ORGANIC SYNTHESIS/MEDICINAL CHEMISTRY RESEARCH GROUP

ORGANIC SYNTHESIS/MEDICINAL CHEMISTRY RESEARCH GROUP

DEPARTMENT OF PURE AND INDUSTRIAL CHEMISTRY

CONCEPT/JUSTIFICATION:

From the traditional applications of phenothiazines and phenoxazines as dyes and pigments, these compounds have gained prominent place in medicines as pharmacologically lead structures. In addition, sulphonamides were the first efficient antibiotic drug employed systematically for the prevention and cure of bacterial infections. Recent reviews and reports had demonstrated that various synthesized derivatives of phenothiazines, phenoxazines and sulphonamides exhibited promising antibacterial, antifungal, anticancer, anti-inflammatory, anticonvulsant, analgesic, immunosuppressive, anti-malaria activities amongst other properties. Natural products have always being the starting point of any drug discovery and as such remains a focal point in medicinal chemistry research.

The vast medicinal applications of phenothiazines, phenothiazines and sulphonamides have prompted unprecedented exploratory modification of the parent structure via organic synthesis with a view of synthesizing novel derivatives with improved or new biological activities. Moreover, the growing incidence of microbial resistance to currently used antibiotics represents a serious health problem. There is, therefore, need to develop new classes of therapeutic agents to combat microbial infections and other health challenges.

Research Focus:

Applications of classical and modern organic synthetic methodologies in the synthesis and functionalization/derivatization of novel phenothiazine, phenoxazine and sulphonamide motifs.
Structure activity relationship studies of newly synthesized derivatives.
Isolation, purification, structural elucidation and total synthesis of bioactive components from plant material

Research topics:

Synthesis of new complex phenothiazines and phenoxazines.
Functionalization/Derivatization of known phenothiazines and phenoxazines ring system via transition metal catalyzed tandem reactions.
Structural activity relationship study of functionalized/derivatized phenothiazine ring system
Structural activity relationship study of functionalized/derivatized phenoxazine ring system
Synthesis and structural activity relationship studies of sulphonamide derivatives
Synthesis and structural activity relationship studies of sulphonamide derivatives of anarcadic acid from cashew nut shell liquid
Synthesis and structural activity relationship studies of polyfunctional sulphonamide derivatives of phenoxazines and phenothiazines
Isolation and purification of bioactive components from plant materials
Structural elucidation of bioactive components from plant materials
Total synthesis of novel bioactive components from plant materials

COMPOSITION:

Coordinator: Prof. U C Okoro email: uchechukwu.okoro@unn.edu.ng

MEMBERS:

