http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
- 中文 을 입력하시려면 zhongwen을 입력하시고 space를누르시면됩니다.
- 北京 을 입력하시려면 beijing을 입력하시고 space를 누르시면 됩니다.
RISS 인기검색어
- 검색키워드
- 저자 : Muqadar, Urooj (검색결과 1 건)
- 무료
- 기관 내 무료
- 유료
-
Larik, Fayaz Ali,Saeed, Aamer,Channar, Pervaiz Ali,Muqadar, Urooj,Abbas, Qamar,Hassan, Mubashir,Seo, Sung-Yum,Bolte, Michael S.E.C.T. [etc.] 2017 European journal of medicinal chemistry Vol.141 No.-
<P><B>Abstract</B></P> <P>A series of novel 1-pentanoyl-3-arylthioureas was designed as new mushroom tyrosinase inhibitors and free radical scavengers. The title compounds were obtained in excellent yield and characterized by FTIR, <SUP>1</SUP>H NMR, <SUP>13</SUP>C NMR and X-ray crystallography in case of compound (<B>4a</B>). The inhibitory effects on mushroom tyrosinase and DPPH were evaluated and it was observed that 1-Pentanoyl-3-(4-methoxyphenyl) thiourea (<B>4f</B>) showed tyrosinase inhibitory activity (IC<SUB>50</SUB> 1.568 ± 0.01 mM) comparable to Kojic acid (IC<SUB>50</SUB> 16.051 ± 1.27 mM). Interestingly compound <B>4f</B> exhibited higher antioxidant potential compared to other derivatives. The docking studies of synthesized 1-Pentanoyl-3-arylthioureas analogues were also carried out against tyrosinase protein (PDBID 2ZMX) to compare the binding affinities with IC<SUB>50</SUB> values. The predicted binding affinities are in good agreement with the IC<SUB>50</SUB> values as compound (<B>4f</B>) showed highest binding affinity (−7.50 kcal/mol) compared to others derivatives. The kinetic mechanism analyzed by Line-weavere Burk plots exhibited that compound (<B>4f</B>) inhibit the enzyme inhibits the tyrosinase non-competitively to form an enzyme inhibitor complex. The inhibition constants Ki calculated from Dixon plots for compound (<B>4f</B>) is 1.10 μM. It was also found from kinetic analysis that derivative <B>4f</B> irreversible enzyme inhibitor complex. It is proposed on the basis of our investigation that title compound (<B>4f</B>) may serve as lead structure for the design of more potent tyrosinase inhibitors.</P> <P><B>Highlights</B></P> <P> <UL> <LI> A small library of novel 1-Pentanoyl-3-arylthioureas (<B>4a-4j</B>) synthesized. </LI> <LI> Mushroom tyrosinase inhibition and free radical scavenging activity were evaluated. </LI> <LI> Most of the compounds show excellent activity, particularly <B>4f</B> higher than the standard. </LI> <LI> The kinetic mechanism proposed <B>4f</B> is non-competitive inhibitor of mushroom tyrosinase. </LI> <LI> Molecular docking, druglikeness, Ramachandran graph, Chemo-informatics and Lipinski's rule were studied. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
연관 검색어 추천
이 검색어로 많이 본 자료
활용도 높은 자료
