Synthesis, Antimicrobial Activities and Molecular Docking Studies of Novel 6-Hydroxybenzofuran-3(2H)-one Based 2,4-Disubstituted 1,3-Thiazoles

被引：0

作者：

Laczkowski, Krzysztof Z. ^{[1
]}

Misiura, Konrad ^{[1
]}

Biernasiuk, Anna ^{[2
]}

Malm, Anna ^{[2
]}

Siwek, Agata ^{[3
]}

Plech, Tomasz ^{[3
]}

机构：

[1] Nicholas Copernicus Univ, Fac Pharm, Dept Chem Technol & Pharmaceut, Coll Med, PL-85089 Bydgoszcz, Poland

[2] Med Univ Lublin, Fac Pharm, Dept Pharmaceut Microbiol, PL-20093 Lublin, Poland

[3] Med Univ Lublin, Fac Pharm, Dept Organ Chem, PL-20093 Lublin, Poland

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2013年 / 10卷 / 09期

关键词：

Thiazoles; Thiosemicarbazones; Benzofuranone; Antimicrobial drugs; N-myristoyltransferase; Molecular modeling; FUNGAL N-MYRISTOYLTRANSFERASE; IN-VITRO ACTIVITY; ANTIFUNGAL AGENTS; CRYSTAL-STRUCTURE; CANDIDA-ALBICANS; 2-THIAZOLYLHYDRAZONE DERIVATIVES; BIOLOGICAL EVALUATION; ASYMMETRIC-SYNTHESIS; INHIBITORS; THIAZOLES;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis, characterization and investigation of antibacterial and antifungal activities of thirteen novel 6-hydroxybenzofuran-3(2H)-one based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using NMR, FAB MS and HRMS analyses. The results of microbiological screening reveal that three derivatives containing fluorine, bromine and hydrogen substituents at the phenyl ring are the most active antimicrobial compounds. Molecular docking studies of all compounds on the active sites of microbial enzymes indicated a possible target N-myristoyltransferase (NMT).

引用

页码：798 / 807

页数：10

共 50 条

[1] Facile and convenient synthesis of 2,4-disubstituted and 2,3,4-trisubstituted 1,3-thiazoles
Hassan, Alaa A.
Mohamed, Shaaban K.
Mohamed, Nasr K.
El-Shaieb, Kamal M. A.
Abdel-Aziz, Ahmed T.
Mague, Joel T.
Akkurt, Mehmet
JOURNAL OF SULFUR CHEMISTRY, 2016, 37 (02) : 162 - 175
[2] Synthesis and Antimicrobial Activity of Novel 2,4-Disubstituted Thiazoles
Tran Nguyen Minh An
Lee, Kap Duk
ASIAN JOURNAL OF CHEMISTRY, 2013, 25 (18) : 10160 - 10164
[3] REACTION OF 1-ALKYNYL THIOCYANATES WITH NUCLEOPHILIC-REAGENTS - SYNTHESIS OF 2,4-DISUBSTITUTED 1,3-THIAZOLES
DEJONG, RLP
MEIJER, J
SUKHAI, RS
BRANDSMA, L
RECUEIL DES TRAVAUX CHIMIQUES DES PAYS-BAS-JOURNAL OF THE ROYAL NETHERLANDS CHEMICAL SOCIETY, 1982, 101 (09): : 310 - 313
[4] Synthesis of some novel 2,4-disubstituted thiazoles as possible antimicrobial agents
Wagle, Shivananda
Adhikari, Airody Vasudeva
Kumari, Nalilu Suchetha
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2008, 183 (05) : 1285 - 1300
[5] Synthesis of some novel 2,4-disubstituted thiazoles as possible antimicrobial agents
Karegoudar, Prakash
Karthikeyan, Mari Sithambaram
Prasad, Dasappa Jagadeesh
Mahalinga, Manjathuru
Holla, Bantwal Shivarama
Kumari, Nalilu Sucheta
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2008, 43 (02) : 261 - 267
[6] SIMPLE NEW SYNTHESES OF 2,4-DISUBSTITUTED AND 2,4,5-TRISUBSTITUTED 1,3-THIAZOLES
DUBS, P
STUESSI, R
SYNTHESIS-STUTTGART, 1976, (10): : 696 - 697
[7] Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine
Tran Nguyen Minh An
Pham Thai Phuong
Nguyen Minh Quang
Nguyen Van Son
Nguyen Van Cuong
Le Van Tan
Mai Dinh Tri
Alam, Mahboob
Pham Van Tat
CURRENT ORGANIC SYNTHESIS, 2020, 17 (02) : 151 - 159
[8] A Novel One-Pot Multicomponent Enzymatic Synthesis of 2,4-Disubstituted Thiazoles
Zhang, Huiping
CATALYSIS LETTERS, 2014, 144 (05) : 928 - 934
[9] A Novel One-Pot Multicomponent Enzymatic Synthesis of 2,4-Disubstituted Thiazoles
Huiping Zhang
Catalysis Letters, 2014, 144 : 928 - 934
[10] Synthesis, characterization and anti-microbial studies of some novel 2,4-disubstituted thiazoles
Vijesh, A. M.
Isloor, Arun M.
Prabhu, Vivek
Ahmad, Shaoib
Malladi, Shridhar
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2010, 45 (11) : 5460 - 5464

← 1 2 3 4 5 →