Dr. B. E. Ezema email: benjamin.ezema@unn.edu.ng

Dr. (Mrs.) M. A. Ezeokonkwo email: mercy.ezeokonkwo@unn.edu.ng

Dr. E. A. Onoabedje email: efeturi.onoabedje@unn.edu.ng

Mrs. F. U. Eze email: florence.ali@unn.edu.ng

Mr. D. I. Ugwu email: izuchukwu.ugwu@unn.edu.ng

Mrs. F. N. Ibeanu email: ibeanungozi@gmail.com

Mr. J. I. Ayogu email: jude.ayogu@unn.edu.ng

Mrs. C. P. Uzoewulu email: chiamaka.obimma@unn.edu.ng

CURRICULUM VITAE

BIO DATA

NAME: Okoro, Uchechukwu Chris DATE OF BIRTH: 12th October, 1956

State of Origin: Enugu L. G. A OF ORIGIN: Aninri

NATIONALITY: Nigerian MARITAL STATUS: Married

PERMANENT HOME ADDRESS : No 13B Ekwedike Avenue, Ndeaboh, Aninri LGA

CONTACT ADDRESS: Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka

PHONE NUMBER: 08038995403

EMAIL ADDRESS: uchechukwu.okoro@unn.edu.ng

QUALIFICATIONS: B. Sc (Chem) Unilag, 1983, Ph.D ( Oganic Chemistry) Nig. 1989

EMPLOYMENT STATUS

Employer: University of Nigeria, Nsukka, Rank: Professor

Area of Specialization: Synthetic Organic and Materials Chemistry

Research Interest: Synthesis of Biologically Active Compounds.Our group focuses on the synthesis of linear phenothiazine and phenoxazine compounds of pharmaceutical interest. Both base and acid catalyzed coupling reactions are employed in the synthesis of these compounds from readily available starting materials. Often synthesis involves creative manipulation of organic heterocyclic precursors. Synthesis and application of active herbicides are also undertaken in this direction. We also focus on the synthesis and characterization of polycyclic angular phenothiazines that are deep coloured compounds. Often we are interested in molecular modifications of the angular systems to produce analogues capable of absorbing light in the region between 700-900nm in the visible region of the electromagnetic spectrum which makes these compounds applicable as laser dyes. Reactions employed here include base catalyzed coupling under anhydrous media as well as transition metal catalyzed coupling reactions typified by Suzuki- Miyaura, Mizoroki-Heck and Buchwald-Hartwig methodologies etc. Our mode of operation also involves green chemistry methodologies e.g solvent free reactions under microwave irradiations and in ionic liquids.

PROFESSIONAL AFFILIATIONS

Fellow Chemical Society of Nigeria (CSN)
Fellow Institute of Chartered Chemists of Nigeria (ICCON)
Member New York Academy of Science

PUBLICATIONS:

A U Ofoefule, U C Okoro and O D Onukwuli, Biogas Production from Waste By-product of Ethanol Production: 2, Effect of Batch co-digestion with Some Animal and Plant Wastes on Biogas Production, Int. J. Current Res, 4(11), 86-91, (2012)
A U Ofoefule, U C Okoro, C N Ibeto and OD Onukwuli, Biodiesel Production from Tigernut (Cypenis esculartus) oil and Characterization of its Blend with Petro-diesel, Physical Review and Research Intl. 3(2), 145-153, (2013)
A U Ofoefule, U C Okoro , O D Onukwuli and C. N. Anyanwu, Biogas Production from Waste By-product of Ethanol Production: 3, Modeling of Gas Yield with Time, Physical Review and Research Intl. 3 (1), 18-27. (2013).

4.Ugwu, D. I and Okoro, U. C (2014) Synthesis, Characterisation and Antifungal activities of [4- methylphenyl sulphonamide]-N-(pyridin-2-yl)acetamide derivatives, Medicinal Chemistry, 4, 330-333.

Ozoh, C.F, Okoro, U.C and Ugwu, D.I (2014) Synthesis and Antimicrobial activities of N-(heteroaryl substituted)-p-toluene sulphonamide, Organic Chemistry International, 2014, doi:10.1155/2014/748257

Ugwu David I and Okoro Uchechukwu C (2014) Synthesis, Characterisation and Evaluation for Antibacterial Activities of N-Pyridin-2-yl Substituted-p-Toluene Sulphonamoyl Ethanamides, Int. J. Sci. Res. 3(9), 35-38.

Ugwu DI, Okoro UC, Chukwurah TD (2014) Nickel Catalyzed Synthesis of N-aryl and N-heteroaryl Substituted Benzene Sulphonamides and their Biological Activity Evaluation. Med Chem. 4:357-360.

CURRICULUM VITAE

BIO-DATA

NAME: EZEMA, BENJAMIN EBERE DATE OF BIRTH: 26^th OCTOBER 1968

STATE OF ORIGIN: ENUGU L G. A: NSUKKA

NATIONALITY: NIGERIA MARITAL STATUS: MARRIED

PERMANENT HOME ADDRESS: Central School Edem Ani, Nsukka

CONTACT ADDRESS: Department of Pure & Industrial Chemistry, University of Nigeria, Nsukka

E-Mail: eberechy2007@yahoo.com benjamin.ezema@unn.edu.ng

Mobile no. +2348066072738

QUALIFICATIONS: B.Sc (Chem) Nig., 1995; M.Sc (Organic Chem) Nig., 1999; Ph.D (Organic Chem) Nig., 2009.

