{"doi":"10.17615/cffm-d878","title":"Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors","abstract":"The current optimization of 2,4-diarylaniline analogs (DAANs) on the central phenyl ring provided a series of new active DAAN derivatives 9a–9e, indicating an accessible modification approach that could improve anti-HIV potency against wild-type and resistant strains, aqueous solubility, and metabolic stability. A new compound 9e not only exhibited extremely high potency against wild-type virus (EC50 0.53 nM) and several resistant viral strains (EC50 0.36 – 3.9 nM), but also showed desirable aqueous solubility and metabolic stability, which were comparable or better than those of the anti-HIV-1 drug TMC278 (2). Thus, new compound 9e might be a potential drug candidate for further development of novel next-generation NNRTIs.","journal":"UNC Libraries","year":2020,"id":142592,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":0,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9439,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":543891,"name":"Li Huang","orcid":"0000-0003-3910-3982","position":1,"is_corresponding":false},{"id":540035,"name":"Kuo Hsiung Lee","orcid":null,"position":2,"is_corresponding":false},{"id":519381,"name":"Lan Xie","orcid":"0000-0001-5831-8730","position":3,"is_corresponding":false},{"id":544635,"name":"Bingjie Qin","orcid":null,"position":4,"is_corresponding":false},{"id":536002,"name":"Keduo Qian","orcid":null,"position":5,"is_corresponding":false},{"id":607471,"name":"Lian Qi Sun","orcid":null,"position":6,"is_corresponding":false},{"id":540034,"name":"Chin Ho Chen","orcid":null,"position":0,"is_corresponding":true}],"reference_count":0,"raw_metadata":null,"created_at":"2026-07-18T23:17:31.424593Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}