Mylari, Banavara L. published the artcilePotent, orally active aldose reductase inhibitors related to zopolrestat: surrogates for benzothiazole side chain, Computed Properties of 4760-35-4, the publication is Journal of Medicinal Chemistry (1992), 35(3), 457-65, database is CAplus and MEDLINE.
A broad structure-activity program was undertaken in search of effective surrogates for the key benzothiazole side chain of the potent aldose reductase inhibitor, zopolrestat. A structure-driven approach was pursued, which spanned exploration of three areas: (1) 5/6 fused heterocycles, such as benzoxazole, benzothiophene, benzofuran, and imidazopyridine; (2) 5-membered heterocycles, including oxadiazole, oxazole, thiazole, and thiadiazole, with pendant aryl groups, and (3) thioanilide as a formal equivalent of benzothiazole. Several benzoxazole- and 1,2,4-oxadiazole-derived analogs were found to be potent inhibitors of aldose reductase from human placenta and were orally active in preventing sorbitol accumulation in rat sciatic nerve, in an acute test of diabetic complications. Phthalazineacetic acid I was the best of the benzoxazole series ([C50 = 3.2 × 10-9M); it suppressed accumulation of sorbitol in rat sciatic nerve by 78% at an oral dose of 10 mg/kg. Oxadiazolyl derivative II with IC50 < 1.0 × 10-8M, caused a 69% reduction in sorbitol accumulation in rat sciatic nerve at an oral dose of 25 mg/kg. The thioanilide side chain features in III proved to be an effective surrogate for benzothiazole. III was highly potent in vitro (IC50 = 5.2 × 10-8M) but did not show oral activity when tested at 100 mg/kg. Addnl. structure-activity relationships encompassing a variety of heterocyclic side chains are discussed.
Journal of Medicinal Chemistry published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C9H9ClN2, Computed Properties of 4760-35-4.
Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem