title: Triazino indole-quinoline hybrid: a novel approach to antileishmanial agents.
abstract: A novel series of 1,2,4-triazino-[5,6b]indole-3-thione covalently linked to 7-chloro-4-aminoquinoline have been synthesized and evaluated for their in vitro activity against extracellular promastigote and intracellular amastigote form of Leishmania donovani. Among all tested compounds, compounds 7a and 7b were found to be the most active with IC50 values 1.11, 0.36μM and selectivity index (SI) values 67, >1111, respectively, against amastigote form of L. donovani which is several folds more potent than the standard drugs, miltefosine (IC50=8.10μM, SI=7) and sodium stibo-gluconate (IC50=54.60μM, SI⩾7).
authors: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors: Rashmi
authors: R
authors: Sharma
authors: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors: Anand Kumar
authors: AK
authors: Pandey
authors: Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors: Rahul
authors: R
authors: Shivahare
authors: Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors: Khushboo
authors: K
authors: Srivastava
authors: Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
authors: Suman
authors: S
authors: Gupta
authors: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India. Electronic address: prem_chauhan_2000@yahoo.com.
authors: Prem M S
authors: PM
authors: Chauhan
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014227:Triazines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000634:Aminoquinolines; D000981:Antiprotozoal Agents; D007211:Indoles; D014227:Triazines; C047186:7-chloro-4-aminoquinoline
keywords: Antileishmanial; Hybrid; In vitro; Leishmania donovani; Quinoline; Triazino-indole