Authors Alfayomy, AM; Abdel-Aziz, SA; Marzouk, AA; Shaykoon, MSA; Narumi, A; Konno, H; Abou-Seri, SM; Ragab, FAF in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about in [Alfayomy, Abdallah M.; Abdel-Aziz, Salah A.; Marzouk, Adel A.; Shaykoon, Montaser Sh. A.] Al Azhar Univ, Dept Pharmaceut Chem, Fac Pharm, Assiut 71524, Egypt; [Abdel-Aziz, Salah A.] Deraya Univ, Dept Pharmaceut Chem, Fac Pharm, Al Minya, Egypt; [Narumi, Atsushi] Yamagata Univ, Grad Sch Organ Mat Sci, Jonan 4-3-16, Yonezawa, Yamagata 9928510, Japan; [Konno, Hiroyuki] Yamagata Univ, Grad Sch Sci & Engn, Yonezawa, Yamagata 9928510, Japan; [Abou-Seri, Sahar M.; Ragab, Fatma A. F.] Cairo Univ, Dept Pharmaceut Chem, Fac Pharm, Kasr El Aini St,POB 11562, Cairo 11562, Egypt in 2021, Cited 49. Recommanded Product: 123-11-5. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
Two new series of 1,3,4-oxadiazole and coumarin derivatives based on pyrimidine-5-carbonitrile scaffold have been synthesized and evaluated for their COX-1/COX-2 inhibitory activity. Compounds 10c, 10e, 10h-j, 14e-f, 14i and 16 were found to be the most potent and selective inhibitors of COX-2 (IC50 0.041-0.081 mu M, SI 139.74-321.95). Eight compounds were further investigated for their in vivo anti-inflammatory activity. The most active derivatives 10c, 10j and 14e displayed superior in vivo anti-inflammatory activity (% edema inhibition 39.3-48.3, 1 h; 58.4-60.5, 2 h; 70.8-83.2, 3 h; 78.9-89.5, 4 h) to the reference drug celecoxib (% edema inhibition 38.0, 1 h; 48.8, 2 h; 58.4, 3 h; 65.4, 4 h). These derivatives were also tested for their ulcerogenic liability, compound 10j showed better safety profile with reference to celecoxib while 10c and 14e exhibited mild lesions. Molecular docking studies of 10c, 10j, and 14e in the COX-2 active site revealed similar orientation and binding interactions as selective COX-2 inhibitors with a higher liability to access the selectivity side pocket.
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles