Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate.


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
12 12 2019
Historique:
pubmed: 12 11 2019
medline: 23 6 2020
entrez: 12 11 2019
Statut: ppublish

Résumé

The identification of a novel class of potent pan-genotypic NS5A inhibitors with good pharmacokinetic profile suitable for potential use in treating HCV infections is disclosed here. The present series of compounds are with less complex tricyclic central core, identified through a systematic SAR study carried out on biphenyl moiety. The SAR outcome has confirmed the requirement of near planar and linear conformation of the molecule to achieve the best pan-genotypic activity. In addition, SAR with substituted imidazoles on improvement of antiviral activity is disclosed. The newly identified compounds

Identifiants

pubmed: 31710479
doi: 10.1021/acs.jmedchem.9b01562
doi:

Substances chimiques

Antiviral Agents 0
Viral Nonstructural Proteins 0
NS-5 protein, hepatitis C virus EC 2.7.7.48

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

10563-10582

Auteurs

Vidya Ramdas (V)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Rashmi Talwar (R)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Moloy Banerjee (M)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Advait Arun Joshi (AA)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Amit Kumar Das (AK)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Deepak Sahebrao Walke (DS)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Prashant Borhade (P)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Usha Dhayagude (U)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Rajesh Loriya (R)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Ganesh Gote (G)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Apparao Bommakanti (A)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Aruna Sivaram (A)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Gautam Agarwal (G)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Arnab Goswami (A)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Prashant Nigade (P)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Maneesh Mehta (M)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Vinod Patil (V)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Dipak Modi (D)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Hemant Kumar (H)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Sadanand Mallurwar (S)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Amruta Dash (A)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Falguni Modi (F)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Sandip Kuldharan (S)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Pratima Srivastava (P)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Minakshi Singh (M)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Lakshmi Narasimham (L)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Jayasagar Gundu (J)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Sharad Sharma (S)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Rajender Kumar Kamboj (RK)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Venkata P Palle (VP)

Novel Drug Discovery & Development , Lupin Ltd. , Lupin Research Park, Survey No. 46 A/47 A, Village Nande, Taluka Mulshi , Pune 412115 , India.

Articles similaires

Populus Soil Microbiology Soil Microbiota Fungi
Animals Swine Antiviral Agents Swine Diseases Coronavirus Infections
Humans Carcinoma, Hepatocellular Liver Neoplasms Aged United States
Triticum Transcription Factors Gene Expression Regulation, Plant Plant Proteins Salt Stress

Classifications MeSH