“SYNTHESIS AND BIOLOGICAL ACTIVITY OF CERTAIN HETEROCYCLIC RING SYSTEMS”

SYNOPSIS FOR

M.PHARM DISSERTATION

SUBMITTED TO

RAJIVGANDHIUNIVERSITY OF HEALTH SCIENCES

KARNATAKA

BY

RAJESHKUMAR SAHU

B. Pharm

UNDER THE GUIDANCE OF

DR. GOVINDARAJAN R.

M.Pharm Ph.D

DEPARTMENT OF PHARMACEUTICAL CHEMISTRY

S.A.C.COLLEGE OF PHARMACY

B.G.NAGARA, KARNATAKA -571448

RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES,

BANGALORE, KARNATAKA

Curriculum Development Cell

CONFIRMATION FOR REGISTRATION OF SUBJECTS FOR DISSERTATION

Registration No.

Name of the Candidate- RAJESH KUMAR SAHU

Address- SAC COLLEGE OF PHARMACY

B. G. NAGARA-571 448

Name of the Institution- S.A.C. COLLEGE OF PHARMACY

B.G. NAGARA

Course of study and Subject- M.Pharm. In Pharmaceutical Chemistry

Date of admission to Course - 09/04/2008

Title of the Topic - SYNTHESIS AND BIOLOGICAL ACTIVITY OF

CERTAIN HETEROCYCLIC RING SYSTEMS

Brief resume of the intended work- Attached

Signature of the Student -

Guide name - DR. GOVINDARAJAN R.

Remarks of the Guide -The mentioned title compounds would be synthesized and screened for the activity. Their structures will be confirmed by spectroscopical studies under the guidance of me in the P. G. Department of Pharmaceutical chemistry of our college.

Signature of the Guide -

Co-Guide name - JAISHREE VAIJANATHAPPA

Signature of the Co-Guide -

HOD name - Dr. B. RAMESH

Signature of the HOD -

Principal name - Dr. B. RAMESH

Mobile no. - +091-9845863779

e-mail I.D. -

Signature

RAJIVGANDHIUNIVERSITY OF HEALTH SCIENCES,

BANGALORE, KARNATAKA

ANNEXURE-II

PROFORMA FOR REGISTRATION OF SUBJECT FOR DISSERATION

01 / Name of the candidate & Address / RAJESHKUMAR SAHU
S.A.C.COLLEGE OF PHARMACY
B.G.NAGARA-571448
PERMANENT ADDRESS
RAJESHKUMAR SAHU
A/P JOGNIPALI-493 558
TALUKA-SARAIPALI
DIST -MAHASAMUND
STATE-CHHATTISGARH.
02 / Name of the institute / S.A.C.COLLEGE OF PHARMACY
B.G.NAGARA
KARNATAKA -571448
03 / Course of the study / MASTER OF PHARMACY (Pharmaceutical chemistry)
04 / Date of admission / 09/04/2008
05 / Title of the topic / SYNTHESIS AND BIOLOGICAL ACTIVITY OF
CERTAIN HETEROCYCLIC RING SYSTEMS.
06 /

BRIEF RESUME OF THE INTENDED WORK.

6.1 NEED FOR THE STUDY:
A continuous need for new synthetic antimicrobial drugs which are potent with lesser side effects for the treatment of various microbial diseases, made us to undertaker the present work .It is a known fact that the organic molecules possessing benzofuran nucleus are often endowed with useful antimicrobial properties. In view of this fact benzofuran coupled with nitrogen heterocycles have received considerable attention of research workers during the last few decades.
Benzofuran nucleus may be combined with nitrogen heterocycles in different ways .The five member ring systems may be fused together as in most of the natural products or both ring systems may be linked to each other directly to produce biheterocycles and triheterocycles of through a carbon or nitrogen bridge. Although there is a considerable amount of synthetic and biological work is done on such derivatives. It is still a more fruitful field for further investigations.
6.2 REVIEW OF LITERATURE:
Benzofuropyridines are the most extensively investigated systems among the condensed benzofurans. Although the synthesis and becteriostatic activity of 2-chloro-5,6,7,8-tetrahydrobenzofuro(2,3-b) pyridine(1) were reported in 19691 . The extensive investigation of this heterocycles commenced only when cocker and co-workers 2 prepared a series of 1, 3-disubstituted derivatives of this heterocycles and showed them to possess antiviral activity.

(1)
Benzofurans containing alkylamino side chain are known for antimicrobial3 and antiviral activities. Benzofuran derivative griseofulvin (2) is official antifungal drug in various pharmacopoeias4 .

(2)
The other ways of combining various heterocyclic systems with benzofuran nucleus involve direct linkage of heterocyclic systems so as to produce biheterocycles and triheterocycles or through carbon are nitrogen bridges. This type of mixed heterocycles with benzofuran as one of the component has been of much interest to explore biological activities. Several research workers have tried to design and synthesize such molecule in a search for potent drug molecules, following this approach most of such work has come up during the last two decades 5-9 . The following antibacterial molecule(s) is example of such work.

