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New carbodithioate derivatives: synthesis, characterization, and in vitro antibacterial, antifungal, antitubercular, and antimalarial activity

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Abstract

A series of structurally new, 2-(5-substituted-2,3-dioxoindolin-1-yl)ethyl/propyl 4-(3,4-dichlorophenyl)piperazine-1-carbodithioate derivatives 5a–j were designed and synthesized by conventional technique as well as ultrasound irradiation. All the new compounds were characterized by spectral and elemental analyses. Furthermore, they were evaluated for their in vitro antibacterial, antifungal, antitubercular, and antimalarial activities. The results indicated that some of the synthesized compounds posses promising antimicrobial activity against some gram-positive and gram-negative bacteria. Compounds 5b, 5d, and 5e displayed the highest inhibition (99 %) in the range of 3.10–6.25 μg/ml against Mycobacterium tuberculosis H 37 Rv, while compounds 5b–g displayed promising antimalarial activity in the range of 0.043–0.092 μg/mL against Plasmodium falciparum 3D7. Thus, these molecules can provide prospective leads in chemotherapy against tuberculosis and malaria.

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Acknowledgments

The author wish to express his thanks to Chairman—Charutar Vidya Mandal (Dr. C.L. Patel), Director —SICART (Dr. V.S. Patel) and Director—ARIBAS (Dr. P.S. Patel) for providing necessary research facilities. We are also thankful to Mr. Priyakant R. Raval and Dr. Kishor R. Desai, Director, Department of Chemistry, Uka—Tarsadia University, Bardoli, for research advice and encouragement.

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  1. Department of Pharmaceutical Chemistry, Ashok & Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences (ARIBAS), New Vallabh Vidyanagar, 388121, Gujarat, India

    Tarunkumar Nanjibhai Akhaja & Jignesh Priyakant Raval

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  1. Tarunkumar Nanjibhai Akhaja
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  2. Jignesh Priyakant Raval
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Correspondence to Tarunkumar Nanjibhai Akhaja.

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Akhaja, T.N., Raval, J.P. New carbodithioate derivatives: synthesis, characterization, and in vitro antibacterial, antifungal, antitubercular, and antimalarial activity. Med Chem Res 22, 4700–4707 (2013). https://doi.org/10.1007/s00044-013-0472-0

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