293329-65-4

Upstream product

• 1634-04-4 tert-butyl methyl ether 
• 541-41-3 chloroformic acid ethyl ester 
• 148747-59-5 5-benzyloxycarbonylamino-6-oxo-2-phenyl-1,6-dihydropyrimidin-1-ylmethylcarboxylic acid 
• 251540-53-1 2-tert-Butyl-1,3,4-oxadiazole 
• 42826-42-6 pivalohydrazide 
• 598-98-1 Methyl pivalate 
• 337969-29-6 N-[(1S)-2-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-2-hydroxy-1-(methylethyl)ethyl]-2-{6-oxo-2-phenyl-5-[(phenylmethoxy)carbonylamino]hydropyrimidinyl}acetamide 
• 251540-54-2 {1-[(5-tert-butyl-[1,3,4]oxadiazol-2-yl)-hydroxy-methyl]-2-methyl-propyl}-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

1,3,4-oxadiazole derivatives and process for producing the same

Oxadiazole derivatives represented by formula (I): (wherein R1represents a hydrogen atom or an amino-protective group; R2, R3, and R4each independently represents an alkyl group, a cycloalkyl group, a phenyl gro

Development of orally active nonpeptidic inhibitors of human neutrophil elastase

5-Amino-2-phenylpyrimidin-6-ones, some of their desamino derivatives, and miscellaneous derivatives were synthesized and biologically evaluated on both in vitro activity and oral activity in an acute hemorrhagic assay. These compounds contained an α-keto-1,3,4-oxadiazole moiety to bind covalently to the Ser-195 hydroxy group of human neutrophil elastase (HNE). Among those tested, compounds 11a-c,e,i-l(F), 11d,e,k(H), 21d,e,k(F), and 21d,e(H) showed a good oral profile. RS-Mixture 3(H) was selected for clinical evaluation based on its oral potency, duration of action, enzyme selectivity, safety profile, and ease of synthesis. Structure -activity relationships (SARs) are discussed.