Design, synthesis and evaluation of novel diaryl pyrrolopyrimidine and pyrrolothiazine derivatives as inhibitors of tumor necrosis factor stimulated gene-14 (TSG-14) production.
A novel series of pyrrolothiazines 2-4 and pyrrolopyrimidines 5-7 have been synthesized. The structures of these compounds were established by spectroscopic and element microanalytical data. The newly synthesized compounds were evaluated as inhibitors of TSG-14. The most effective results were obtained by the S-sec-butyl derivatives 6e (80%) and the N-ethyl derivatives 4e (70%).
Department of Chemistry, Faculty of Science, Monufyia University, Shebin El-Kom, Egypt. Electronic address: hilmykhaled@yahoo.com.
Khalid M H
KM
Hilmy
Pharmaceutical Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
Dalia H
DH
Soliman
Department of Biochemistry, Faculty of Medicine (Girls), Al-Azhar University, Cairo, Egypt.
Esmat B A
EB
Shahin
Department of Chemistry, Faculty of Science, Monufyia University, Shebin El-Kom, Egypt.
Hala S
HS
El-Deeb
Department of Chemistry, Faculty of Science, Monufyia University, Shebin El-Kom, Egypt.
Salah M
SM
El-Kousy
D000818:Animals; D002097:C-Reactive Protein / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D011743:Pyrimidines / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D011758:Pyrroles / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D000683:Serum Amyloid P-Component / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000099153:Pentraxins
D002097:C-Reactive Protein; D008070:Lipopolysaccharides; D011743:Pyrimidines; D011758:Pyrroles; D000683:Serum Amyloid P-Component; D013843:Thiazines; D000099153:Pentraxins; C476283:1H-pyrrolo(1,2-c)(1,3)thiazine; C527741:pyrrolopyrimidine
Gene-14 (TSG-14); Pyrrolopyrimidines; Pyrrolothiazines; TNF-α