Synthesis of 2-Mercaptobenzimidazole Derivatives as Potential Anti-microbial and Cytotoxic Agents

被引：25

作者：

Hosamani, Kallappa M. ^{[1
]}

Shingalapur, Ramya V. ^{[1
]}

机构：

[1] Karnatak Univ, PG Dept Studies Chem, Dharwad 580003, Karnataka, India

来源：

ARCHIV DER PHARMAZIE | 2011年 / 344卷 / 05期

关键词：

Antibacterial; Antifungal; Cytotoxicity; 1,3,4-Oxadiazole; 4-Thiazolidinone; 1,3,4-OXADIAZOLE DERIVATIVES; BIOLOGICAL-ACTIVITY; ANTIFUNGAL; INHIBITORS; THIAZOLIDIN-4-ONES; 4-THIAZOLIDINONES; 5-LIPOXYGENASE; CYCLOOXYGENASE; ANTIBACTERIAL; CHEMISTRY;

D O I：

10.1002/ardp.200900291

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 2-(1H-benzimidazol-2-ylsulfanyl)-N-(4-oxo-2-phenyl-thiazolidin-3yl)-acetamide 5a-j have been synthesized from various aldehydes and 2-(5-phenyl-[1,3,4]-oxadiazol-2-ylmethylsulfanyl)-1H- benzimidazole 6a-j from various benzoic acids. These compounds were screened for their in-vitro anti-bacterial activity against Staphylococcus aureus and Enterococcus faecalis as Gram positive, Klebsiella pneumoniae and Escherichia coli as Gram negative bacterial strains and for in-vitro anti-fungal activity against Asperigillus fumigatus and Candida albicans. The in vitro cytotoxic properties were studied using brine shrimp bioassay. Results revealed that, compounds 5b, 5d, 5g, 5i, 6b, 6e, 6f, and 6i showed excellent activity against a panel of microorganisms. The cytotoxic activities of 5b, 5g, 5i, 6b, 6f, 6h, and 6i were found to be good. All the newly synthesized compounds were characterized by elemental analysis, IR, (1)H-NMR, (13)C-NMR and MS.

引用

页码：311 / 319

页数：9

共 31 条

[11]

HIREMATH SP, 1995, J INDIAN CHEM SOC, V72, P391

[12] The combinatorial synthesis of bicyclic privileged structures or privileged substructures [J].

Horton, DA ;

Bourne, GT ;

Smythe, ML .

CHEMICAL REVIEWS, 2003, 103 (03) :893-930

[13]

Hui XP, 2002, INDIAN J CHEM B, V41, P2176

[14] Synthesis of 3-[4′-(p-chlorophenyl)-thiazol-2′-yl]-2-[(substituted azetidinone/thiazolidinone)-aminomethyl]-6-bromoquinazolin-4-ones as anti-inflammatory agent [J].

Kumar, Ashok ;

Rajput, Chatrasal Singh ;

Bhati, Sudhir Kumar .

BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (08) :3089-3096

[15] Synthesis and Antimicrobial Activity of Some Novel 2-[4-(Substituted Piperazin-/Piperidin-1-ylcarbonyl)phenyl]-1H-benzimidazole Derivatives [J].

Kus, Canan ;

Soezuedoenmez, Fatma ;

Altanlar, Nurten .

ARCHIV DER PHARMAZIE, 2009, 342 (01) :54-60

[16] The identification of cyclooxygenase-1 inhibitors from 4-thiazolidinone combinatorial libraries [J].

Look, GC ;

Schullek, JR ;

Holmes, CP ;

Chinn, JP ;

Gordon, EM ;

Gallop, MA .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (06) :707-712

[17] BRINE SHRIMP - A CONVENIENT GENERAL BIOASSAY FOR ACTIVE-PLANT CONSTITUENTS [J].

MEYER, BN ;

FERRIGNI, NR ;

PUTNAM, JE ;

JACOBSEN, LB ;

NICHOLS, DE ;

MCLAUGHLIN, JL .

PLANTA MEDICA, 1982, 45 (01) :31-34

[18]

Mogilaiah K, 2004, INDIAN J CHEM B, V43, P2014

[19]

Moldovan CD, 2008, MATCH-COMMUN MATH CO, V60, P977

[20] Assessment of hypolipidaemic activity of three thiazolidin-4-ones in mice given high-fat diet and fructose [J].

Nampurath, Gopalan Kutty ;

Mathew, Surna P. ;

Khanna, Vivek ;

Zachariah, Robby T. ;

Kanji, Surnan ;

Chamallarnudi, Mallikarjuna Rao .

CHEMICO-BIOLOGICAL INTERACTIONS, 2008, 171 (03) :363-368

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