(3)
Benzofuran derivatives have also been reported to have antioxidant, anticoagulant, anti-inflammatory and analgesic activity etc.
07
08 / 6.3 OBJECTIVES OF THE STUDY:
In the proposed work attempts shall be made.
  1. To synthesize thiazole imidazole thiadiazole and azetidinone derivatives of benzofuran and triazole.
  2. To screen the synthesized compound for antimicrobial, analgesic, anti-inflammatory, antioxidant, anticoagulant activities etc.
MATERIALS AND METHODS:
MATERIALS:
7.1 Source of data
  1. IISC library, Bangalore.
  2. SAC College of pharmacy library, BG Nagara.
  3. RGUHS library, Bangalore.
  4. E-library, SAC College of pharmacy.
5. Chemical abstracts.
6. Indian journal of Heterocyclic chemistry.
  1. Standard text books for carrying out screening of pharmacological activities.
7.2 METHOD OF COLLECTION OF DATA:
DATA COLLECTED FROM
JOURNALS:
  1. Journal of Pharmaceutical Research.
  2. India Journal of Pharmaceutical Sciences.
  3. Indian Journal of Pharmaceutical Education and Research.
  4. Journal of Chromatography.
  5. Asian Journal of Chemistry.
  6. Journal of Pharmaceutical and Biomedical Analysis.
RELATED LINKS:




7.3 Does the study require any investigation or interventions to be conducted on patients or humans or animals? If so please describe briefly.
Yes the study requires investigation on animals by mice and rats to screen for activities likeanalgesic, anti-inflammatory, antioxidant and anticoagulant activities etc.
7.4 Has ethical clearance been obtained from your institution in case
of 7.3
Will be obtained.
List of references
  1. Mooradian, Aram. Aryl and heteroaryl oximes and 4-benzoyloxycyclohexanone oxime. Chemical Abstracts. 1970; 72: 55237z.
  2. Cocker JD, Gregory GI. Synthesis of Benzofuran derivatives. Ger.Offen. 1970; 2: 022, 024.
  3. Grinev AN, Zotova SA, Gololobova TM. Synthesis and biological activity of 2-methyl-5-methoxybenzofuran. Chemical Abstracts. 1986; 104: 68700z.
  4. Controllers of publications. Indian pharmacopoeia. New Delhi India. 1996; 1: 353.
  5. Romeo Paioni, Schilling Walter, Bernasconi Raymond. Benzofuranyl-tetrahydropyridines and piperidines, their acid addition salts and antidepressant preparations. Chemical Abstracts. 1981; 95: 61971a.
  6. Bourgery G, Lacour A, Fr.Demande. 6-N-Arylpiperazinoalkoxy-4,7-dimethoxybenzofuran derivatives and their therapeutic use. Chemical Abstracts. 1981; 95: 43166n.
  7. Scherrer RA, Stern RM, Hammer WJ. Tetrazole-5-yl-2-nitro-3-phenylbenzofurans and their antimicrobial use. Chemical Abstracts. 1986; 104; 19593h.
  8. Gris SPJ, Gonzalez BJM, Roget AJ. Preparation of 4-(7-benzofuryl)-2, 6-dimethyl-1,4-dihydropyridines with one or more chiral substituents, useful as antiarrythmics, and calcium antagonists . Chemical Abstracts. 1990; 113: 40468t.
  9. Gris SPJ Gonzalez BJM, Roget AJ. Preparation of aminoalkyl4-(7-benzofuryl)-2, 6-dimethyl-1, 4-dihydropyridine-3, 5-dicarboxylates useful as vasodilators, antiarrythmics and calcium antagonists. Chemical abstracts.1990; 113: 40469t.
  10. Stanislav Radl, Hezky Petr, Krejci Ivan. Synthesis and analgesic activity of some substituted 1-benzofurans and 1-benzothiophenes. Czech.Chem.Commun. 2000; 65(7):1093-1108.

09 /

Signature of Candidate

/ RAJESH KUMAR SAHU
10 / Remarks of the guide / The mentioned title compounds would be synthesized and screened for the activity. Their structures will be confirmed by spectroscopical studies under the guidance of me in the P. G. Department of Pharmaceutical chemistry of our college.
11 / Name and Designation
(In block letters)
11.1 GUIDE
Guide ship reference No. Of RGUHS
ACA/CDC/PGT-M.Ph/SACP/36/2008-09 ,DT 17/11/2008
11.2 Signature
11.3 Co-Guide
11.4 Signature
11.3 Head of the Department
11.4 Signature / DR. GOVINDARAJAN R.
M.Pharm. Ph.D.
Associate Professor.
Department Of Pharmaceutical Chemistry,
S.A.C. College of Pharmacy,
B. G. Nagara-571448
JAISHREE VAIJANATHAPPA
M.Pharm. Ph.D
Dr. B.RAMESH
M.Pharm. Ph.D.
Professor & Head,
Department of Pharmaceutical Chemistry.
S.A.C.College of Pharmacy,
B. G. Nagara-571448
12 / 12.1Remarks of the Principal
12.2 Signature