Category: pyrazoles-derivativesIn 2017 ,《Novel pyrazolo[1,5-a]pyridines as orally active EP1 receptor antagonists: Synthesis, structure-activity relationship studies, and biological evaluation》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Umei, Kentaro; Nishigaya, Yosuke; Kondo, Atsushi; Tatani, Kazuya; Tanaka, Nobuyuki; Kohno, Yasushi; Seto, Shigeki. The article conveys some information:
Novel pyrazolo[1,5-a]pyridine derivatives were designed, synthesized and evaluated as orally active EP1 antagonists for the treatment of overactive bladder. Matched mol. pair anal. (MMPA) allowed the design of a new series of pyrazolo[1,5-a]pyridine derivatives Structure-activity relationships (SAR) studies of were performed, leading to identification of the nanomolar-level EP1 antagonist I, which exhibited good pharmacol. effect through intraduodenal (id) administration in a 17-phenyltrinor prostaglandin E2-induced bladder contraction model in rats. The experimental part of the paper was very detailed, including the reaction process of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Category: pyrazoles-derivatives)
Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Category: pyrazoles-derivatives
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics