FCRDC,
Frederick, MD 21702, 8/95. Invited Speaker.
14.
Pharmacokinetics of
Drugs, SAIC-NCI-FCRDC,
Frederick, MD
21702, 7/95. Invited Speaker.
15.
Drug Interactions, Students
Hospital of Alexandria University, 3/95. Invited Speaker.
Email: mmohyeldin1@hotmail.com
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