Basic Informations

C.V

Name: Eman Kamal Ahmed Abdelall EDUCATIONAL QUALIFICATIONS: April 2006 Ph.D. Pharmacutical organic chemistry December 2005 Cairo University, Benisuief Branch, Egypt November 1997 Masters Pharmacutical organic chemistry Cairo University, Benisuief Branch, Egypt May 1993 B. Sc. Pharmacy (Honors) Assiut University, Assiut, Egypt HONORS AND AWARDS: May 1991: B. Pharm. Sci. with distinction honors, third position, Assiut University, Egypt. POSITIONS HELD: March 2018: Professor, Department of Pharmaceutical organic chemistry, School of Pharmacy, Beni-Suef Univ MAy 2016-Now: Chair of the department of pharmaceutical organic chemistry, School of Pharmacy, Beni-Suef Univ., Beni-Suef, Egypt. Jan 2013 Associated Professor, pharmaceutical organic chemistry, School of Pharmacy, Beni-Suef Univ. Jan 2006: Lecturer, Department of pharmaceutical organic chemistry, School of Pharmacy, Beni-Suef Univ., Beni-Suef, Egypt. August 2001-Jan 2006: Lecturer assistant in of Pharmacy, Beni-Suef Univ. Dec1995-August 2000: Research and Teaching Assistant School of Pharmacy, Beni-Suef Univ., School of Pharmacy, University Beni-Suef, Egypt

Master Title

Synthesis of some novel pyridinethione nucleoside of expected chemotherapeutic effect

