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Screening and Synthesis of Tetrazole Derivatives that Inhibit the Growth of Cryptococcus Species

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The compounds 8-fluoro-7-methyl-5-(pyridin-2-yl)tetrazolo[1,5-c]pyrimidine and 5-(pyridin-2-yl)-8,9-dihydro-7H-cyclopenta[e]tetrazolo[1,5-c]pyrimidine belong to a novel class of antifungals. Both compounds with tetrazole backbone exhibit inhibitory activity that is equivalent or superior to those of conventional drugs on a weight-per-volume basis, with IC50 equalling 0.05 μM (0.012 μg mL−1) against each Cryptococcus species. Thus, tetrazole-backbone-containing compounds may be novel antifungal drugs with distinct mechanisms against cryptococcosis.antifungal agentsCandidaCryptococcushigh-throughput screeningtetrazoles


Cryptococcosis has become a major health problem worldwide and caused morbidity and mortality in immunocompromised patients, especially those infected with human immunodeficiency virus (HIV). Despite the global distribution of cryptococcosis, the number and types of the available antifungals are limited, and the treatment outcomes in HIV patients are generally poor. In this study, we screened a compound library and identified one tetrazole derivative as an efficient inhibitor of Cryptococcus neoformans and Cryptococcus gattii. We further designed and synthesized a series of tetrazole derivatives and determined their structure-activity relationship, demonstrating that tetrazole backbone-containing compounds could be developed as novel antifungal drugs with distinct mechanisms against Cryptococcus spp. Our findings provide a starting point for novel target identification and structural optimization to develop a distinct class of therapeutics for patients with cryptococcosis.

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