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Showing 193 to 198 of 198 entries
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Synthesis of Novel Thiazole Derivatives Bearing β-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens.

Molecules (Basel, Switzerland)

Malūkaitė D, Grybaitė B, Vaickelionienė R, Vaickelionis G, Sapijanskaitė-Banevič B, Kavaliauskas P, Mickevičius V.
PMID: 35011308
Molecules. 2021 Dec 23;27(1). doi: 10.3390/molecules27010074.

Rapidly growing antimicrobial resistance among clinically important bacterial and fungal pathogens accounts for high morbidity and mortality worldwide. Therefore, it is critical to look for new small molecules targeting multidrug-resistant pathogens. Herein, in this paper we report a synthesis,...

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Malūkaitė D, Grybaitė B, Vaickelionienė R, et al. Synthesis of Novel Thiazole Derivatives Bearing β-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens. Molecules. 2021;27(1)doi: 10.3390/molecules27010074.
Malūkaitė, D., Grybaitė, B., Vaickelionienė, R., Vaickelionis, G., Sapijanskaitė-Banevič, B., Kavaliauskas, P., & Mickevičius, V. (2021). Synthesis of Novel Thiazole Derivatives Bearing β-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens. Molecules (Basel, Switzerland), 27(1), . https://doi.org/10.3390/molecules27010074
Malūkaitė, Dovilė, et al. "Synthesis of Novel Thiazole Derivatives Bearing β-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens." Molecules (Basel, Switzerland) vol. 27,1 (2021). doi: https://doi.org/10.3390/molecules27010074
Malūkaitė D, Grybaitė B, Vaickelionienė R, Vaickelionis G, Sapijanskaitė-Banevič B, Kavaliauskas P, Mickevičius V. Synthesis of Novel Thiazole Derivatives Bearing β-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens. Molecules. 2021 Dec 23;27(1). doi: 10.3390/molecules27010074. PMID: 35011308.
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Semicarbazones, thiosemicarbazone, thiazole and oxazole analogues as monoamine oxidase inhibitors: Synthesis, characterization, biological evaluation, molecular docking, and kinetic studies.

Bioorganic chemistry

Qazi SU, Naz A, Hameed A, Osra FA, Jalil S, Iqbal J, Shah SAA, Mirza AZ.
PMID: 34364054
Bioorg Chem. 2021 Oct;115:105209. doi: 10.1016/j.bioorg.2021.105209. Epub 2021 Jul 27.

A series of semicarbazone, thiosemicarbazone, thiazole, and oxazole derivatives were designed, synthesized, and examined for monoamine oxidase inhibition using two isoforms, i.e., MAO-A and MAO-B. Among all the analogues, 3c and 3j possessed substantial activity against MAO-A with IC

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Qazi SU, Naz A, Hameed A, et al. Semicarbazones, thiosemicarbazone, thiazole and oxazole analogues as monoamine oxidase inhibitors: Synthesis, characterization, biological evaluation, molecular docking, and kinetic studies. Bioorg Chem. 2021;115:105209doi: 10.1016/j.bioorg.2021.105209.
Qazi, S. U., Naz, A., Hameed, A., Osra, F. A., Jalil, S., Iqbal, J., Shah, S. A. A., & Mirza, A. Z. (2021). Semicarbazones, thiosemicarbazone, thiazole and oxazole analogues as monoamine oxidase inhibitors: Synthesis, characterization, biological evaluation, molecular docking, and kinetic studies. Bioorganic chemistry, 115105209. https://doi.org/10.1016/j.bioorg.2021.105209
Qazi, Syeda Uroos, et al. "Semicarbazones, thiosemicarbazone, thiazole and oxazole analogues as monoamine oxidase inhibitors: Synthesis, characterization, biological evaluation, molecular docking, and kinetic studies." Bioorganic chemistry vol. 115 (2021): 105209. doi: https://doi.org/10.1016/j.bioorg.2021.105209
Qazi SU, Naz A, Hameed A, Osra FA, Jalil S, Iqbal J, Shah SAA, Mirza AZ. Semicarbazones, thiosemicarbazone, thiazole and oxazole analogues as monoamine oxidase inhibitors: Synthesis, characterization, biological evaluation, molecular docking, and kinetic studies. Bioorg Chem. 2021 Oct;115:105209. doi: 10.1016/j.bioorg.2021.105209. Epub 2021 Jul 27. PMID: 34364054.
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Simple Synthesis of a Heterocyclophane Exhibiting Anti-c-Met Activity by Acting as a Hatch Blocking Access to the Active Site*.

