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Chapter 4 Synthesis of highly substituted pyrazolopyrimidine Song Qing Wang et al. 21 have been designed some new 5-methyl-7- substituted–pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives on the basis of the Zaleplon structure for studies on their hypnotic activity. The preliminary pharmacological evaluations indicated that some compounds showed hypnotic activity, among that one compound (Figure-6) was the most potent one. Figure-6 Robert H. Springer et al. 22 has prepared a number of 3,7-disubstituted 6- carbethoxypyrazolo[ 1,5-a]pyrimidines and 3,7-disubstituted 6-ethoxypyrazolo-[1,5- a]pyrimidines (Figure-7) have been and evaluated as adenosine cyclic 3’,5’- phosphate (cAMP) phosphodiesterase (PDE) inhibitors vs. the low K, enzyme isolated from beef heart, rabbit lung, and kidney preparations. The results were found to be between 0.5 to 13 times as potent as theophylline as inhibitors of PDE, depending on the tissue source. A number of these PDE inhibitors exhibited significant physiological effects in different animal systems, suggesting it should be possible to obtain selective PDE inhibition in various tissues. Several of these heterocycles were found superior to adenosine in inhibiting ADP-induced platelet aggregation in vitro. N R 1 N R 1 O R 2 N N R 1 =H, C 2 H 5 ,NO 2 , Br, COOEt R 2 =OH, NH 2 ,OC 2 H 5 ,SH,SC 2 H 5 Figure-7 Robin R. Frey et al. 23 have discovered 7-aminopyrazolo[1,5-a]pyrimidine urea receptor tyrosine kinase inhibitors. Investigation of structure-activity relationships of the pyrazolo[1,5-a]pyrimidine nucleus led to a series of 6-(4-N,N′-diphenyl)ureas that potently inhibited a panel of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) kinases. Several of these compounds are potent inhibitors of kinase insert domain-containing receptor tyrosine kinase (KDR) both enzymatically(
Chapter 4 Synthesis of highly substituted pyrazolopyrimidine In addition, compound (Figure-8) possesses a favorable pharmacokinetic profile and demonstrates efficacy in the estradiol-induced murine uterine edema (UE) model (ED 50 ) 1.4mg/kg). Figure-8 Rui Ding et al. 24 has synthesized compound 5-((2-aminoethylamino)methyl)- 7-(4-bromoanilino)-3-cyanopyrazolo[1,5-a]pyrimidine (ABCPP) via conjugated with N-mercaptoacetylglycine (MAG), N-mercaptoacetylphenylalanine (MAF) and N- mercaptoacetylvaline (MAA), (Figure-9) respectively. These three compounds were labeled successfully with [ 99m TcN] 2+ intermediate in high radiochemical purities. Biodistribution in tumor-bearing mice demonstrated that the three new complexes showed tumor accumulation, high tumor-to muscle (T/M) ratios and fast clearance from blood and muscle. Among them, the 99mTcNMAG-ABCPP showed the most favorable characteristics, with tumor/blood and tumor/muscle ratios reaching 1.51 and 2.97 at 30 min post-injection, 1.84 and 2.49 at 60 min post-injection, suggesting it could be further studied as potential tumor imaging agent for single photon emission computed tomography (SPECT). Figure-9 Osama M. Ahmed et al. 25 has synthesized some new pyrazolo[1,5- a]pyrimidine derivatives, (Figure-10) which showed potent anti-tumor cytotoxic activity in vitro using different human cancer cell linesHepG2 (hepatocellular carcinoma cell line), MCF7 (breastcarcinoma cell line), HCT116 (colon carcinoma cell line), HeLa (cervix carcinoma cell line). Department of Chemistry, <strong>Saurashtra</strong> university, Rajkot-360005 125
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Saurashtra University Re - Accredit
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Statement under O.Ph.D.7 of Saurash
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I am thankful to FIST/DST and SAP/U
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Chapter 4 Synthesis and Characteriz
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Chapter - 1 Palladium Catalyzed Syn
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Chapter 1 Synthesis of functionaliz
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Chapter - 2 Synthesis and Biologica
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Chapter 6 Synthesis of benzodiazepi
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pyrazole derivative were faster and
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Conferences participated 1. “15 t
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