Literature DB >> 16759086

Discovery of new antitubercular oxazolyl thiosemicarbazones.

Dharmarajan Sriram1, Perumal Yogeeswari, Rathinasababathy Thirumurugan, Roheet Kumar Pavana.   

Abstract

Twenty 4-(5-cyclobutyloxazol-2-yl)thiosemicarbazones were synthesized and evaluated for preliminary in vitro and in vivo activity against Mycobacterium tuberculosis H37Rv (MTB) and multidrug-resistant Mycobacterium tuberculosis (MDR-TB). Among them, (4-bromophenyl)(phenyl)methanone N-(5-cyclobutyl-1,3-oxazol-2-yl)thiosemicarbazone 6q was found to be the most active compound in vitro with minimum inhibitory concentration of 0.05 microg/mL against MTB and MDR-TB. In the in vivo animal model 6q decreased the bacterial load in lung and spleen tissues with 2.1 log 10 and 3.72 log 10 protections, respectively, at 50 mg/kg body weight dose.

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Year:  2006        PMID： 16759086     DOI： 10.1021/jm060339h

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  9 in total

1.  Improving Antimicrobial Activity and Physico-Chemical Properties by Isosteric Replacement of 2-Aminothiazole with 2-Aminooxazole.

Authors:  Martin Juhás; Andrea Bachtíková; Daria Elżbieta Nawrot; Paulína Hatoková; Vinod Sukanth Kumar Pallabothula; Adéla Diepoltová; Ondřej Janďourek; Pavel Bárta; Klára Konečná; Pavla Paterová; Vít Šesták; Jan Zitko
Journal:  Pharmaceuticals (Basel)       Date:  2022-05-06

2.  Design, Synthesis, Antibacterial Evaluations and In Silico Studies of Novel Thiosemicarbazides and 1,3,4-Thiadiazoles.

Authors:  Sara Janowska; Dmytro Khylyuk; Sylwia Andrzejczuk; Monika Wujec
Journal:  Molecules       Date:  2022-05-15       Impact factor: 4.927

3.  Synthesis and Antimycobacterial Activity of some Triazole Derivatives-New Route to Functionalized Triazolopyridazines.

Authors:  Kamaleddin Haj Mohammad Ebrahim Tehrani; Vida Mashayekhi; Parisa Azerang; Somayeh Minaei; Soroush Sardari; Farzad Kobarfard
Journal:  Iran J Pharm Res       Date:  2015       Impact factor: 1.696

4.  Synthesis, Characterization and Antibacterial Activity of some Novel Thiosemicarbazides, 1,2,4-Triazol-3-thiols and their S-substituted Derivatives.

Authors:  Mehdi Kalhor; Mahboobeh Shabani; Iraj Nikokar; Seyedeh Reyhaneh Banisaeed
Journal:  Iran J Pharm Res       Date:  2015       Impact factor: 1.696

5.  Crystal structure and Hirshfeld surface analysis of (E)-2-(5-bromo-2-hy-droxy-benzyl-idene)hydrazine-carbo-thio-amide di-methyl sulfoxide monosolvate.

Authors:  Palaniyappan Sivajeyanthi; Muthaiah Jeevaraj; Bellarmin Edison; Kasthuri Balasubramani
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2018-01-09

6.  Synthesis and Biological Evaluation of Thiosemicarbazide Derivatives Endowed with High Activity toward Mycobacterium Bovis.

Authors:  Soroush Sardari; Samaneh Feizi; Ali Hossein Rezayan; Parisa Azerang; Seyyed Mohammad Shahcheragh; Ghazaleh Ghavami; Azizollah Habibi
Journal:  Iran J Pharm Res       Date:  2017       Impact factor: 1.696

7.  Preparation, structure elucidation, and antioxidant activity of new bis(thiosemicarbazone) derivatives.

Authors:  Hasan Yakan
Journal:  Turk J Chem       Date:  2020-08-18       Impact factor: 1.239

8.  Synthesis, Structure and Antioxidant Activity of (Tetra-O-acetyl-β-D-galactopyranosyl)thiosemicarbazones of Substituted Benzaldehydes.

Authors:  Nguyen D Thanh; Le T Hoai
Journal:  Indian J Pharm Sci       Date:  2012-01       Impact factor: 0.975

9.  Synthesis and Bioactivity of Thiosemicarbazones Containing Adamantane Skeletons.

Authors:  Van Hien Pham; Thi Phuong Dung Phan; Dinh Chau Phan; Binh Duong Vu
Journal:  Molecules       Date:  2020-01-13       Impact factor: 4.411
  9 in total

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