{"doi":"10.1111/cbdd.13836","title":"Facile synthesis and antimycobacterial activity of isoniazid, pyrazinamide and ciprofloxacin derivatives","abstract":"Abstract Several rationally designed isoniazid (INH), pyrazinamide (PZA) and ciprofloxacin (CPF) derivatives were conveniently synthesized and evaluated in vitro against H37Rv Mycobacterium tuberculosis ( M. tb ) strain. CPF derivative 16 displayed a modest activity (MIC = 16 µg/ml) and was docked into the M. tb DNA gyrase. Isoniazid‐pyrazinoic acid (INH‐POA) hybrid 21a showed the highest potency in our study (MIC = 2 µg/ml). It also retained its high activity against the other tested M. tb drug‐sensitive strain (DS) V4207 (MIC = 4 µg/ml) and demonstrated negligible cytotoxicity against Vero cells (IC 50 ≥ 64 µg/ml). Four tested drug‐resistant (DR) M. tb strains were refractory to 21a , similar to INH, whilst being sensitive to CPF. Compound 21a was also inactive against two non‐tuberculous mycobacterial (NTM) strains, suggesting its selective activity against M. tb . The noteworthy activity of 21a against DS strains and its low cytotoxicity highlight its potential to treat DS M. tb .","journal":"Chemical Biology & Drug Design","year":2021,"id":188932,"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":15,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9435,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2021-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":352337,"name":"Shichun Lun","orcid":null,"position":1,"is_corresponding":false},{"id":364244,"name":"Alan D. Payne","orcid":"0000-0003-4530-6348","position":2,"is_corresponding":false},{"id":241544,"name":"William R. Bishai","orcid":"0000-0002-8734-4118","position":3,"is_corresponding":false},{"id":364245,"name":"Hendra Gunosewoyo","orcid":"0000-0003-3897-1948","position":4,"is_corresponding":false},{"id":364243,"name":"Shahinda S. R. Alsayed","orcid":"0000-0003-0277-255X","position":0,"is_corresponding":true}],"reference_count":53,"raw_metadata":null,"created_at":"2026-07-18T23:49:14.547082Z","pmid":"33638304","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":[]}