title: Synthesis and antifilarial activity of chalcone-thiazole derivatives against a human lymphatic filarial parasite, Brugia malayi.
abstract: Here we report the synthesis of novel chalcone-thiazole compounds and their antifilarial activity. The antifilarial properties of these hybrids were assessed against microfilariae as well as adult worms of Brugia malayi. Among all the synthesized compounds, only two compounds, namely 4g and 4n were identified to be promising in vitro. These active compounds were tested in B. malayi-jird (Meriones unguiculatus) and B. malayi-Mastomys coucha models. Compound 4n showed 100% embryostatic effect and 49% macrofilaricidal in jirds and M. coucha models, respectively. This study provides a new structural clue for the development of novel antifilarial lead molecules.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, Uttar Pradesh 226031, India. Electronic address: sashidhar123@gmail.com.
authors.forename: Koneni V
authors.initials: KV
authors.lastname: Sashidhara
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, Uttar Pradesh 226031, India.
authors.forename: K Bhaskara
authors.initials: KB
authors.lastname: Rao
authors.affiliation: Division of Parasitology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Vikas
authors.initials: V
authors.lastname: Kushwaha
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, Uttar Pradesh 226031, India.
authors.forename: Ram K
authors.initials: RK
authors.lastname: Modukuri
authors.affiliation: Division of Parasitology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Richa
authors.initials: R
authors.lastname: Verma
authors.affiliation: Division of Parasitology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India. Electronic address: drpkmurthy@yahoo.com.
authors.forename: P K
authors.initials: PK
authors.lastname: Murthy
mesh_terms: D000818:Animals; D017178:Brugia malayi / Q000187:drug effects*; D002599:Chalcone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005260:Female; D005368:Filariasis / Q000188:drug therapy* / Q000469:parasitology; D005369:Filaricides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005849:Gerbillinae; D008297:Male; D015394:Molecular Structure; D051189:Murinae; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D005369:Filaricides; D013844:Thiazoles; D002599:Chalcone
keywords: Albendazole; Brugia malayi; Diethylcarbamazine; Ivermectin; Macrofilariae; Microfilariae