Master Abstract

The present investigation comprises a survey covering the synthesis and biological importance of many imidazo and oxazolo[4,5-b]pyridines. The thesis involves the preparation of 2,3-diaminopyridine (VIIa) and 2-amino-3-hydroxypyridine (VIIb) and their reaction with p-aminobenzoic to give the imidazo and oxazolopyridines VIIIa,b. The latter were halogenated to afford VIIIc-h. The imidazo and oxazolopyridines VIIIa-h were aceylated with acetyl chloride, chloroacetyl chloride, dichloroacetyl chloride and benzoyl chloride to give the corresponding acylated derivatives IXa-h, XIa-h, XIIa-h and XIIIa-h. The diacetyl derivatives Xa-d were also synthesized. On the other hand, the imidazo and oxazolopyridines VIIIa-h were diazotized and the diazonium salts of VIIIa,b were reacted with diethylmalonate to give XIVa,b. The latter were condensed with two hydrazines to give the cyclized products XVa-d. The intermediates XIVa,b were also reacted with urea and thiourea to give the cyclized derivatives XVIa-d. Moreover, the diazonium salts of VIIIa,b,g and h were reacted with malononitrile to afford the dicyano derivatives XVIIa-d. The latter when condensed with hydrazine afforded compounds XVIIIa-d. In addition a number of azo dyes of imidazo and oxazolopyridines were also, synthesized XIXa-v via coupling of the diazonium salts of VIIIa-h with different phenolic compounds. The azo dyes XIXa,f,o and p were acetylated to give the corresponding acetyl derivatives XXa-d. The investigation comprises also the reaction of VIIIa-h with different aromatic aldehydes to give arylidine derivatives XXIa-v. Some of the latter were reacted with chloroacetyl chloride to yield ß-lactam containing derivatives XXIIa-d and with thioglycolic acid to give compounds XXIIIa-d. Additionally some of these new imidazo and oxazolo[4,5-b]pyridine derivatives were subjected to antimicrobial screening and molecular modeling study. The study includes the synthesis of certain unavailable starting and intermediates materials: 1) Ethyl pyridine-3-carboxylate (Ethyl nicotinate) (I). 2) Pyridine-3-carboxhydrazide (Nicotinhydrazide) (II). 3) 3-Ethoxycarbonylaminopyridine (III). 4) 3-Ethoxycarbonylamino-2-nitropyridine (IV). 5) 3-Amino-2-nitropyridine (V). 6) 2,3-Diaminopyridine (VIIa). 7) 3-Hydroxy-2-nitropyridine (VI). 8) 2-Amino-3-hydroxypyridine (VII b). 9) 2-(4-Aminophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIIIa,b. The thesis includes also the synthesis of certain new intermediates and final products: 1) 2-(4-Amino-3-iodophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIIIc,d. 2) 2-(4-Amino-3-chlorophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIIIe,f. 3) 2-(4-Acetamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines IXa,b. 4) 2-(4-Acetamido-3-bromophenyl)imidazo(or oxazolo)[4,5-b]pyridines IXc,d. 5) 2-(4-Amino-3-bromophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIII g,h. 6) 2-(4-Acetamido-3-halophenyl)imidazo(or oxazolo)[4,5-b]pyridines IXe-h. 7) 2-(4-Diacetylaminophenyl)oxazolo[4,5-b]pyridines (Xa-d). 8) 2-(4-Chloroacetamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines XIa-h. 9) 2-(4-Dichloroacetamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines XIIa-h. 10) 2-(4-Benzamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines XIIIa-h. 11) 2-{4-[N2(Bis(ethoxycarbonyl)methylene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XIVa,b. 12) 2-{4-[N2-(3,5-Dioxopyrazolidin-4-ylidene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XVa-d. 13) 2-{4-[N2-(2,4,6-Trioxoperhydropyrimidin-5-ylidene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XVIa,c. 14) 2-{4-[N2-(4,6-Dioxo-2-thioxoperhydropyrimidin-5-ylidene)hydrazino]phenyl} imidazo (or oxazolo )[4,5-b]pyridines XVIb,d. 15) 2-{4-[N2(Bis(cyano)methylene)hydrazino]phenyl}imidazo(or oxazolo) [4,5-b]pyridines XVIIa-d. 16) 2-{4-[N2-(3,5-Diaminopyrazol-4-ylidene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XVIIIa-d. 17) 2-[4-Arylazophenyl]imidazo(or oxazolo)[4,5-b]pyridines XIXa-v. 18) 2-[4-(4-acetoxyphenyl)azophenyl]imidazo(or oxazolo)[4,5-b]pyridines XXa-d. 19) 2-[4-Arylidenaminophenyl]imidazo(or oxazolo)[4,5-b]pyridines XXIa-v. 20) 2-[4-(3-Chloro-2-oxo-4-substituted phenylazetidin-1-yl)phenyl]imidazo (or oxazolo)[4,5-b]pyridines XXIIa-d. 21) 2-[4-(4-oxo-2-subsituted phenylthiazolidin-3-yl)phenyl]imidazo (or oxazolo)[4,5-b]pyridines XXIIIa-d. The structure of the new compounds was substantiated from elemental analysis as well as IR and in certain cases 1H-NMR and mass spectra.

PHD Title

synthesis of many imidazo and oxazolo[4,5-b]pyridines with a biological importance