Chemistry (Weinheim an der Bergstrasse, Germany)

Takimoto T, Sasaki H, Tsue H, Takahashi H, MacKerell AD, Nakamura A, Nakano K, Okazaki E, Betsuyaku T, Tachibana R, Hioki K, Yoluk O, Jo S.
PMID: 33258147
Chemistry. 2021 Jan 21;27(5):1648-1654. doi: 10.1002/chem.202001382. Epub 2020 Dec 15.

A simple approach to the synthesis of heterocyclophane consisting of two 4,4'-bithiazoles has been developed in mild conditions. The heterocyclophane with two short chains was conveniently prepared by Hantzsch thiazoles synthesis using the reaction of 3-tert-butoxycarbonyl-3-azapentanethiocarboxamide with 1,4-dibromobutane-2,3-dione in...

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Takimoto T, Sasaki H, Tsue H, et al. Simple Synthesis of a Heterocyclophane Exhibiting Anti-c-Met Activity by Acting as a Hatch Blocking Access to the Active Site*. Chemistry. 2020;27(5):1648-1654doi: 10.1002/chem.202001382.
Takimoto, T., Sasaki, H., Tsue, H., Takahashi, H., MacKerell, A. D., Nakamura, A., Nakano, K., Okazaki, E., Betsuyaku, T., Tachibana, R., Hioki, K., Yoluk, O., & Jo, S. (2021). Simple Synthesis of a Heterocyclophane Exhibiting Anti-c-Met Activity by Acting as a Hatch Blocking Access to the Active Site*. Chemistry (Weinheim an der Bergstrasse, Germany), 27(5), 1648-1654. https://doi.org/10.1002/chem.202001382
Takimoto, Tatsuya, et al. "Simple Synthesis of a Heterocyclophane Exhibiting Anti-c-Met Activity by Acting as a Hatch Blocking Access to the Active Site*." Chemistry (Weinheim an der Bergstrasse, Germany) vol. 27,5 (2021): 1648-1654. doi: https://doi.org/10.1002/chem.202001382
Takimoto T, Sasaki H, Tsue H, Takahashi H, MacKerell AD, Nakamura A, Nakano K, Okazaki E, Betsuyaku T, Tachibana R, Hioki K, Yoluk O, Jo S. Simple Synthesis of a Heterocyclophane Exhibiting Anti-c-Met Activity by Acting as a Hatch Blocking Access to the Active Site*. Chemistry. 2021 Jan 21;27(5):1648-1654. doi: 10.1002/chem.202001382. Epub 2020 Dec 15. PMID: 33258147; PMCID: PMC7887132.
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Recent Trends for Drug Development for the treatment of Adenocarcinoma breast cancer: Thiazole, Triazole, and Thiosemicarbazone Analogues as Efficient Scaffolds.

Anti-cancer agents in medicinal chemistry

Scarim CB, Chin CM.
PMID: 34852749
Anticancer Agents Med Chem. 2021 Dec 01; doi: 10.2174/1871520621666211201152815. Epub 2021 Dec 01.

Thiazoles, triazoles, and thiosemicarbazones function as efficient scaffolds in compounds for the treatment of several illnesses, including cancers. In this review article, we demonstrate the various studies involving these three pharmacophore classes (thiazoles, triazoles, and thiosemicarbazones) in the medicinal...

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Scarim CB, Chin CM. Recent Trends for Drug Development for the treatment of Adenocarcinoma breast cancer: Thiazole, Triazole, and Thiosemicarbazone Analogues as Efficient Scaffolds. Anticancer Agents Med Chem. 2021;doi: 10.2174/1871520621666211201152815.
Scarim, C. B., & Chin, C. M. (2021). Recent Trends for Drug Development for the treatment of Adenocarcinoma breast cancer: Thiazole, Triazole, and Thiosemicarbazone Analogues as Efficient Scaffolds. Anti-cancer agents in medicinal chemistry, . https://doi.org/10.2174/1871520621666211201152815
Scarim, Cauê Benito, and Chin, Chung Man. "Recent Trends for Drug Development for the treatment of Adenocarcinoma breast cancer: Thiazole, Triazole, and Thiosemicarbazone Analogues as Efficient Scaffolds." Anti-cancer agents in medicinal chemistry vol. (2021). doi: https://doi.org/10.2174/1871520621666211201152815
Scarim CB, Chin CM. Recent Trends for Drug Development for the treatment of Adenocarcinoma breast cancer: Thiazole, Triazole, and Thiosemicarbazone Analogues as Efficient Scaffolds. Anticancer Agents Med Chem. 2021 Dec 01; doi: 10.2174/1871520621666211201152815. Epub 2021 Dec 01. PMID: 34852749.
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Nanomolar potency of imidazo[2,1-b]thiazole analogs as indoleamine 2,3-dioxygenase inhibitors.

