Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents

Özlen GÜZEL AKDEMİR, (İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, İstanbul, Türkiye)
Kübra DEMİR-YAZICI, (İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, İstanbul, Türkiye)
Muhammed TRAWALLY, (İstanbul Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, İstanbul, Türkiye)
Serap İpek DİNGİŞ BİRGÜL, (Bezmialem Vakıf Üniversitesi, Eczacılık Fakültesi, Farmakoloji Anabilim Dalı, Bilgisayar Destekli İlaç Keşif Laboratuvarı, İstanbul, Türkiye)
Atilla AKDEMİR (Bezmialem Vakıf Üniversitesi, Eczacılık Fakültesi, Farmakoloji Anabilim Dalı, Bilgisayar Destekli İlaç Keşif Laboratuvarı, İstanbul, Türkiye)
Organic Communications
2 0
Yıl: 2020 Cilt: 13 Sayı: 2 Sayfa Aralığı: 33 - 50 Metin Dili: İngilizce DOI: http://doi.org/10.25135/acg.oc.78.20.05.1655 İndeks Tarihi: 17-12-2020

Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents

Öz:
A small collection of 2-hydroxy-N-(5-methyl/nonsubstituted 4-oxo-2-substituted phenyl-1,3-thiazolidin-3-yl)-2-phenylacetamides (3-16) was synthesized from the cyclocondensation of 2-hydroxy-2-phenyl-N'-[(substitutedphenyl)methylene]acetohydrazides (2) and mercaptoethanoic acid or 2-mercaptopropanoic acid,characterized with spectral and elemental analysis. In order to explore their antimycobacterial potential, newlysynthesized fourteen compounds were screened for their inhibitory activity against Mycobacterium tuberculosis strainH37Rv at 6.25 μg/mL with in-vitro primary tests. Compound 7 was found to provide the highest inhibition (98%) M.tuberculosis strain H37Rv, while most of the new derivatives showed different inhibition ratios. For the search of theputative targets which are considered as related to the antimycobacterial activity of these molecules, docking studieswere performed. With molecular dynamic simulations, further possible interactions between ligands and the active siteof the selected enzymes were investigated. Eventually, molecular modelling studies indicated that at least part of themechanism of action of these compounds may be mediated by inhibition of MtInhA.
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APA GÜZEL AKDEMIR O, Demir-Yazıcı K, Trawally M, Dingiş Birgül S, Akdemir A (2020). Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. , 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
Chicago GÜZEL AKDEMIR OZLEN,Demir-Yazıcı Kübra,Trawally Muhammed,Dingiş Birgül Serap İpek,Akdemir Atilla Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. (2020): 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
MLA GÜZEL AKDEMIR OZLEN,Demir-Yazıcı Kübra,Trawally Muhammed,Dingiş Birgül Serap İpek,Akdemir Atilla Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. , 2020, ss.33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
AMA GÜZEL AKDEMIR O,Demir-Yazıcı K,Trawally M,Dingiş Birgül S,Akdemir A Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. . 2020; 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
Vancouver GÜZEL AKDEMIR O,Demir-Yazıcı K,Trawally M,Dingiş Birgül S,Akdemir A Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. . 2020; 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
IEEE GÜZEL AKDEMIR O,Demir-Yazıcı K,Trawally M,Dingiş Birgül S,Akdemir A "Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents." , ss.33 - 50, 2020. http://doi.org/10.25135/acg.oc.78.20.05.1655
ISNAD GÜZEL AKDEMIR, OZLEN vd. "Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents". (2020), 33-50. https://doi.org/http://doi.org/10.25135/acg.oc.78.20.05.1655
APA GÜZEL AKDEMIR O, Demir-Yazıcı K, Trawally M, Dingiş Birgül S, Akdemir A (2020). Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. Organic Communications, 13(2), 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
Chicago GÜZEL AKDEMIR OZLEN,Demir-Yazıcı Kübra,Trawally Muhammed,Dingiş Birgül Serap İpek,Akdemir Atilla Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. Organic Communications 13, no.2 (2020): 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
MLA GÜZEL AKDEMIR OZLEN,Demir-Yazıcı Kübra,Trawally Muhammed,Dingiş Birgül Serap İpek,Akdemir Atilla Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. Organic Communications, vol.13, no.2, 2020, ss.33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
AMA GÜZEL AKDEMIR O,Demir-Yazıcı K,Trawally M,Dingiş Birgül S,Akdemir A Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. Organic Communications. 2020; 13(2): 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
Vancouver GÜZEL AKDEMIR O,Demir-Yazıcı K,Trawally M,Dingiş Birgül S,Akdemir A Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents. Organic Communications. 2020; 13(2): 33 - 50. http://doi.org/10.25135/acg.oc.78.20.05.1655
IEEE GÜZEL AKDEMIR O,Demir-Yazıcı K,Trawally M,Dingiş Birgül S,Akdemir A "Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents." Organic Communications, 13, ss.33 - 50, 2020. http://doi.org/10.25135/acg.oc.78.20.05.1655
ISNAD GÜZEL AKDEMIR, OZLEN vd. "Evaluation of new 2-hydroxy-N-(4-oxo-2-substituted phenyl-1,3- thiazolidin-3-yl)-2-phenylacetamide derivatives as potential antimycobacterial agents". Organic Communications 13/2 (2020), 33-50. https://doi.org/http://doi.org/10.25135/acg.oc.78.20.05.1655
Sayfa Oluşturulma Tarihi
23-04-2024 16:5

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