Synthesis and in-vitro anti-leishmanial activity of (4-arylpiperazin-1-yl)(1-(thiophen-2-yl)-9H-pyrido[3,4-b]indol-3-yl)methanone derivatives |
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| Affiliation: | 1. Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India;2. Department of Applied Biology and Chemical Technology and State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Hong Kong;3. Department of Biological Sciences, Birla Institute of Technology & Science, Pilani 333031, Rajasthan, India;1. Colorado College, Department of Chemistry and Biochemistry, 14 E. Cache La Poudre, Colorado Springs, CO 80903, United States;2. Instituto de Parasitología y Biomedicina “López-Neyra” Consejo Superior de Investigaciones Científicas (CSIC), Granada 18100, Spain;1. Université de Lyon, UMR 5086 CNRS/Université Lyon 1, IBCP, 69367 Lyon, France;2. Department of Applied Biology and Chemical Technology, and State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Hung Hom, Hong Kong Special Administrative Region;1. Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India;2. Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India;1. Department of Life Sciences, School of Natural Sciences, Shiv Nadar University, India;2. Department of Chemistry, School of Natural Sciences, Shiv Nadar University, India;3. Department of Physics, School of Natural Sciences, Shiv Nadar University, India;4. Special Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi, India;1. Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, India;2. Department of Applied Chemistry, Giani Zail Singh Campus College of Engineering & Technology, MRSPTU, Dabwali Road, Bathinda, 151001, India |
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| Abstract: | In the present study, we have reported synthesis and biological evaluation of a series of fifteen 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole derivatives against both promastigotes and amastigotes of Leishmania parasites responsible for visceral (L. donovani) and cutaneous (L. amazonensis) leishmaniasis. Among these reported analogues, compounds 7b, 7c, 7f, 7g, 7i, 7j, 7m, 7o displayed potent activity (15.55, 7.70, 7.00, 3.80, 14.10, 9.25, 3.10, 4.85 μM, respectively) against L. donovani promastigotes than standard drugs miltefosine (15.70 μM) and pentamidine (32.70 μM) with good selectivity index. In further, in-vitro evaluation against amastigote forms, two compounds 7g (8.80 μM) and 7i (7.50 μM) showed significant inhibition of L. donovani amastigotes. Standard drug amphotericin B is also used as control to compare inhibition potency of compounds against both promastigote (0.24 μM) and amastigote (0.05 μM) forms. |
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| Keywords: | Leishmaniasis Promastigote Amastigote β-carboline |
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