Archiv der Pharmazie

Ewida MA, Ewida HA, Ahmed MS, Allam HA, ElBagary RI, George RF, Georgey HH, El-Subbagh HI.
PMID: 34313342
Arch Pharm (Weinheim). 2021 Nov;354(11):e2100202. doi: 10.1002/ardp.202100202. Epub 2021 Jul 27.

Novel series of imidazo[2,1-b]thiazole analogs were designed, synthesized, and biologically evaluated as indoleamine 2,3-dioxygenase (IDO1) inhibitors. Imidazo[2,1-b]thiazoles 6, 7, and 8 showed inhibitory profiles against IDO1 at IC

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Ewida MA, Ewida HA, Ahmed MS, et al. Nanomolar potency of imidazo[2,1-b]thiazole analogs as indoleamine 2,3-dioxygenase inhibitors. Arch Pharm (Weinheim). 2021;354(11):e2100202doi: 10.1002/ardp.202100202.
Ewida, M. A., Ewida, H. A., Ahmed, M. S., Allam, H. A., ElBagary, R. I., George, R. F., Georgey, H. H., & El-Subbagh, H. I. (2021). Nanomolar potency of imidazo[2,1-b]thiazole analogs as indoleamine 2,3-dioxygenase inhibitors. Archiv der Pharmazie, 354(11), e2100202. https://doi.org/10.1002/ardp.202100202
Ewida, Menna A, et al. "Nanomolar potency of imidazo[2,1-b]thiazole analogs as indoleamine 2,3-dioxygenase inhibitors." Archiv der Pharmazie vol. 354,11 (2021): e2100202. doi: https://doi.org/10.1002/ardp.202100202
Ewida MA, Ewida HA, Ahmed MS, Allam HA, ElBagary RI, George RF, Georgey HH, El-Subbagh HI. Nanomolar potency of imidazo[2,1-b]thiazole analogs as indoleamine 2,3-dioxygenase inhibitors. Arch Pharm (Weinheim). 2021 Nov;354(11):e2100202. doi: 10.1002/ardp.202100202. Epub 2021 Jul 27. PMID: 34313342.
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Organocatalytic Asymmetric Cascade Michael-acyl Transfer Reaction between 2-Fluoro-1,3-diketones and Unsaturated Thiazolones: Access to Fluorinated 4-Acyloxy Thiazoles.

Organic letters

Biswas RG, Ray SK, Unhale RA, Singh VK.
PMID: 34351776
Org Lett. 2021 Aug 20;23(16):6504-6509. doi: 10.1021/acs.orglett.1c02313. Epub 2021 Aug 05.

Quinine derived bifunctional urea catalyzed cascade Michael-acyl transfer reaction of 5-alkenyl thiazolones and monofluorinated β-diketones has been developed. The fluorine containing 4-acyloxy thiazoles were synthesized in high yields and good diastereo-and excellent enantioselectivities. Synthetic transformations, including synthesis of 4-hydroxy...

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Biswas RG, Ray SK, Unhale RA, et al. Organocatalytic Asymmetric Cascade Michael-acyl Transfer Reaction between 2-Fluoro-1,3-diketones and Unsaturated Thiazolones: Access to Fluorinated 4-Acyloxy Thiazoles. Org Lett. 2021;23(16):6504-6509doi: 10.1021/acs.orglett.1c02313.
Biswas, R. G., Ray, S. K., Unhale, R. A., & Singh, V. K. (2021). Organocatalytic Asymmetric Cascade Michael-acyl Transfer Reaction between 2-Fluoro-1,3-diketones and Unsaturated Thiazolones: Access to Fluorinated 4-Acyloxy Thiazoles. Organic letters, 23(16), 6504-6509. https://doi.org/10.1021/acs.orglett.1c02313
Biswas, Rayhan G, et al. "Organocatalytic Asymmetric Cascade Michael-acyl Transfer Reaction between 2-Fluoro-1,3-diketones and Unsaturated Thiazolones: Access to Fluorinated 4-Acyloxy Thiazoles." Organic letters vol. 23,16 (2021): 6504-6509. doi: https://doi.org/10.1021/acs.orglett.1c02313
Biswas RG, Ray SK, Unhale RA, Singh VK. Organocatalytic Asymmetric Cascade Michael-acyl Transfer Reaction between 2-Fluoro-1,3-diketones and Unsaturated Thiazolones: Access to Fluorinated 4-Acyloxy Thiazoles. Org Lett. 2021 Aug 20;23(16):6504-6509. doi: 10.1021/acs.orglett.1c02313. Epub 2021 Aug 05. PMID: 34351776.
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Showing 193 to 198 of 198 entries