RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCE
BANGALORE, KARNATAKA
Annexure- II
Proforma for Registration of Subjects for Dissertation
1 / Name of The Candidate AndAddress ( In Block Letters ) / YOUNUS KHAN.
KARNATAKA COLLEGE OF PHARMACY, MANHALLI ROAD, BIDAR – 585 403
2 / Name of The Institution / KARNATAKA COLLEGE OF PHARMACY, BIDAR – 585 403
3 / Course of study and subject / M. PHARM
(BULK DRUGS)
4 / Date of Admission to Course / 05-07-2010
5 / Title Of The Topic
SYNTHESIS, CHARACTERIZATION AND
BIOLOGICAL ACTIVITIES OF SOME NEW
BENZO (b) THIOPHENE DERIVATIVES.
6 / Brief resume of the intended work:
6.1 Need For The Study Enclosure-I
6.2 Review Literature Enclosure-II
6.3 Objective Of The Study Enclosure-III 6.4 Methodology Enclosed- IV
7 / Materials And Methods :
7.1 Sources Of Data Enclosure-V
7.2 Methods Of Collection Of data Enclosure-VI
7.3 Does the study require any investigation or intervention to be conducted on patients
or humans and animals? If so please describe briefly:
… Yes ….
7.4 Has ethical clearance been obtained from yours institution? If so please describe
briefly: …Applied …
8 / List of References / Enclosure-VII
9 / Signature of the candidate /
YOUNUS KHAN.
10 / Remarks of the guide / SATISFACTORY.
11 / Name and Designation
(in block letter)
11.1 Guide
11.2 Signature
11.3 Co-guide (if any)
11.4 Signature
11.5 Head of Department
11.6 Signature / Mr. VIJAYKUMAR TIRLAPUR
M. PHARM.( PhD)
ASST. PROFESSOR
DEPARTMENT OF BULK DRUG
KARNATAKA COLLEGE OF
PHARMACY BIDAR.
--
--
Dr. KASHINATH NAUBADE
M. PHARM ,PhD
H.O.D & PROFESSOR
DEPARTMENT OF BULK DRUG
KARNATAKA COLLEGE OF
PHARMACY BIDAR.
12 / 12.1 Remarks of the chairmen and
Principal
12.2 Signature with seal / SATISFACTORY
Prof. SIRSE KRANTIKUMAR.
M. PHARM ,(PhD)
PRINCIPAL & PROFESSOR
KARNATAKA COLLEGE OF PHARMACY, BIDAR.
ENCLOSURE- I
6. BRIEF RESUME OF THE INTENDED WORK.
6.1 Need for the study.
The chemical and biological potentials of five-membered heterocyclic compounds fused with aromatic nuclei have attracted the attention of organic and medicinal chemists for several years. Most of the research programme efforts are directed towards the design of new drugs, because of the unsatisfactory status of present drug side effects and the resistance by the infecting organisms to present drugs.
Sulphur containing heterocycles are the active research in the pharmaceutical chemistry. Now a days benzothiophene derivative in combination with other ring systems have been used extensively in pharmaceutical applications such as antiallergic, analgesic, anti-inflammatory etc.
The present study is focused on the development of new potent heterocyclic moieties containing benzothiophene nucleus for enhancing better biological and pharmacological properties.
ENCLOSURE- II
6.2 Review of Literature
H.s.joshi et al1 synthesis and antimicrobial activity of some new benzo(b)thiophene incorporated dihydroquinolines.
Sembian ruso jayaraman., et al2 3-methyl-4,5,6,7-tetrahydro-1-benzothiophene-2- carboxylic acid.
Arun m.isloor., et al3 synthesis, characterization and biological activities of a number of new benzo[b]thiophene derivatives.
Basavaraj padmashali., et al 4 synthesis of 3-substituted-2-methyl-5, 6, 7, 8-tetrahydrobenzo[b] thino[2, 3-d] pyrimidin-4-(3H)-ones and their pharmacological efficacy.
Basavaraj padmashali., et al 5 synthesis and pharmacological investigation of benzothiophene heterocycle.
Peter langer., et al 6 synthesis of functionalized benzothiophenes by two fold heck and subsequent 6п -eletrocyclization reactions of 2, 3-dibromothiophene.
Fuyao zhang., et al 7 .efficient synthesis of 3-oxygenated benzothiophene derivative.
