SYNTHESIS AND BIOLOGICAL SCREENING OF SOME NOVEL

BENZYLIDINE ANILINE DERIVATIVES

DISSERTATION PROTOCOL

Submitted to the

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,

BANGALORE, KARNATAKA

BY
YOGESH D.B.
M.PHARM, PART- I

DEPARTMENT OF PHARMACEUTICAL CHEMISTRY

UNDER THE GUIDANCE OF

Mr. M.CHANDRASHEKAR M.PHARM

Department Of Pharmaceutical Chemistry

Dr.H.L.T College of Pharmacy,

Kengal, Channapatna-571502

2007

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,

BANGALORE, KARNATAKA.

AnneXUre II

Proforma for Registration of subjects for Dissertation
1. / Name of the Candidate and
Address( in block letters) /

Mr.YOGESH D.B

M. PHARM, PART-I
DEPARTMENT OF PHARMACEUTICAL CHEMISTRY.
Dr. H. L. T.COLLEGE OF PHARMACY.
KENGAL, CHANNAPATNA-571502
BANGALORE (RURAL), KARNATAKA
2 / Name of the Institution / Dr. H. L. T. College of Pharmacy
Kengal, Channapatna,
Bangalore Rural 571 502
3 / Course of the Study and Subject / Master of Pharmacy in Pharmaceutical Chemistry.
4 / Date of Admission to the Course / 09/06/2007
5 / Title of the Topic / “SYNTHESIS AND BIOLOGICAL SCREENING OF SOME NOVEL BENZYLIDINE ANILINE DERIVATIVES”

6  BRIEF RESUME OF THE INTENDED WORK

6.1  NEED FOR THE STUDY

The approach to the practice of medicinal chemistry has developed from an empirical one involving synthesis of new organic compounds based largely on modifications of chemical compounds of known biological activity could be better explored. It is well established that slight alterations in the structure of certain compounds are able to bring drastic changes to yield better drug with less toxicity to the host. It is observed that chemical modification not only alters physicochemical properties but also pharmacological activities.

Under the proper conditions, diazonium salts reacts with certain aromatic compounds to yield products of the general formula Ar-N=N-Ar1 called azo compounds, reaction is known as coupling1. This is an attempt to synthesize derivatives of benzylidine anilines by substituted phenyl azo compounds.

The schiff and mannich base derivatives drawn a lot of attention on optimal anti microbial activity against wide range of microorganisms like bacteria, fungi, virus and also additional features like anti-protozoal, anti-HIV and antihelminthic activities2.

Owing to the importance and established pharmacological activity of this compounds we directed our attention towards synthesis of some novel derivatives of aniline compounds.

An attempt will be made in our study to synthesize, characterize newer benzylidine anilines and evaluate them for their anti-microbial activity.

6.2.  REVIEW OF LITERATURE

Extensive literature survey was carried out in the library of Dr.H.L.T. College of Pharmacy, Channapatna, IISC, Bangalore and Visiting various web sites through inter net the relevant data has been collected.

Literature survey clearly demonstrates the high synthetic potential of benzylidine aniline derivatives, good amount of information is available on Anti- microbial activity of these compounds.

Ø  Seshaiah Krishnan Sridhar, muniyandy saravanan, Atmakunu Ramesh, reported the anti bacterial activity against gm (+ve) and gm (-ve) standard and pathological bacterial strains by using schiff and mannich bases of isatin derivatives2.

Ø  Halve A K et al., reported the synthesis, anti microbial screening of 2- Hydroxy-5- (nitro-substituted phenyl azo) benzylidine anilines3.

Ø  Anna Fryszkowska et al., studied the phenyl azo group effectively activates both Fluorine and Chlorines towards nucleophilic substitutions, the method is synthetically useful for preparation of substituted anilines4.

Ø  J. Pernak I, Mirska, R.Kmiecik, Prepared analogues of quaternary nitrogen atom showing anti microbial activities using mannich bases5.

Ø  Surendra N. Pandeya et al., reported the synthesis and anti bacterial activity of mannich bases6

6.3.  MAIN OBJECTIVES OF THE STUDY

The objectives of proposed study are:

·  To Synthesize new benzylidine anilines by using substituted anilines, sodium nitrite, Hydro Choric acid, different aldehydes and Aromatic amines etc.

·  Characterizes, identify, quantify, purify the synthesized compounds by thin layer chromatography, melting point determination by Thiels melting point tube (capillary tube method), Infrared Spectroscopy, Nuclear Magnetic Resonance Spectroscopy and Mass Spectroscopy.

·  To screen these newly synthesized compounds for anti microbial activity for various gm (+ve) and gm (-ve) Bacteria.

7.  MATERIALS AND METHODS

7.1  SOURCE OF DATA

The preliminary data required for the experimental study was obtained from:

·  CD-Rom search available at National Center for Scientific Information (NCSI).

·  Chemical Abstract.

·  Scientific Journals.

·  Dr. H.L.T. college of Pharmacy Library.

·  Indian institution of sciences (IISC). Bangalore

·  Internet Sources.