EMPLOYMENT STATUS:

Employer: University of Nigeria, Nsukka. Rank: Senior Lecturer Area of Specialization: Organic Chemistry

Professional Affiliation: MCSN, MICCON

Research Skills: ORGANIC CHEMISTRY (SYNTHESIS)

Synthesis of angular and complex structures of benzophenothiazines and benzophenoxazines compounds of industrial importance. Functionalization for the preparation of the benzophenothiazine and benzophenoxazine derivatives via catalytic protocols of pharmaceutical importance:

PUBLICATIONS:

1. E. O. Adekola, B.E. Ezema, J.I. Ayogu, D.I. Ugwu, C.G. Ezema, P. N. Abuekwu. C.O. Ike, (2014), Synthesis of Benzothiazinophenothiazine Derivatives and Their Antimicrobial Screening, Oriental Journal of Chemistry, vol. 30, No.4, 1-8.
2. D.I. Ugwu, B.E. Ezema, F.U. Eze, D.I. Ugwuja, (2014), Synthesis and Structural Activity Relationship Study of Antitubercular Carboxamides, International Journal of Medicinal Chemistry, vol. 2014, 1-17.
3. B. E. Ezema; C.G. Ezema; David I. Ugwu; Jude I. Ayogu, (2014), Synthesis of Heterocyclic Azo Dyes from Quinolin-8-ol, Chemistry and Material Research, Vol. 6, No.9. 1-6.
4. B. E. Ezema; L. E. S. Akpaisi; C. G. Ezema; A. E. Onoabedje, (2014), A new method of Dimroth rearrangement in fused triazole[1,5-d]-1,2,4-triazine, Journal of heterocyclic chemistry.
5. B.E. Ezema; C.G. Ezema; A.E. Onoabedje; D.I. Ugwu. (2013), Synthesis of a new and the first triazadibenzo[a,n]triphenodithiazine, Chemical and Process Engineering

Research, Vol. 8, 35-41

CURRICULUM VITAE

BIO-DATA

NAME: Ezeokonkwo, Mercy Amarachukwu DATE OF BIRTH: 9/05/64

STATE OF ORIGIN: Anambara L. G. A. OF ORIGIN: Aguata

NATIONALITY: Nigerian MARITAL STATUS: MARRIED

MAIDEN NAME: Nnabugwu

PERMANENT HOME ADDRESS: Ezeotakwu Ward, Ikenga, Aguata LGA; Anambra State

CONTACT ADDRESS: Department of Pure & Industrial Chemistry, University of Nigeria, Nsukka

PHONE NUMBER: 08035486024

E-mail ADDRESS: mercy.ezeokokwo@unn.edu.ng ; mercy.ezeokonkwo@yahoo.com

QUALIFICATIONS: N. C. E. (Bio/Chem) Alva Ikoku , Owerri,1988; B.Sc (Chem) Unical, 1995;

M.Sc (Organic Chem) Nig., 1999; Ph.D (Organic Chem) Nig., 2010.

EMPLOYMENT STATUS:

Employer: University of Nigeria, Nsukka. Rank: Senior Lecturer AREA OF SPECIALIZATION: Organic Chemistry

RESEARCH INTEREST: Synthetic Organic Chemistry; Synthesis, Characterization and Biological activity of functionalized Phenothiazines and Phenoxazines; Synthesis and Structure activity Relationship of Heterocyclic Compounds including Sulphonamides, Imidazoles and Thiozoles; Extraction, Isolation and Phytochemical Studies of Active agents in plants of Pharmaceutical and Industrial interest.

PROFESSIONAL AFFLIATIONS

(i) Member, Chemical Society of Nigeria (CSN) (CSN/ENU/06/010) 2006

(ii) Member, Institute of Chartered Chemists of Nigeria (ICCON) (ICC NO 1/3/07/0778) 2007

PUBLICATIONS:

A. Ezeokonkwo, F. O. Ugwuona¹ and I.C. Ugwu (2015), (Accepted for publication), “Synthesis and Antibacterial Studies of Some Alkynylated Benzo[a]phenoxazin-5-one and 1,4-Naphthoquinone Derivatives, Asian J. Chem.

