Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists

Kim, Hyojin; Cho, Suk Joon; Yoo, Minjin; Kang, Seung Kyu; Kim, Kwang-Rok; Lee, Hwan Hee; Song, Jin Sook; Rhee, Sang Dal; Jung, Won Hoon; Ahn, Jin Hee; Jung, Jae‐Kyung; Jung, Kwan‐Young

doi:10.1016/j.bmcl.2017.10.046

Cited by 20 publications

(13 citation statements)

References 25 publications

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“…Kitas et al61 synthesized sulfonylureido thiazole derivatives and analyzed their inhibitory effect on fructose-1,6-bisphosphatase for the cure of non-insulin dependent diabetes. Compound 160 showed good activity in the inhibition of fructose-1,6-bisphosphatase for the cure of type-2 diabetes with IC 50 HL 0.13, HL IC 50 F2 0.09, ML EC 50 value 10.Kim et al117 synthesized new analogs containing 4-(phenoxymethyl) thiazole and analyzed these for antidiabetic activity. Using in vitro method, two derivatives 161 and 162 were screened for anti-diabetic activity taking GPR119 into consideration.…”

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confidence: 99%

Thiazoles: A Retrospective Study on Synthesis, Structure-activity Relationship and Therapeutic Significance

Sharma¹,

Devgun²,

Narang³

et al. 2022

IJPER

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Thiazole or 1,3-thiazole is a distinct heterocyclic compound which incorporates sulphur and nitrogen atoms. It is a vital framework present in numerous pharmacologically active compounds, be it of natural origin or of synthetic nature. Many thiazoles having antitumor and antiviral activities, originate from microbes and marine organisms. A variety of synthetic drugs, having thiazole group, like antimicrobial sulfathiazole, antibiotic penicillin, antidepressant pramipexole, antineoplastic agent bleomycin, antiretroviral drug ritonavir, histamine H 2 receptor antagonist nizatidine, anti-inflammatory drug meloxicam, antifungal stilbene derivatives have been in the markets for quite some time. Hofmann and Hantzsch laid the groundwork for further development in the field of thiazole chemistry. The interaction of α-haloketones or α-halogenaldehyde and thioamide to obtain thiazoles is beautifully described by Hantzsch. Various studies have reported methods for the synthesis of the thiazoles; thioforamide, thiourea, α-thiocyanotoketones, and vinyl bromide have been extensively employed to synthesize thiazoles. The thiazoles have immense potential and this study tries to enlighten the crucial role of thiazoles for the betterment of society. The review provides different directions in the synthesis of novel thiazoles and also reveals diverse targets for augmentation in the field of designing of novel thiazoles.

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confidence: 99%

Thiazoles: A Retrospective Study on Synthesis, Structure-activity Relationship and Therapeutic Significance

Sharma¹,

Devgun²,

Narang³

et al. 2022

IJPER

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“…A solution of tert -butyl 4-carbamothioylpiperidine-1-carboxylate 3 (8.25 mmol), which can be prepared from piperidine-4-carboxamide, 29 in tetrahydrofuran (50 mL) was added to the intermediate 2 (9.07 mmol) while stirring and refluxing for 3 h. The solvent was evaporated, and the residue was dissolved using ethyl acetate (50 mL). The organic layer was washed with sodium hydroxide solution (1 mol L −1 , 50 mL) and saturated brine (50 mL) successively and then dried over anhydrous sodium sulfate.…”

Section: Methodsmentioning

confidence: 99%

Design, synthesis and fungicidal activity of isothiazole–thiazole derivatives

Zhao

Fan

et al. 2018

RSC Adv.

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“…[54] Kim et al used the Lawesson's reagent (LR) to convert N-Boc-piperidine-4-carboxamide 104 to N-Boc-piperidine-4-carbothioamide 106 which was reacted with 1,3dichloroacetone 107 to give the thiazole 108 (Scheme 30). [55] Thiazole derivatives 113 were obtained by the reaction of 4 0 -trifluoromethyl-benzaldehyde 109 with thiosemicarbazide 110 in the presence of hydrochloric acid as a catalyst. Then, reacted 111 with various a-halogenated ketones 112 and yield thiazole derivatives 113 (Scheme 31).…”

Section: Scheme 25 Synthesis Of Thiazole Derivatives 88mentioning

confidence: 99%