{"doi":"10.1128/aac.01715-21","title":"Fluorine Modifications Contribute to Potent Antiviral Activity against Highly Drug-Resistant HIV-1 and Favorable Blood-Brain Barrier Penetration Property of Novel Central Nervous System-Targeting HIV-1 Protease Inhibitors <i>In Vitro</i>","abstract":"To date, there are no specific treatment regimens for HIV-1-related central nervous system (CNS) complications, such as HIV-1-associated neurocognitive disorders (HAND). Here, we report that two newly generated CNS-targeting HIV-1 protease (PR) inhibitors (PIs), GRL-08513 and GRL-08613, which have a P1-3,5- bis -fluorophenyl or P1- para -monofluorophenyl ring and P2-tetrahydropyrano-tetrahydrofuran ( Tp -THF) with a sulfonamide isostere, are potent against wild-type HIV-1 strains and multiple clinically isolated HIV-1 strains (50% effective concentration [EC 50 ]: 0.0001 to ∼0.0032 μM).","journal":"Antimicrobial Agents and Chemotherapy","year":2022,"id":274887,"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":9,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9547,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2022-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":943915,"name":"Ravikiran S. Yedidi","orcid":"0000-0003-2755-1307","position":1,"is_corresponding":false},{"id":944509,"name":"Pedro Miguel Salcedo-Gómez","orcid":null,"position":2,"is_corresponding":false},{"id":295828,"name":"Hironori Hayashi","orcid":"0000-0002-5892-0040","position":3,"is_corresponding":false},{"id":623764,"name":"Kazuya Hasegawa","orcid":"0000-0003-0331-1624","position":4,"is_corresponding":false},{"id":50463,"name":"Cuthbert D. Martyr","orcid":null,"position":5,"is_corresponding":false},{"id":233704,"name":"Arun K. Ghosh","orcid":"0000-0003-2472-1841","position":6,"is_corresponding":false},{"id":295833,"name":"Hiroaki Mitsuya","orcid":"0000-0001-9274-3853","position":7,"is_corresponding":false},{"id":651046,"name":"Masayuki Amano","orcid":"0000-0003-0516-9502","position":0,"is_corresponding":true}],"reference_count":73,"raw_metadata":null,"created_at":"2026-07-19T00:28:16.928746Z","pmid":"34978889","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":[]}