A. EZUGWU, M. A. EZEOKONKWO, F. O UGWUONA, I. C. UGWU,(2015), (In press), Palladium-catalyzed sonogashira snythesis of alkynylated derivatives of quinoline-5,8-

dione and their antimicrobial activity, J. Organic Synthesis.

U.C. Okoro, M. A. Ezeokonkwo, E. A. Ujah and R. C. Nweloke (2015), (In press), Synthesis of highly functionalized angular azaphenoxazines and related benzo analogues via suzuki-miyaura cross-coupling reaction, Indian J. Chem.

C. Okoro, M. A. Nnnabugwu, and C. A. Nwadinigwe (2008); Synthesis of some new diaza-analogues of angular phenothiazine as stable cyclic quinoneimines; International Journal of Chemistry, 18 (4), 171-180.

A. Nnabugwu, U. C. Okoro, C. A. Nwadinigwe and L. E. S. Akpanisi (2011), Synthesis of 1,9,11-triaza phenothiazine derivatives; International Journal of Chemistry, 21 (3), 201-206.

A. Ezeokonkwo and U. C. Okoro (2012); New Dyes for petroleum products; Journal of Emerging Trends in Engineering and Applied Sciences, 3 (1), 8-11.

CURRICULUM VITAE

BIO DATA

Name: ONOABEDJE Efeturi Abraham Date of Birth: 11/01/78

State of Origin: Delta L. G. A.: Ughelli North

Nationality: Nigerian Marital Status: Single

Permanent home Address: 7 Okpagha Street, Oteri-Ughelli.

Contact Address: Dept. Pure & Ind. Chemistry, UNN.

Cell Phone Numbers: +2348037295871, +2348079644945

E-mail Address: efeturi.onoabedje@unn.edu.ng

QUALIFICATIONS: BSc (Hons), 2004; MSc, 2008 & Ph.D, 2014 ( Nigeria)

EMPLOYMENT STATUS

Employer: University of Nigeria, Nsukka Rank: Lecturer II

AREA OF SPECIALIZATION: Organic synthesis and medicinal chemistry

RESEARCH INTEREST: Organic synthesis and medicinal chemistry

Utility of metal catalyzed synthetic methodologies in functionalization/derivatization of phenoxazine and phenothiazine motifs.
Study of structural activity relationship of newly synthesized phenoxazine and phenothiazine derivatives.

PROFESSIONAL AFFILIATION: Member of chemical society of Nigeria (MCSN).

AWARDS: PTDF scholar 2012 – 2013

PUBLICATIONS:

U.C.Okoro, E.A. Onoabedje & E.M. Odim,The First Angular Triazaphenothiazine and Related Diaza-Analogue and their Anilino Derivatives, Inter. Jour. of Chemistry, Vol 19 No. 4 Pp. 197-210,2009.
E. A. Onoabedje, B. E. Ezema and S. A. Egu, Synthesis of a Diaza Benzophenothiazine Ring System and its Anilino-Derivatives, Inter. Jour. of Chemistry, Vol 22 No. 2 Pp. 197-210, 2012.

Curriculum Vitae

Name: Eze Florence Uchenna Date of birth: 18^th February, 1983

State of origin: Enugu LGA: Igboeze-North

Nationality: Nigerian Marital status: married

Permanent home address: St. Peter’s Catholic Church, Umachi, Enugu-Ezike

Contact address: Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka

Phone Number: +2348068074457

Email: florence.ali@unn.edu.ng

Qualifications: B.Sc. (Nig.) Pure and Industrial Chemistry 2008, M.Sc. (Nig.) Organic Chemistry 2013

Employment status:

Employer: University of Nigeria, Nsukka Rank: Lecturer II

Area of Specialization: Organic Chemistry

Research Interest: Synthesis of functionalized phenoxazines, phenothiazine and sulphonamides of pharmacological importance. The chemistry of natural products with special interest in anti-tuberculosis

Selected Publications:

Ugwu, D. I., Ezema, B. E., Eze, F. U., Ayogu, J. I., Ezema, C. G. and Ugwuja, D. I. (2014) Synthesis and Biological Applications of Hydroxamates American Journal of Organic Chemistry, 2014, 4(2), 26-51.