PHD Abstract

The present investigation comprises a survey covering the synthesis and biological importance of many imidazo and oxazolo[4,5-b]pyridines. The thesis involves the preparation of 2,3-diaminopyridine (VIIa) and 2-amino-3-hydroxypyridine (VIIb) and their reaction with p-aminobenzoic to give the imidazo and oxazolopyridines VIIIa,b. The latter were halogenated to afford VIIIc-h. The imidazo and oxazolopyridines VIIIa-h were aceylated with acetyl chloride, chloroacetyl chloride, dichloroacetyl chloride and benzoyl chloride to give the corresponding acylated derivatives IXa-h, XIa-h, XIIa-h and XIIIa-h. The diacetyl derivatives Xa-d were also synthesized. On the other hand, the imidazo and oxazolopyridines VIIIa-h were diazotized and the diazonium salts of VIIIa,b were reacted with diethylmalonate to give XIVa,b. The latter were condensed with two hydrazines to give the cyclized products XVa-d. The intermediates XIVa,b were also reacted with urea and thiourea to give the cyclized derivatives XVIa-d. Moreover, the diazonium salts of VIIIa,b,g and h were reacted with malononitrile to afford the dicyano derivatives XVIIa-d. The latter when condensed with hydrazine afforded compounds XVIIIa-d. In addition a number of azo dyes of imidazo and oxazolopyridines were also, synthesized XIXa-v via coupling of the diazonium salts of VIIIa-h with different phenolic compounds. The azo dyes XIXa,f,o and p were acetylated to give the corresponding acetyl derivatives XXa-d. The investigation comprises also the reaction of VIIIa-h with different aromatic aldehydes to give arylidine derivatives XXIa-v. Some of the latter were reacted with chloroacetyl chloride to yield ß-lactam containing derivatives XXIIa-d and with thioglycolic acid to give compounds XXIIIa-d. Additionally some of these new imidazo and oxazolo[4,5-b]pyridine derivatives were subjected to antimicrobial screening and molecular modeling study. The study includes the synthesis of certain unavailable starting and intermediates materials: 1) Ethyl pyridine-3-carboxylate (Ethyl nicotinate) (I). 2) Pyridine-3-carboxhydrazide (Nicotinhydrazide) (II). 3) 3-Ethoxycarbonylaminopyridine (III). 4) 3-Ethoxycarbonylamino-2-nitropyridine (IV). 5) 3-Amino-2-nitropyridine (V). 6) 2,3-Diaminopyridine (VIIa). 7) 3-Hydroxy-2-nitropyridine (VI). 8) 2-Amino-3-hydroxypyridine (VII b). 9) 2-(4-Aminophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIIIa,b. The thesis includes also the synthesis of certain new intermediates and final products: 1) 2-(4-Amino-3-iodophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIIIc,d. 2) 2-(4-Amino-3-chlorophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIIIe,f. 3) 2-(4-Acetamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines IXa,b. 4) 2-(4-Acetamido-3-bromophenyl)imidazo(or oxazolo)[4,5-b]pyridines IXc,d. 5) 2-(4-Amino-3-bromophenyl)imidazo(or oxazolo)[4,5-b]pyridines VIII g,h. 6) 2-(4-Acetamido-3-halophenyl)imidazo(or oxazolo)[4,5-b]pyridines IXe-h. 7) 2-(4-Diacetylaminophenyl)oxazolo[4,5-b]pyridines (Xa-d). 8) 2-(4-Chloroacetamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines XIa-h. 9) 2-(4-Dichloroacetamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines XIIa-h. 10) 2-(4-Benzamidophenyl)imidazo(or oxazolo)[4,5-b]pyridines XIIIa-h. 11) 2-{4-[N2(Bis(ethoxycarbonyl)methylene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XIVa,b. 12) 2-{4-[N2-(3,5-Dioxopyrazolidin-4-ylidene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XVa-d. 13) 2-{4-[N2-(2,4,6-Trioxoperhydropyrimidin-5-ylidene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XVIa,c. 14) 2-{4-[N2-(4,6-Dioxo-2-thioxoperhydropyrimidin-5-ylidene)hydrazino]phenyl} imidazo (or oxazolo )[4,5-b]pyridines XVIb,d. 15) 2-{4-[N2(Bis(cyano)methylene)hydrazino]phenyl}imidazo(or oxazolo) [4,5-b]pyridines XVIIa-d. 16) 2-{4-[N2-(3,5-Diaminopyrazol-4-ylidene)hydrazino]phenyl}imidazo (or oxazolo)[4,5-b]pyridines XVIIIa-d. 17) 2-[4-Arylazophenyl]imidazo(or oxazolo)[4,5-b]pyridines XIXa-v. 18) 2-[4-(4-acetoxyphenyl)azophenyl]imidazo(or oxazolo)[4,5-b]pyridines XXa-d. 19) 2-[4-Arylidenaminophenyl]imidazo(or oxazolo)[4,5-b]pyridines XXIa-v. 20) 2-[4-(3-Chloro-2-oxo-4-substituted phenylazetidin-1-yl)phenyl]imidazo (or oxazolo)[4,5-b]pyridines XXIIa-d. 21) 2-[4-(4-oxo-2-subsituted phenylthiazolidin-3-yl)phenyl]imidazo (or oxazolo)[4,5-b]pyridines XXIIIa-d. The structure of the new compounds was substantiated from elemental analysis as well as IR and in certain cases 1H-NMR and mass spectra.