7.2.  METHODS OF COLLECTION OF DATA

A)  Synthetic Studies:

As per literature review the newer benzylidine anilines will be synthesized and progress of reaction as follows:

Substituted anilines

Substituted diazonium salt

+

Different Aldehyde

Substituted aryl Aldehyde

+

Aromatic amines

Derivatives of benzylidine anilines

B)  Purity and characteristic studies:

Purity of these compounds will be checked by thin layer chromatography and they will be characterized by spectroscopic data.

C)  Biological screening:

Antibacterial activity will be carried out by zone of inhibition studies by cup plate method.

7.3 Does the study require any investigations or interventions to be conducted on patients or other humans or animals? If so please describe briefly.

The study does not require any investigations on patients or humans or animals.

7.4  Has ethical clearance been obtained from your institution in case of 7.3.

……………………..Not Applicable………………………………………..

8.  LIST OF REFERENCES

1.  Jerry march, Advanced organic chemistry, 4th ed, John willey and sons publications, New York, 1992: 896-897.

2.  Seshaih Krishnan Sridhar, Muniyandy saravanan, atmakuru ramesh. Eur.J. Med.chem,2001; 36:615-625.

3.  Halve A.K. et al., Indian Journal Of pharmaceutical sciences, 2006; 68:510-514.

4.  Anna Fryszkowska et al., Tetrahedron, 2005; 61:2327-2333.

5.  J.Pernak, I.Mirska, R. Kmiecik, Eur.j. Med.chem, 1999; 34:765-771.

6.  S.N.Pandeya, et al., Eur.j. Med.chem, 2000; 35:249-255.

7.  David A. Williams, Thomas L.Lemke, Foeye’s Principles of medicinal chemistry, 5th ed, Lippincott Williams and Wilkins publication. New delhi, 2002:819-890.

8.  Egen stanl, Thin layer chromatography, 2nd ed, Springer publication .2005:52-105.

9.  Leo A. Paquette, Encyclopedia of reagents for organic synthesis, John willey and sons publications. New York, 1995:268-385.

10.  Pelczar, Michael Joseph, Microbiology, 5th ed, Tata M C Graw-Hill publications. 1993:151-320.

11.  I.L. Finnar, Textbook of Organic Chemistry, ELBS Publication. 1989,1:214.

12.  Vogel’s Organic Practical Chemistry, 4th ed, ELBS publication.1989: 782.

13.  Hobart H.Willard, lynne L.merit, Jr.John A.Dean, Frank A, Settle, Jr.Instrumental Method Of Analysis, 7th ed, Wads Worth publishing company, California.1988: 465-505.

9 / Signature of the candidate
10 / Remarks of the Guide / Topic selected for Dissertation work is satisfactory. This can be carried out in our Laboratory.
11 / Name and Designation of
(In Block Letters)
11.1  Guide
11.2  Signature / Mr. M. CHANDRASHEKAR M Pharm
PROFESSOR
DEPT. OF PHARMACEUTICAL CHEMISTRY.
Dr. H. L. T. COLLEGE OF PHARMACY,
KENGAL, CHANNAPATNA-571 502
BANGALORE (RURAL), KARANATAKA.
11.3  Co – Guide
(If any)
11.4  Signature
11.5  Head of the Department
11.6 Signature / Mr. M. GURUMURTHY.M. Pharm
ASSISTANT PROFESSOR
DEPT. OF PHARMACEUTICAL CHEMISTRY.
Dr. H. L. T. COLLEGE OF PHARMACY,
KENGAL, CHANNAPATNA-571 502
BANGALORE (RURAL), KARANATAKA.
12 / 12.1  Remarks of the Chairman and Principal
12.2  Signature / The above mentioned information is correct and I recommend the same for approval.

From

YOGESH D B

M.Pharm, Dept.of Pharmaceutical Chemistry,

Dr.H.L.T College of Pharmacy,

Kengal, Channapatna.

To

The Registrar (Evaluation),

Rajiv Gandhi University of Health Sciences,

4th ‘‘T’’ Block, Jayanagar,

Bangalore-560 041

(Through Proper Channel)

Sub: Submission of Synopsis of Dissertation

Respected Sir,

Herewith, I am submitting synopsis of dissertation work “SYNTHESIS AND BIOLOGICAL SCREENING OF SOME NOVEL BENZYLIDINE ANILINE DERIVATIVES” for registration in M.Pharm (Pharmaceutical chemistry) of Rajiv Gandhi University of Health Sciences, Bangalore, Karnataka.

Kindly accept the same and oblige.

Thanking you,

Yours faithfully,

Place: Channapatna (YOGESH D.B.)

Date:

Guide:

Mr. M.CHANDRASHEKAR, M.Pharm

DEPT. OF PHARMACEUTICAL CHEMISTRY PRINCIPAL

Dr. H.L.T.College of Pharmacy, Dr. H.L.T.College of Pharmacy,

Kengal, Channapatna. Kengal, Channapatna.

Bangalore (Rural)-571 502 Bangalore (Rural) 571 502