I. Ugwu, B. E. Ezema, F. U. Eze and D. I. Ugwuja, (2014) Synthesis and Structural Activity Relationship Study of Antitubercular Carboxamides, International Journal of Medicinal Chemistry, Article ID 614808, 18 pages doi.org/10.1155/2014/614808

Ugwu, DI, Ezema, BE, Eze, FU, Onoabedje, EA, Ezema, CG, Ekoh, OC, Ayogu, JI (2015) Synthesis and Antimalarial Activities of Chalcone Derivatives, Int. J. ChemTech Res. 7 (4) 1966-1984

Curriculum Vitae

Name: Ugwu, David Izuchukwu Date of birth: 24^th June, 1983

State of origin: Enugu LGA: Udenu

Nationality: Nigerian Marital status: single

Permanent home address: All Saints Catholic Church, Ezimo Udenu

Contact address: Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka

Phone Number: +2347060870918, +2348112016672

Email: izuchukwu.ugwu@unn.edu.ng

Qualifications: National Diploma in Science Laboratory Technology 2006; B.Sc. (Nig.) Pure and Industrial Chemistry 2010; M.Sc. (Nig.) Organic Chemistry 2014

Employment status:

Employer: University of Nigeria, Nsukka Rank: Assistant Lecturer

Area of Specialization: Organic Chemistry

Research Interest: Synthetic bioorganic medicinal chemistry: Synthesis of functionalized sulphonamides, chalcones, phenoxazines, phenothiazines and hydroxamates of pharmacological importance.

Selected Publications:

Ezema, BE, Ezema, CG, Onoabedje, EA and Ugwu, DI Synthesis of a new and first triazadibenzo[a,n]triphenodithiazine, Chemical and Process Engineering Research, 8, 35-41, 2013.

Onoabedje, EA, Ezema, BE, Ezema, CG and Ugwu, DI Synthesis of some derivatives of benzophenithiazinone of pharmaceutical interestvia nickel catalyzed Grignard couplings, Chemical and Process Engineering Research, 8, 6-11, 2013.

Ugwu, DI and Okoro, UC Synthesis, Characterisation and Antifungal activities of [4- methylphenyl sulphonamide]-N-(pyridin-2-yl) acetamide derivatives, Medicinal Chemistry, 4, 330-333, 2014.

Ozoh, CF, Okoro, UC and Ugwu, DI Synthesis and Antimicrobial activities of N-(heteroaryl substituted)-p-toluene sulphonamide, Organic Chemistry International, 2014, 2014.

Ugwu DI and Okoro UC Synthesis, Characterisation and Evaluation for Antibacterial Activities of N-Pyridin-2-yl Substituted-p-Toluene Sulphonamoyl Ethanamides, Int. J. Sci. Res. 3(9), 35-38, 2014.

CURRICULUM VITAE

BIO-DATA

NAME: Ibeanu, Fidelia Ngozi DATE OF BIRTH: 3^rd February, 1965

STATE OF ORIGIN: Anambra L.G.A. OF ORIGIN: Anaocha

NATIONALITY: Nigerian MARITAL STATUS: Married

PERMANENT HOME ADDRESS: St Peter’s Catholic church, Adazi-Ani, Anaocha L.G.A.

CONTACT ADDRESS: Natural Science Unit, School of General Studies, U.N.N.

