Waechter, Gerald A. published the artcileTetrahydronaphthalenes: Influence of Heterocyclic Substituents on Inhibition of Steroidogenic Enzymes P450 arom and P450 17, Category: pyridazine, the publication is Journal of Medicinal Chemistry (1996), 39(4), 834-41, database is CAplus and MEDLINE.
In search of new leads for selective inhibition of estrogen and androgen biosynthesis, resp., heterocyclic substituted 2-(arylmethylene)-1-tetralones (1-4, 9-17), 2-(arylhydroxymethyl)-1-tetralones (5-8), exo-1a,2,3,7b-tetrahydro-1H-cyclopropa[a]naphthalenes (18-24), and 3-alkyl substituted 4,5-dihydronaphtho[1,2-c]pyrazoles (25-27) were synthesized and tested for inhibitory activity toward four steroidogenic enzymes, P 450 arom, P 450 17, P 450 18, and P 450 scc, as well as another P 450 enzyme, thromboxane A2 (TXA2) synthase. The test compounds inhibited human placental P 450 arom, showing a wide range of inhibitory potencies. (Z)-4-Imidazolyl compound 17 was the most potent inhibitor, with a relative potency (rp) of 110 [rp of aminoglutethimide (AG) = 1, rp of fadrozole = 359]. A competitive type of inhibition was shown by the (E)-4-imidazolyl compound 16 (rp = 71). On the other hand some of these compounds inhibited rat testicular P 450 17. Maximum activity was shown by the 3-pyridyl compound 20 (rp = 10, rp of ketoconazole = 1). Compound 20 was the only compound which exhibited a marked inhibition of TXA2 synthase (IC50 = 14.5 μM; IC50 of dazoxiben = 1.1 μM). Regarding selectivity toward the steroidogenic enzymes, compound 16 was relatively selective toward P 450 arom, whereas compound 20 was relatively selective toward P 450 17 (P 450 arom: Km testosterone = 42 nM, Ki 16 = 33 nM, Ki 20 = 3 μM; P 450 17: Km progesterone = 7 μM, Ki 16 = 9 μM, Ki 20 = 80 nM). Compounds 17 and 24 were not selective since they showed strong inhibition of P 450 arom (Ki 17 = 26 nM, Ki 24 = 0.12 μM) and P 450 17 (Ki 17 = 0.7 μM, Ki 24 = 0.11 μM).
Journal of Medicinal Chemistry published new progress about 50901-42-3. 50901-42-3 belongs to pyridazine, auxiliary class Pyridazine,Aldehyde, name is Pyridazine-4-carbaldehyde, and the molecular formula is C11H12O4, Category: pyridazine.
Referemce:
https://en.wikipedia.org/wiki/Pyridazine,
Pyridazine | C4H4N2 – PubChem