545389-98-8Relevant academic research and scientific papers
Synthesis of azabicyclo[3.1.0]amine analogues of anacardic acid as potent antibacterial agents
Vempati, Ravi Kumar,Reddy,Alapati, Srinivasa Rao,Dubey
, p. 986 - 994 (2013/06/26)
Azabicyclo[3.1.0]amine analogues of anacardic acid (16a, 16b, 18a, 18b, 19 and 19b) were synthesized from anacardic acid and tested for their antibacterial activity against Gram positive and Gram negative bacteria. Most of the compounds are having potency at par with ampicillin and inferior with other standard drugs.
1,4-dihydropyridine and pyridine compounds as calcium channel blockers
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Page/Page column 37, (2010/02/05)
The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related
Design, synthesis and biological evaluation of benzimidazole/benzothiazole and benzoxazole derivatives as cyclooxygenase inhibitors
Paramashivappa,Phani Kumar,Subba Rao,Srinivasa Rao
, p. 657 - 660 (2007/10/03)
We have synthesised a series of 2-[[2-alkoxy-6-pentadecylphenyl)methyl]thio]-1H-benzimidazoles/benzothiazoles and benzoxazoles from anacardic acid and investigated their ability to inhibit human cyclooxygenase-2 enzyme (COX-2). The active compounds were s
SUBSTITUTED DIHYDROPYRIMIDINES, DIHYDROPYRIMIDONES AND DIHYDROPYRIMIDINETHIONES AS CALCIUM CHANNEL BLOCKERS
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Page 27, (2008/06/13)
The present invention is directed in part towards methods of modulating the function of calcium channels with pyrimidine-based compounds. In addition, the invention describes methods of preventing and treating calcium channel-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyrimidine-based compounds and pharmaceutical compositions comprising these compounds.
Synthesis and evaluation of a new class of nifedipine analogs with T-type calcium channel blocking activity
Phani Kumar,Stotz, Stephanie C.,Paramashivappa,Beedle, Aaron M.,Zamponi, Gerald W.,Srinivasa Rao
, p. 649 - 658 (2007/10/03)
We have synthesized a novel series of 18 dialkyl 1,4-dihydro-4-(2′alkoxy-6′-pentadecylphenyl)-2,6-dimethyl-3,5 pyddine dicarboxylates from anacardic acid, a natural compound found in cashew nut shells, and investigated their blocking action on L- and T-type calcium channels transiently expressed in tSA-201 cells. The IC50 values for L-type calcium channel block obtained with the series ranged from 1 to ~40 μM, with higher affinities being favored by increasing the size of the alkoxy group on the 4-phenyl ring and ester substituent in the 3,5 positions. A detailed analysis of the strongest L-type channel blocker of the series (PPK-12) revealed that block was poorly reversible and mediated an apparent speeding of the time course of inactivation. Moreover, in the presence of PPK-12, the midpoint of the steady state inactivation curve was shifted by 20 mV toward more hyperpolarized potentials, resulting in an increase in blocking efficacy at more depolarized holding potentials. Surprisingly, PPK-12 blocked T- and L-type calcium channels with similar affinities. One of the weakest L-type channel inhibitors (PPK-5) exhibited a T-type channel affinity that was similar to that seen with PPK-12, resulting in a 40-fold selectivity of PPK-5 for T- over L-type channels. Thus, dialkyl 1,4-dihydro-4-(2′alkoxy-6′-pentadecylphenyl)-2,6-dimethyl-3,5 pyridine dicarboxylates may serve as excellent candidates for the development of T-type calcium-channel specific blockers.
