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  • The structures of these compounds were confirmed from

    2024-06-14

    The structures of these compounds were confirmed from their spectral and micro analytical data. Based on [M + H] 367, molecular formula of was established as CHON. The IR spectrum of showed Cy3.5 NHS ester (non-sulfonated) due to CO stretching at 1700 Cm & OH stretching at 3188 Cm indicating that compound contains one carbonyl group, a free hydroxyl group and ether stretching at 1089 Cm. Therefore the product was inferred to contain a indanone containing amino alcohol in final structure. H NMR spectrum (300 MHz) of recorded in CDCl exhibited signals arising due to typical secondary alcohol attached CH. The spectrum contained multiplet at 4.22–4.13 integrating for one proton, CH present in between CH and oxygen shows doublet at 4.09 for 2H, CH present in between CH and nitrogen shows doublet at 3.09 for 2H. : Angiotensin converting enzyme (ACE) inhibition of new triazole derivatives and -amino alcohols were examined in vitro using recently developed high-throughput colorimetric screening method , . Most of these anti-hypertensive peptides have been characterized by the rabbit lung ACE inhibitor assay, based on the hydrolysis of the synthetic peptide hippuryl-histidyl-leucine (HHL). Angiotensin converting enzyme (ACE) hydrolyses HHL to hippuric acid (HA) and histidyl-leucine (HL). HA released is directly proportional to the ACE activity. In this screening method, the released hippuric acid from the substrate hippuryl-histidyl-leucine (HHL) was transformed into yellow color by mixing with pyridine and benzene sulfonyl chloride. The resulted yellow color was determined colorimetrically at absorbance 410 nm. The average ACE inhibitor activity was measured in triplicate for new analogues and the standard drugs Lisinopril (). The experiment carried out at 1.0 µM concentration of test compounds revealed 20–58% of ACE inhibition activity. , and have better ACE inhibitor activity (>70%) at 2.0 µM concentration, when compared to other substituted analogues. Relative to the reference drug Lisinopril these three analogues , and were comparably active with 70%, 79% and 78% ACE inhibition, respectively (). We also noted that, , and resulted in lower ACE inhibitor activity compared to all the other analogues. The average ACE inhibitor activity was measured in triplicate for new analogues and the standard drugs Lisinopril (). The experiment carried out at 2.0 µM concentration of test compounds revealed ACE inhibition activity. and have better ACE inhibitor activity (100%) at 2.0 µM concentration, when compared to other substituted analogues. Relative to the reference (standard) drug Lisinopril, these two analogues and were comparably active with 100% ACE inhibition (). We also noted that, and resulted in lower ACE inhibitor activity compared to all the other analogues. In summary, we have synthesized novel triazole derivatives(±)-2-(hydroxymethyl)-7,8-dihydro-1-indeno[5,4-]furan-6(2)-one () were effectively, the reaction between racemic azide and terminal acetylenes under click chemistry reaction conditions. -Amino alcohol derivatives of 1-indanone were synthesized from 5-hydroxy indanone, Negative supercoiling was reacted with epi chlorohydrin and followed by oxirane ring was opened with various piperazine derivatives and evaluated as angiotensin converting enzyme (ACE) inhibitors. Among the newly synthesized compounds , , , and exhibited good ACE inhibitor activity (>70%) at 2.0 µM concentration comparable to clinical drug Lisinopril. This study provides valuable information for further designing and developing newer and more potent anti-hypertensive agents. Acknowledgments The authors (VHR & YKS) gratefully acknowledge the Council of Scientific and Industrial Research (CSIR), New Delhi, India for the award of fellowship and DST-SERB/EEQ-095/2017.
    Introduction The 1986 introduction of the Quota Management System (QMS) to New Zealand's fishery was followed by a steep decline in the number of fishers operating in the inshore fishery. Quota ownership became increasingly concentrated. Many fishers found they had insufficient quota to carry on a viable operation, and the cost of acquiring additional quota was beyond their financial capability [1]. Consequently, many chose to exit the industry.