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2,4-Disubstituted thiazoles as multitargated bioactive molecules

  • Review Article
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Abstract

Thiazoles are important heterocyclics exhibiting boundaryless biological activities, such as antibacterial, antifungal, anti-inflammatory, antitumor, antitubercular, antidiabetic, antiviral, and antioxidant. Substituents on a particular position of the thiazole ring affect the biological outcomes to a great extent. Therefore, researchers have synthesized compounds containing the thiazole ring with variable substituents as target structures, and evaluated their biological activities. The present review describes the biological importance of recently developed 2,4-disubstituted thiazole derivatives. Moreover, we have thrown light on various targets of 2,4-disubstituted thiazoles through which they induce biological effects, which will be helpful to those who are working on the design and structure–activity relationship of bioactive molecules.

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Abbreviations

Akt:

A protein kinase B

AMPA:

α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor

CAs:

carbonic anhydrases

CDK7/9:

cyclin-dependent kinases 7/9

COX-2:

cyclooxygenase-2

DHFR:

dihydrofolate reductase

14α-DM:

14α-demethylase

DNA:

deoxyribonucleic acid

DPP IV:

dipeptidyl peptidase IV

ED50 :

effective dose, 50 %

Env protein:

envelope protein

mtFabH:

Mycobacterium tuberculosis β-ketoacyl-acyl carrier protein synthase III encoded by FabH gene

FOXM1:

forkhead box M1

GABAA α2/α3:

γ-aminobutyric acid type A receptors containing α2/α3 subunits

GGR:

glucagon receptor

GI50 :

growth inhibition, 50 %

GIP-R:

gastric inhibitory polypeptide receptor

mGlu5:

metabotropic glutamate receptor subtype 5

GPase:

glycogen phosphorylases

HATs:

histone acetyltransferases

HCV NS3/5A:

hepatitis C virus non-structural protein 3/5A

HDACs:

histone deacetylases

HIV:

human immunodeficiency virus

11β-HSD1:

11-β-hydroxysteroid dehydrogenase type 1

HSV UL5/8/52:

Herpes simplex virus helicase-primase complex

IKK β:

inhibitor of nuclear factor kappa-B kinase subunit beta

IMPd:

inosine monophosphate dehydrogenase

InhA:

enoyl–acyl carrier protein reductase encoded by inhA gene

JAK1:

Janus kinase 1

JUNV:

Junin virus

KCNQ1:

potassium voltage-gated channel KQT-like subfamily member 1

Kv7.1:

voltage-gated potassium channel

LD50 :

lethal dose, 50 %

MetAP:

methionine aminopeptidase

MGIT:

mycobacterial growth indicator tube

MG-MID:

mean-graph midpoint value

MIC:

minimum inhibitory concentration

MM2:

a molecular mechanics force field

MycG B:

mycobacterial gyrase B

NFκB:

nuclear factor kappa beta

NMDAR:

N-methyl-D-aspartate receptor

NO•:

nitric oxide radical

Nrf2:

nuclear factor erythroid 2-related factor 2

OH•:

hydroxyl radical

PADs:

protein arginine deiminases

PBP:

penicillin-binding protein

PD50 :

protective dose, 50 %

PDE4:

phosphodiesterase-4

PGE2:

prostaglandin E2

PI3 kinase:

phosphoinositide 3-kinase

PIKfyve:

phosphatidylinositol 3-phosphate 5-kinase

PPARγ:

peroxisome proliferator-activated receptors gamma

PRMTs:

protein arginine methyl transferases

PTPs:

protein tyrosine phosphatases

ROO•:

alkyl peroxy radical

RT RNase H:

reverse transcriptase-associated ribonuclease H

SAR:

structure–activity relationship

SGLT 2:

sodium glucose co-transporter 2

SK channel:

small-conductance calcium-activated potassium channels

SMT:

sterol 24-C-methyltransferase

SphK1:

sphingosine kinase 1

23S rRNA-L11:

L11 binding domain of 23S ribosomal RNA

TD50 :

toxic dose, 50 %

TGI:

total growth inhibition

TI value:

therapeutic index value

TNF-α:

tumor necrosis factor alpha

Topo II:

type II topoisomerases

UDP Glmutase:

UDP-galactopyranosemutase

WHO:

World Health Organization

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  1. Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Phagwara 144401, Punjab, India

    Preeti Arora, Rakesh Narang, Surendra Kumar Nayak & Sachin Kumar Singh

  2. Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar 125001, Haryana, India

    Vikramjeet Judge

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Arora, P., Narang, R., Nayak, S.K. et al. 2,4-Disubstituted thiazoles as multitargated bioactive molecules. Med Chem Res 25, 1717–1743 (2016). https://doi.org/10.1007/s00044-016-1610-2

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