tetrazole

Tetrazole (1H-TETRAZOLE) is the bioisoster of carboxylic acid, possess considerable antibacterial property.

Mephetyl tetrazole is a potassium channel (Kv1.5) blocker with an IC50 value of 330 nM. It is applicable in cancer research.

Valsartan (CGP 48933) is a tetrazole derivative and angiotensin II type 1 receptor blocker that is used to treat hypertension.

Bentemazole has been investigated as an antifungal compound.

MK-8245 trifluoroacetate is a phenoxy piperidine isoxazole derivative functioning as a potent, liver-targeting stearoyl-CoA desaturase (SCD) inhibitor, demonstrating significant anti-diabetic and anti-dyslipidemic effects. It showcases high specificity and efficacy against SCD1 across various species, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1. MK-8245's mechanism includes a tetrazole acetic acid moiety that facilitates liver-targeting through OATPs recognition. Its inhibition potency in rat hepatocyte assays (IC50 of 68 nM) surpasses that in HepG2 cell assays devoid of active OATPs (IC50 of ~1 μM), highlighting its liver specificity. Moreover, MK-8245 exhibits over 100,000-fold selectivity against Δ-5 and Δ-6 desaturases in comparative assays. In vivo studies reveal MK-8245's preferential liver distribution in mice, rats, dogs, and rhesus monkeys, underscoring its potential for minimizing adverse effects in non-target tissues. Additionally, its administration in eDIO mice before glucose challenges significantly improves glucose clearance, indicating its therapeutic promise in diabetes management.

CB 168 is a potent selective aminoacylaminoaryl tetrazole inhibitor targeting isoleucine tRNA synthetase (IleRS).

Antifungal agent 52 (compound 6c), a tetrazole derivative, inhibits ergosterol synthesis and significantly exhibits antifungal activity against Candida albicans by affecting the permeabilization of the C. albicans sessile cell membrane [1].

Tubulin Inhibitor 38 (Compound 14), a tetrazole-based agent, demonstrates significant antiproliferative effects by inducing mitotic arrest and blocking the cell cycle at the G2 M phase, ultimately triggering apoptosis. Administered at 100 nM for 24 hours, it shows considerable cytotoxicity and selectivity within HeLa, MCF7, and U87 MG cell lines [1].

rac-Valsartan-d9 is a deuterated compound of rac-Valsartan. rac-Valsartan has a CAS number of 137862-53-4. Valsartan is a tetrazole derivative and angiotensin II type 1 receptor blocker that is used to treat hypertension.