Pawan Bajpai, Shelesh Jain, Ankur Choubey*
School of Pharmacy, Madhyanchal Professional University, Bhopal-462024.
*Corresponding Author E-mail: chaubey.ankur03@gmail.com
ABSTRACT:
Thiazolidine is become an important ring in the development various antagonist against different diseases such as diabetes, cancer, inflammation, microbial infection etc. Thiazolidine derivatives showed improved pharmacological activity in different pathophysiological conditions than its standard drug. Thiazolidine2,4-dione, 1, 3 thiazolidines, 2, 4 dione,4-oxo thiazolidine contains basic thiazolidine skeleton. The present science migrates to the development of drugs on the basis of structure-based drug design in the presence of protein structure. The difference between the designed drug and their synthesis can be minimized by showing the ligand protein interaction. The present study includes the thiazolidine derivatives and their pharmacological activities in the treatment of various diseases.
KEYWORDS: Thiazolidine, Antibacterial, Anticancer, Anti-inflammatory.
1. INTRODUCTION:
Thiazolidine (1) is an important five membered heterocyclic ring system with a thio group, oxo group and amine group that exhibit a range of pharmacological activities, but not limited to, including anti-cancer [1], hyperglycemic [2], anti-arthritic [3] anti-inflammatory [4] and anti-microbial [5] etc. Among them, anti- hyperglycemic is the widely studied effect of TZD derivatives that has also been extended to the development of clinically used “glitazone” drugs such as pioglitazone [6], troglitazone [7], rosiglitazone [8], and lobeglitazone [9] etc. Cancer is one of the world’s most serious illnesses; every ten in a hundred people are suffering from cancer. Clinically, many chemotherapeutic drugs provide a satisfactory response when they are first exposed to the tumors, but they cause a variety of side effects to the patients. Therefore, there is an urgent need for potential, selective anticancer drugs in modern oncology. [10]
Molecular formula: C3H3NO2S
MoleculeWeight: 117.13g/mol
3. Biological Activity of Heterocyclic Ring:
The thiazolidine ring has been incorporated into various type of biological compounds either a substituents group or a replacement of another ring. Researchers have prepared a various compounds containing this moiety.
A) Anti Bacterial Activity:
Antibacterials, are medications that slow down or destroy the growth of bacteria. Anti Bacterial drug are used to treatment of many diseases which is caused by bacteria.
· Mulwad et al [11] prepared a series of N-[coumarin-6-yl] spiro-indoloazetidin-2-ones thiazolidin-4-ones (2) derivatives.
· Singh et al [12] prepared a series of thiazolyl –thiazolidinylbenzo-thiazoles (3) and analyzed for their antibacterial activity against Gram-positive bacteria S.aureus and E.coli.
· Sayed et al [13] prepared a series of 3-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-2-(2- hydroxy-3,5-diiodophenyl)-thiazolidin -4-one (4) which showed antibacterial activity against E.coli,B.subtillis and S.typhi respectively.
B) ANTINEOPLASTIC ACTIVITY:
Anticancer drug or antineoplastic
drug, are such types drug that is effective in the treatment of cancerous
disease and malignant. They are classify several major classes of anticancer
drugs; these include antimetabolites, natural products, alkylating agents, and hormones.
There fore the researchers developed the new effective anti cancer drugs.
· Gududuru et al [14] prepared a series of 2-arylthiazolidine -4-carboxylic acid amides (5) that showed activity in prostate cancer.
· Raheman et al [15] prepared a series of thiazolidine derivatives (6) and showed activity against human cancer cells.
C) Analgesic Activity:
Analgesic drugs are used for relief from pain.
· Ottana et al [16] prepared 3,3’-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] (7) and analyzed for their analgesic activity.
· Bhati et al [17]investigated the analgesic activity of 2-aryl-3-{5-[([1,3,4]thiadiazino[6,5-b]indol-3-ylamino)methyl]-1,3,4-thiadiazol-2-yl}-1,3-thiazolidin-4-one (8).
D) Anti Inflammatory Activity:
· Uchova et al [18] prepared (5Z, E)-3-[2-(4-chlorophenyl)-2-oxoethyl]-5-(1H-indol-3-ylmethylene)-thiazolidine- 2,4-dione which showed 67.2% inhibition zone (9).
· Amin et al [19] investigated the series of spiro [(2H, 3H) quinazoline-2,10-cyclohexan]-4(1H)-one and analyzed their anti inflammatory activity (10).
· A series of 2-(3-Aryl-1-phenyl-1H-pyrazole-4-yl)-3-(4-fluorobenzyl)-4-oxothiazolidine compounds gave less activity compared to indomethacin (11).
E) Antidepressant Activity:
Antidepressants drugs are used for the treatment of major depressive disorder and other conditions like dysthymia, anxiety disorders etc.
· Akulla et al [20] investigated 3-[1H-benzimidazole-2-yl-amino]-2-phenyl-1,3-thiazolidin-4-one (12) gave the promising anti depressant activity.
· Series of 3-[(3-substituted-5-methyl-4-thiazolidinon-2 ylidene) hydrazono]-1H-2-indolinone (13) compounds gave anti depressant activity.
I. Marketed Drugs:
Pharmaceutical drugs are used to treat or cure or to prevent a disease or to promote well-being. The drug synthesized by organic reaction. The drug used in treatment of bacterial infection and also drug decrease the blood sugar in our body.
Rosiglitazone:
Its trade name is Avandia. It is an antidiabetic drug in the thiazolidine derivatives (14) class of drug. This drug used in decreasing blood sugar. [21]
Pioglitazone (15):
Its trade name is Actos. This drug is used in decrease the blood sugar and also used in cardiovascular treatment. It also used in the treatment of high depression in person. This drug is not used for with hypersensitivity person [22].
Benzylpenicillin (17):
It’s also known as a penicillin G. It is used in bacterial infection in body. This drug was discovered in 1929 and used in 1942. It is on the WHO List of Medicines, the most safe and effective medicines needed in a health System.
Teneligliptin (18):
It is also known as a Tenelia. It used in treatment of 2 types of diabetes mellitus.
CONCLUSION:
Finally, we may conclude that heterocyclic compounds containing thiazolidine moiety plays a very important role in the field of medicinal chemistry. It shows a wide range of biological activity ranging from anti-hypertensive, anti-malarial, anti-diabetic to simple anti inflammatory activity. Many of these are available in various dosage forms and marketed drugs widely as discussed in this review.
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Received on 02.05.2020 Modified on 18.05.2020
Accepted on 31.05.2020 ©AJRC All right reserved
Asian J. Research Chem. 2020; 13(4):283-286.
DOI: 10.5958/0974-4150.2020.00055.3