title: 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.
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, 4.85μM, respectively) against L. donovani promastigotes than standard drugs miltefosine (15.70μM) and pentamidine (32.70μM) with good selectivity index. In further, in-vitro evaluation against amastigote forms, two compounds 7g (8.80μM) and 7i (7.50μM) 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 (0.24μM) and amastigote (0.05μM) forms.
authors.affiliation: Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India. Electronic address: penta.ashok@gmail.com.
authors.forename: Penta
authors.initials: P
authors.lastname: Ashok
authors.affiliation: Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India.
authors.forename: Subhash
authors.initials: S
authors.lastname: Chander
authors.affiliation: Department of Applied Biology and Chemical Technology and State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Hong Kong. Electronic address: larry.chow@polyu.edu.hk.
authors.forename: Larry M C
authors.initials: LM
authors.lastname: Chow
authors.affiliation: Department of Applied Biology and Chemical Technology and State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Hong Kong.
authors.forename: Iris L K
authors.initials: IL
authors.lastname: Wong
authors.affiliation: Department of Biological Sciences, Birla Institute of Technology & Science, Pilani 333031, Rajasthan, India.
authors.forename: Rajnish Prakash
authors.initials: RP
authors.lastname: Singh
authors.affiliation: Department of Biological Sciences, Birla Institute of Technology & Science, Pilani 333031, Rajasthan, India.
authors.forename: Prabhat Nath
authors.initials: PN
authors.lastname: Jha
authors.affiliation: Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India. Electronic address: murugesan@pilani.bits-pilani.ac.in.
authors.forename: Murugesan
authors.initials: M
authors.lastname: Sankaranarayanan
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D002478:Cells, Cultured; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D007891:Leishmania / Q000187:drug effects*; D007893:Leishmania donovani / Q000187:drug effects; D007896:Leishmaniasis / Q000188:drug therapy / Q000469:parasitology; D008264:Macrophages / Q000469:parasitology; D051379:Mice; D013876:Thiophenes / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000981:Antiprotozoal Agents; D007211:Indoles; D013876:Thiophenes
keywords: Amastigote; Leishmaniasis; Promastigote; β-carboline