Antileishmanial evaluation of triazole–butenolide conjugates: design, synthesis, in vitro screening, SAR and in silico ADME predictions

Author:

Pandey Alka Raj12,Singh Suriya Pratap1,Ramalingam Karthik3,Yadav Kanchan4ORCID,Bisen Amol Chhatrapati56,Bhatta Rabi Sankar56ORCID,Srivastava Mrigank4,Tripathi Renu4,Goyal Neena3,Sashidhara Koneni V.126ORCID

Affiliation:

1. Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P, India

2. Sophisticated Analytical Instrument Facility & Research, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P, India

3. Division of Biochemistry and Structural Biology, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P, India

4. Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, Lucknow 226031, U.P, India

5. Pharmaceutics and Pharmacokinetics Division, CSIR-Central Drug Research Institute, Lucknow 226031, U.P, India

6. Academy of Scientific and Innovative Research (AcSIR), Ghaziabad-201002, U.P, India

Abstract

Synthesis of a novel series of 23 triazole–butenolide conjugates utilizing click chemistry and their antileishmanial, antimalarial, and antifilarial activity along with SAR, ADME predictions and pharmacokinetic study are discussed.

Funder

Department of Science and Technology, Ministry of Science and Technology, India

Indian Council of Medical Research

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

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