!"# $ "!%&$ !"## $ '( ) * * ! +$ ! ,-$ ) ( ( ( (
* .( '& /-.(
0 - ( 0 1 2 3 . 4 5 6 7
8 ( ( 9 ( /01 . 1 : 0( ( 7 ( - - 5 / & 0
!" ## $% &
! "#
! " # $ !% ! & $ ' ' ($ ' # % % ) %* %' $ ' + " % & ' ! # $, ( $ - . ! "- ( %
. % % % % $ $ $ - -
- - / / $$$ 0 1"1"#23."
"0" )*4/ +) * !5 !& 6!7%66898& % ) 2 : ! * & / - ;96d >6e >6c >6b Metformin and glybenclamide were used as standard antidiabetic drug in both the models. All values are represented in Table.
45
Table In vivo antihyperglycemic activity of various oxazolidines derivatives (6a–e) in streptozotocin (STZ) and sucrose-loaded (SLM) rat models Compounds
% Blood sugar lowering activity (100mg/kg) STZ model
SLM model
6a
52.0
72.0
6b
19.6
NIL
6c
13.4
33.2
6d
48.5
66.4
6e
10.9
43.6
Metformin
19.7
13.5
Glybenclamide
31.2
39.4
46
References 1. Diabetes. World Health Organization. Information Bulletin No.312 (2006). 2. Trivedi, B., Mazumdar, J. D., Hemavathi, K.G., Effect of Shilajit on blood glucose and lipid profile in alloxan-induced diabetic rats. Indian J Pharmacol, 36(6), 373-376 (2004).
47
6. Summary and Conclusion Summary ¾ In the present study, novel oxazolidine derivatives were synthesized and characterized by IR,
1
H-NMR, mass
spectral data and elemental analysis. ¾ All
the
synthesized
compounds
were
screened
for,
antihyperglycemic activity ¾ Structure activity relationship studies indicated that different substitutions on the oxazolidine nucleus exerted varied biological activity. The electronic nature of the substituent groups at second, third and fourth positions in oxazolidine nucleus led to significant variation in antihyperglycemic activity. The substituted aniline and alkoxy groups enhanced the antihyperglycemic activity. ¾ In the present study, oxazolidine moiety exhibited potential antihyperglycemic activity.
48
Conclusions The project has outlined the chemistry and biological activities of the oxazolidine scaffold. The synthetic methods are indicates the simplicity, quality and versatility, which offer the medicinal chemist a complete range of novel derivatives. Given the advances in synthetic methodology and technology in recent years and the continued interest in the oxazolidine skeleton in medicinal chemistry and drug development, the development of efficient and reliable methods for the construction of these molecules will ensure that this is an active and important area of research in heterocyclic chemistry. Thus oxazolidine scaffold is not only synthetically important but also possesses a wide range of promising biological activities. Future investigations of this platform could give some more encouraging results. Therefore may serves as a lead molecule for further modification to obtained clinically useful novel entities in the new millennium.
49
50
51
52
53
54
55
56
57
Paper Publication Theivendren Panneer Selvam, Palanirajan Vijayaraj Kumar, Parthasarathi Ramu, Arumugam Siva Kumar, Synthesis, characterization and anti hyperglycemic activity of novel oxazolidines derivatives, Archives of Pharmacal Research, 34 (6) (2011) 887-891. DOI: 10.1007/s12272-011-0604-3
58
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