Gary.f.filzen. et al 8 synthesis and SAR of selective benzothiophene,benzofuran, and indole-based peroxisome proliferator-activated receptor agonists δ agonists.
Samir j.naik and Uma p.halkar., et al 9 synthesis 4, 5, 6, 7-tetrahydrobenzo [b]thiophene based azo disperse dyes.
Manish dixit and Atul goel., etal 10 synthesis regioselective synthesis of functionalized naphtho[b]thiophene through a ‘lactone methodology’.
Ming-wei wang., et al 11 synthesis benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.
Mahesh attimarad et al12 synthesis of hydroxyl benzothiophene/Naphthalene carboxylic acid as potent NSAIDS
Guillaume de nanteuil., et al 13 synthesis new fibrinolytic agents’ benzo thiophene derivatives as inhibitors of the t-PA-PAI-1 complex formation.
Salvatore cabiddu., et al 14 a convenient synthesis of benzothiophene derivatives.
Yaroslav v.bilokin .,et al 15 synthesis a novel and expedient approach to new heterocycles containing benzothiophene, benzothieno [2, 3-d] pyrimidine and coumarin moieties.
Thomas c.britton., et al 16 structure activity relationships of a series of benzothiophene-derived NPY Y1 antagonist: optimization of the C-2 side chain.
G.primofiore., et al17 isosteric replacement of the indole nucleus by benzo- thiophene and benzofuran in a series of indolylglyoxylylamine derivatives with partial agonist activity at the benzodiazepine receptor.
ENCLOSURE- III
6.3 Objective of the Study
In view of the significance of naturally occurring and physiologically active benzothiophene stimulated our interest in the synthesis of several heterocyclic compounds containing benzothiophene ring either in fused form or as substituted.
The newly synthesized molecules will be established on the basis of physical data, analytical data and spectral studies such as IR, 1H NMR, 13C NMR and mass and were screened for their biological and pharmacological activities on the basis of literature survey. The results of biological and pharmacological activities of the newly synthesized compounds were compared with standard drug.
ENCLOSURE- IV
6.4 METHODOLOGY
In the present investigation required starting material substituted benzo(b)thiophenes was prepared when substituted cinnamic acid was made react with thionyl chloride under reflux condition. Then the intermediate was converted into different heterocyclic compounds.
All the synthesized compounds will be evaluated for invitro antibacterial activity.
ENCLOSURE- V
7. MATERIALS AND METHODS
7.1 Source of data
In the present investigation we planned to synthesized benzothiophene derivatives by closing the thiophene ring on the benzoid ring. This synthetic work mainly a laboratory based work. All the basic facilities which required carrying out are available in our laboratory.
The literature survey pertaining to present investigation will done by referring chemical abstracts, internet, national and international journals.
The day to day development in the area will be updated by literature survey through e-publishing, internet and current periodicals in our library and else where.
ENCLOSURE- VI
7.2 Method of collection of data.
The chemical structure of synthesized compounds will be established on the basis of physical, chemical and analytical data. Melting point of newly synthesized compounds will be determined by open capillary tube and is uncorrected they are expressed in degree centigrade. The compounds synthesized will be characterized by IR, 1HNMR and Mass Spectral data. This will be collected by sending the sample to other advanced research center.
The main objective of the present investigation is to explore newer molecule with potent biological and pharmacological activities.
7.3 Does the study require any investigation or investigations to be conducted on patients or other human or animals? If so, please describe briefly.
Yes, at the later stage, after successful synthesis of molecules. The compound will be screened for pharmacological actions on albino mice and rats.
7.4 Has ethical clearance been obtained from your institution in case?
Yes ethical clearance committee had been obtained by our Institution.
ENCLOSURE- VII
8. References
1. H.s.joshi.,k.m.thaker,B.l..dodiya,K.a.joshi,R.m.ghetiya,P.b.vekariya synthesis and antimicrobial activity of some new benzo[b]thiophene incorporate dihydroquinolines.
Indian journal of heterocyclic chemistry., 20, 21(2010).
2. Sembian ruso jayaraman., Madhavan sridharan and Rajendiran nagappan ,3-methyl-4,5,6,7-tetrahydro-1-benzothiophene-2- carboxylic acid.
Molbank journal.M648 (2010)
3. Arun m.isloor., Balakrishna kalluraya., K.sridhar pai., Synthesis, characterization
and biological activities of some new benzo[b]thiophene derivatives.
