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Antimalarial activity of 3-hydroxyalkyl-2-methylene-propionic acid derivatives
Several Baylis-Hillman adducts and their derivatives were synthesized and evaluated as targeted potential anti-malarials. The compounds 4, 7 and 9 were found to have highest potency against P. falciparum in vitro. The in vivo test result of compound 4 and 9 against P. berghei demonstrated activity a...
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Published in: | Bioorganic & medicinal chemistry letters 1999-03, Vol.9 (5), p.731-736 |
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container_start_page | 731 |
container_title | Bioorganic & medicinal chemistry letters |
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creator | Kundu, Mrinal K. Sundar, N. Kumar, Srinivas K. Bhat, Sujata V. Biswas, Sukla Valecha, Neena |
description | Several Baylis-Hillman adducts and their derivatives were synthesized and evaluated as targeted potential anti-malarials. The compounds
4, 7 and
9 were found to have highest potency against
P. falciparum in vitro. The
in vivo test result of compound
4 and
9 against
P. berghei demonstrated activity at 80 mg/Kg dose level.
Synthesis and evaluation studies of some new anti-malarials is reported. |
doi_str_mv | 10.1016/S0960-894X(99)00057-8 |
format | article |
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4, 7 and
9 were found to have highest potency against
P. falciparum in vitro. The
in vivo test result of compound
4 and
9 against
P. berghei demonstrated activity at 80 mg/Kg dose level.
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4, 7 and
9 were found to have highest potency against
P. falciparum in vitro. The
in vivo test result of compound
4 and
9 against
P. berghei demonstrated activity at 80 mg/Kg dose level.
Synthesis and evaluation studies of some new anti-malarials is reported.</description><subject>Animals</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antimalarials - chemical synthesis</subject><subject>Antimalarials - chemistry</subject><subject>Antimalarials - pharmacology</subject><subject>Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Chloroquine - pharmacology</subject><subject>Drug Evaluation, Preclinical</subject><subject>Drug Resistance</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Plasmodium berghei - drug effects</subject><subject>Plasmodium falciparum - drug effects</subject><subject>Propionates - chemical synthesis</subject><subject>Propionates - chemistry</subject><subject>Propionates - pharmacology</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><recordid>eNqFkE1PGzEQhq0KVELKTyjKAVVwcDtef6x9qhAqHxKih4LEzXLsWWHq7Kb2Jur--25IVLhxmsvzzjvzEPKZwVcGTH37BUYB1UY8nhpzBgCypvoDmTChBOUC5B6Z_EcOyGEpzwBMgBAfyQGDCpjmekLuzts-LlxyObo0c76P69gPs66Zcfo0hNz9HVz6PSRa0QX2T0PCFukyd8vYtdGPgRhmAXNcuzGJ5RPZb1wqeLSbU_Jw-eP-4pre_ry6uTi_pZ6D7KmuGmHEXDPPOUNlaiVxHlTF68qrmrM6NMjmGr2E4IBJMMKbpnIKGTcGNZ-SL9u94yl_Vlh6u4jFY0quxW5VrDJKS63NCMot6HNXSsbGLvP4bx4sA7sRaV9E2o0la4x9EWk3Bce7gtV8geFNamtuBE52gCvepSa71sfyytWSV-NDU_J9i-FoYx0x2-Ijth5DzOh7G7r4ziX_AGrqkAI</recordid><startdate>19990308</startdate><enddate>19990308</enddate><creator>Kundu, Mrinal K.</creator><creator>Sundar, N.</creator><creator>Kumar, Srinivas K.</creator><creator>Bhat, Sujata V.</creator><creator>Biswas, Sukla</creator><creator>Valecha, Neena</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19990308</creationdate><title>Antimalarial activity of 3-hydroxyalkyl-2-methylene-propionic acid derivatives</title><author>Kundu, Mrinal K. ; Sundar, N. ; Kumar, Srinivas K. ; Bhat, Sujata V. ; Biswas, Sukla ; Valecha, Neena</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c305t-82f494b81c331e69765ebd62372c67317dfe1b8ec50da015094c9f2a6e1399e83</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Animals</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antimalarials - chemical synthesis</topic><topic>Antimalarials - chemistry</topic><topic>Antimalarials - pharmacology</topic><topic>Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>Chloroquine - pharmacology</topic><topic>Drug Evaluation, Preclinical</topic><topic>Drug Resistance</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Plasmodium berghei - drug effects</topic><topic>Plasmodium falciparum - drug effects</topic><topic>Propionates - chemical synthesis</topic><topic>Propionates - chemistry</topic><topic>Propionates - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kundu, Mrinal K.</creatorcontrib><creatorcontrib>Sundar, N.</creatorcontrib><creatorcontrib>Kumar, Srinivas K.</creatorcontrib><creatorcontrib>Bhat, Sujata V.</creatorcontrib><creatorcontrib>Biswas, Sukla</creatorcontrib><creatorcontrib>Valecha, Neena</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kundu, Mrinal K.</au><au>Sundar, N.</au><au>Kumar, Srinivas K.</au><au>Bhat, Sujata V.</au><au>Biswas, Sukla</au><au>Valecha, Neena</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antimalarial activity of 3-hydroxyalkyl-2-methylene-propionic acid derivatives</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>1999-03-08</date><risdate>1999</risdate><volume>9</volume><issue>5</issue><spage>731</spage><epage>736</epage><pages>731-736</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Several Baylis-Hillman adducts and their derivatives were synthesized and evaluated as targeted potential anti-malarials. The compounds
4, 7 and
9 were found to have highest potency against
P. falciparum in vitro. The
in vivo test result of compound
4 and
9 against
P. berghei demonstrated activity at 80 mg/Kg dose level.
Synthesis and evaluation studies of some new anti-malarials is reported.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>10201838</pmid><doi>10.1016/S0960-894X(99)00057-8</doi><tpages>6</tpages></addata></record> |
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language | eng |
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source | ScienceDirect Journals |
subjects | Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Antiparasitic agents Biological and medical sciences Chloroquine - pharmacology Drug Evaluation, Preclinical Drug Resistance Medical sciences Pharmacology. Drug treatments Plasmodium berghei - drug effects Plasmodium falciparum - drug effects Propionates - chemical synthesis Propionates - chemistry Propionates - pharmacology |
title | Antimalarial activity of 3-hydroxyalkyl-2-methylene-propionic acid derivatives |
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