PHONE NUMBER: 08062385748, 07053821689, 08188385914

EMAIL ADDRESS: ibeanungozi@gmail.com

QUALIFICATIONS: M.Sc (Organic chemistry), 1998; Postgraduate Diploma in Education 1988; B.Sc. (Hons) Pure Chemistry, 1986

EMPLOYMENT STATUS:

EMPLOYER: University of Nigeria RANK: Lecturer I

AREA OF SPECIALIZATION: Heterocyclic and Colour Chemistry

RESEARCH INTEREST:

synthesis, characterization and Biological Screening of angular Phenothiazines and Phenoxazines
The Utility of Buchwald-Hartwig and Mizoroki-Heck Cross-Coupling reactions in the synthesis of angular aza-phenothiazine and phenoxazine derivatives: Characterization and Biological Screening.

PROFESSIONAL AFFILIATION: Member, Chemical Society of Nigeria

PUBLICATIONS:

An Alternative Synthesis of Para Red (4-Nitrobenzene-azo-2-naphthol)

CURRICULUM VITAE

BIO-DATA

Name: Ayogu, Jude Ikechukwu Date of Birth: 20^th June, 1986

State of Origin: Enugu L.G.A: Igbo-Eze South

Nationality: Nigeria Marital Status: Single

Permanent Home Address: 65D Nsukka Road Ibagwa-Aka, Igbo-Eze South L.G.A., Enugu State.

Contact Address: Department of Pure and Industrial Chemistry, University Of Nigeria, Nsukka, Enugu State,

Phone Number: +2348060542419

E-mail Address: jude.ayogu@unn.edu.ng

EDUCATIONAL QUALIFICATION: BSc (Hons) Nig. 2011

EMPLOYMENT STATUS:

Employer: University of Nigeria, Nsukka Rank: Graduate Assistant

AREA OF SPECIALIZATION: Organic Chemistry

RESEARCH INTEREST: Organic Synthesis, Catalysis, Medicinal Chemistry and Natural Product Chemistry.

PUBLICATIONS:

Emmanuel O. Adekola, Benjamin E Ezema, Jude I. Ayogu, David I. Ugwu, Chidimma G. Ezema , Abuekwu P. Nwasi & Christian O. Ike (2014).Synthesis of Benzothiazinophenothiazine Derivatives and their Antimicrobial Screening, Oriental Journal of Chemistry, 30 (4): 1493-1500.

Benjamin E. Ezema, Chidimma G. Ezema, David I. Ugwu, Jude. I. Ayogu (2014). Synthsis of Hetercyclic Azo Dyes from Quinolin-8-ol, Chemistry and Materials Research, 6 (9).

David I. Ugwu, Benjamin E. Ezema, Florence U. Eze, Jude I. Ayogu, Chidimma G. Ezema, Daniel I. Ugwuja (2014). Synthesis and Biological Applications of Hydroxamates, American Journal of Organic Chemistry, 4 (2): 26-51.

Ugwu, David I.; Ezema, Benjamin E.; Eze, Florence U.; Onoabedj, Efeturi, A.; Ezema, Chidimma G.; Ekoh, Ogechi C.; Ayogu, Jude I. (2014-2015). Synthesis and Antimalarial Activities of Chalcone Derivatives, Int. J. ChemTech Res., 7 (4):1966-1984.

CURRICULUM VITAE

BIO-DATA

NAME: Uzoewulu Chiamaka Peace DATE OF BIRTH: 3rd February, 1991

STATE OF ORIGIN: Anambra L.G.A: Nnewi-North

NATIONALITY: Nigeria MARITAL STATUS: Married

PERMANENT HOME ADDRESS:

CONTACT ADDRESS: Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka. Enugu State.

PHONE NO: 07038694243

E-MAIL: chiamaka.obimma@unn.edu.ng

QUALIFICATIONS: B.Sc (Hons) Nig. 2012

EMPLOYMENT STATUS

Employer: University of Nigeria, Nsukka.

Rank: Graduate Assistant

Area of Specialization: Organic Chemistry

Research Interest: Chemistry of Natural products, Organic Synthesis.

PUBLICATIONS

J N Ogbonna, B E Ezema, C P obimma, M O Agbo, Phytochemical Properties of Methanol Extract and Antimicrobial Study of Less Polar Fraction of Loranthus Micranthus (Linn.) parasitic on Alstonia Boonei, The Pharma Innovation journal., 2013 vol 2,8, 83-88.