European Journal of medicinal Chemistry., 1(2009).
4. Gadada naganagowda., and Basavaraj padmashali., Synthesis of 3-substituted-2-
methyl-5, 6, 7, 8-tetrahydrobenzo[b]thino[2,3-d]pyrimidin-4-(3H)-ones and their
pharmacological efficacy.
Indian journal of heterocyclic chemistry .,19, 9 (2009).
5. Gadada naganagowda., Basavaraj padmashali and T.h.suresha kumara.,Synthesis and pharmacological investigation of benzothiophene heterocycles.
Indian journal of heterocyclic chemistry., 19, 13(2009).
6. Serge-mither and Tengho toguem ., Munawar hussain ., Imran malik ., Alexander
villinger., Peter langer., Synthesis of functionalized benzothiophene by twofold
heck and subsequent 6п-electrocyclization reaction of 2,3-dibromothiophene.
Tetrahedron Letters., 50, 4962 (2009).
7. Fuyao zhang., David mitchell., Patrick pollock., and Tony y.zhang., Efficient
synthesis of 3-oxygenated benzothiophene derivatives.
Tetrahedron Letters 48., 2349 (2007).
8. Gary f.filzen., Larry bratton ,Xue-min cheng, Noe erasaga, Andrew geyer, Chitase lee, Gina lu, Jim pulaski, Roderick,sorenson, Paul c, Unangst, B.k.trivedi and xiangyang xu,Synthesis and SAR of selective benzothiophene,benzofuran,and indole-based peroxisome proliferator-activated receptor agonists δ agonists.
Bioorganic and Medcinal chemistry letters17(2007)
9. Samir J.naik., and Uma p.halkar., Synthesis of 4, 5, 6, 7-tetrahydrobenzo [b]
thiophene based azo disperse dyes.
Indian Journal of Heterocyclic Chemistry.,.15, 213 (2006).
10. Manish dixit and Atul goe, Regioselective synthesis of functionalized naphtho[b] thiophenes through a ‘lactone methodology.
Tetrahedron Letters., 47, 3557 (2006).
11. Mahesh attimarad,S.mohan and M.srinivas murthy,Synthesis of hydroxyl benzothiophene/naphthalene carboxylic acids as potent NSAIDS.
Indian journal of heterocyclic chemistry .,14, 285 (2005).
12. Qinggang ji., Jie gao., Junbo wang., Chunhao yang., Xin hui., Xueming yan.,
Xihan wu., Yuyuan xie., and Ming-wei wang., Benzothieno [3, 2-b]indole derivatives as potent selective estrogen receptor modulator .
Bioorganic and medicinal Chemistry letters., 15, 2891 (2005).
13. Guillaume de nanteuil.,Christine lila-ambroise., Alain rupin., Marie-odile
vallez., and Tony j.verbeuren., New fibrinolytic agent :Benzothiophene
derivatives as inhibitor of the t-PA- PAI-1 complex formation.
Bioorganic and Medicinal Chemistry letters.,13,1705 (2003).
14. M.grazia cabiddu., Salvatore cabiddu., Enzo cadoni. Stefania demontis,Claudia
fattuoni and Stefana melis., A convenient synthesis of benzothiophene
derivatives
Tetrahedron., 58, 4529 (2002)
15. Yaroslav v.bilokin., A novel and expedient approach to new heterocycles
containing benzothiophene, [2,3-d] pyrimidine and coumarin moieties.
Tetrahedron., 55, 13757 (1999).
16. Thomas c.britton., Patrick g.spinazze., Philip a.hipskind., Dennis
m.zimmerman., Hamideh zarrinmayeh.,Douglas a.scholar., Donald r.gehlert.,
and Robert f.bruns. Strutcure-activity relationshiphs of a series of
benzothiophene –derived NPY Y1 antagonists:optimization of the C-2 side chain.
Bioorganic and medicinal Chemistry Letters., 9, 475 (1999).
17. F da settimo., A lucacchini . , A m marini., C martini ., G primofiore., G
senatore ., S taliani. Isosteric replacement of the indole nucleus by
benzothiophene and benzofuran in a series of indolylglyoxylamine derivatives
with partial agonist activity at the benzodiazepine receptor .
European Journal Medicinal Chemistry., 31, 951 (1996).
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