Abstract
Malaria is an old scourge of mankind and mention of the disease is found in ancient writings in India, Egypt and China [1]. The clinical symptoms of this disease were described by Hippocrates 400 years before the Christian era [1]. Human population affected by malaria is alarmingly large in tropical regions although in the past the disease was also prevalent in temperate regions [1]. The respite from this disease after World War II, due to the success in the control of the vector mosquitoes and development of new antimalarials, was, however, short lived and malaria has staged a come back in recent years. Only two decades back WHO had stated The clinicians have at their disposal a complete series of effective drugs for the treatment of all stages of this disease’ [2] but in 1971 the same organization considered malaria eradication as a difficult problem both technically and politically [3] and commented ‘Thus there is no avoiding the conclusion that malaria will be with us for quite sometime. In order to cope more efficiently with this world-wide problem, much more research is required’ [4]. It would, therefore, be pertinent to analyse the main causes of this set-back. The principal reason is undoubtedly the appearance of drug-resistance in malarial parasites. Resistance to all the currently available drugs is a reality; even the age-old remedy, quinine, has the same limitations as the synthetic drugs.
To whom all correspondence should be made. CDRI communication No. 3364
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References
R. H. Black, C. J. Canfield, D. F. Clyde, W. Peters and W. H. Wernsdorfer: Chemotherapy of Malaria. World Health Organization Monograph Series No. 27, World Health Organization, Geneva 1981.
Wld Hlth Org. techn. Rep. Ser. 296 (1961).
Wld Hlth Org. techn. Rep. Ser. 467 (1971).
T. Lepes: Bull. Wld Hlth Org. 50, 151 (1974).
K. H. Rieckmann, J. V. McNamara, H. Frischer, T. A. Stockert, P. E. Carson and R. D. Powell: Am. J. trop. Med. Hyg. 17, 661 (1968).
K. H. Rieckmann: J. Am. med. Ass. 277, 573 (1971).
P. C. C. Garnham, R. S. Bray, L. J. Bruce-chwatt, C. C. Draper, R. K. Kendrick, P. G. Sergiev, N. A. Tiburskaja, P. G. Shute and M. Maryon: Bull. Wld Hlth Org. 52, 21 (1975).
A. J. Lysenko, A. E. Beljaev and V. M. Rybalka: Bull. Wld Hlth Org. 55, 541 (1977).
W. H. Wernsdorfer: Bull. Wld Hlth Org. 55, 133 (1977).
E. Fink: Bull. Wld Hlth Org. 50, 213 (1974).
R. C. Elderfield: Chem. Eng. News 24, 2598 (1946).
R. F. Loeb: J. Am. med. Ass. 132, 321 (1946).
A. S. Alving, J. Arnold and D. H. Robinson: J. Am. med. Ass. 149, 1558 (1952).
W. C. Cooper, A. V. Myatt, T. Hernandez, G. M. Jeffery and G. R. Coatney: Am. J. trop. Med. Hyg. 2, 949 (1953).
J. H. Edgcomb, J. Arnold, E. H. Yount, Jr., A. S. Alving and L. Eichelberger: J. natn. malar. Soc. 9, 285 (1950).
A. S. Alving, C. F. Johnson, A. R. Tarlov, G. J. Brewer, R. W. Kellermeyer and P. E. Carson: Bull. Wld Hlth Org. 22, 621 (1960).
R. H. Black: Aust. Ann. Med. 1, 259 (1958).
J. Arnold, A. S. Alving, C. B. Clayman and R. S. Hochwald: Trans. R. Soc. trop. Med. Hyg. 55, 345 (1961).
D. S. Rane and K. E. Kinnamon: Am. J. trop. Med. Hyg. 28, 937 (1979).
T. S. Osdene, P. B. Russell and L. Rane: J. med. Chem. 10, 431 (1967).
K. G. Gregory and W. Peters: Ann. trop. Med. Parasit. 65, 15 (1970).
J. Hill: Ann. trop. Med. Parasit. 69, 421 (1975).
D. C. Warhurst and R. O. Folwell: Ann. trop. Med. Parasit. 62, 349 (1968).
H. Most and W. A. Montouri: Am. J. trop. Med. Hyg. 24, 179 (1975).
L. H. Schmidt, R. N. Rossan and K. F. Fisher: Am. J. trop. Med. Hyg. 12, 494 (1963).
O. Y. Magidson and I. T. Strukov: Arch. Pharm. 271, 569 (1933).
O. Y. Magidson, O. S. Madaeva and M. V. Rubzov: Arch. Pharm. 273, 320 (1935).
O. Y. Magidson, N. M. Delektorskaya and I. M. Lipovich: Arch. Pharm. 272, 74 (1934).
A. W. Baldwin and R. Robinson: J. chem. Soc., p. 1264 (1934).
W. Meisel and R. Robinson: J. chem. Soc., p. 1267 (1934).
R. Robinson and M. L.Tomlinson: J. chem. Soc., p. 1524(1934).
W. L. Glen and R. Robinson: J. chem. Soc., p. 557 (1943).
J. Gum and R. Robinson: J. chem. Soc., p. 561 (1943).
O. Y. Magidson and M. D. Bobyshev: J. gen. Chem. USSR 8, 889 (1938).
W. Huber, R. K. Bair, W. Bochme, S. C. Laskowski, M. Jackman and R. O. Clinton: J. Am. chem. Soc. 61, 1849 (1945).
R. C. Elderfield, W. J. Gensler, J. D. Head, H. A. Hageman, C. B. Kremer, J. B. Wright, A. D. Holley, B. Williamson, J. Galbreth, L. Weiderhold III, R. Froherdt, S. Kupchan, T. A. Williamson and O. Birstein: J. Am. chem. Soc. 68, 1524 (1946).
H. Gilmanand L. A. Woods: J. Am. chem. Soc. 67, 1843 (1945).
G. W. Moersch, R. W. Gouley, H. T. Patricson and H. S. Mosher: J. Am. chem. Soc. 69, 2619 (1947).
R. C. Elderfield, C. B. Kremer, S. M. Kupchen, O. Bristein and G. Cortes: J. Am. chem. Soc. 69, 1258 (1947).
N. L. Drake, R. A. Hayes, J. A. Garman, R. B. Johnson, G. W. Kelley, S. Melamed and R. M. Peck: J. Am. chem. Soc. 71, 455 (1949).
N. L. Drake and J. A. Garman: J. Am. chem. Soc. 71, 2425 (1949).
R. C. Elderfield, E. F. Claftin, H. E. Mertel, O. L. McCurdy, R. T. Mitch, C. D. Ver Nooy, B. H. Wark and I. M. Wempen: J. Am. chem. Soc. 77, 4819 (1955).
C. R. Hauser, M. S. Bloom, D. S. Breslow, J. T. Adams, S. T. Amore and M. J. Weiss: J. Am. chem. Soc. 68, 1544 (1946).
T. R. Norton, R. A. Seibert, A. A. Benson and F. W. Bergstrom: J. Am. chem. Soc. 68, 1572 (1946).
W. M. Lauer, R. T. Arnold, B. Tiffenny and C. O. Wilson: J. Am. chem. Soc. 68, 1548 (1946).
W. M. Lauer, C. Rondestvedt, R. T. Arnold, N. L. Drake, J. V. Hook and J. Tinker: J. Am. chem. Soc. 68, 1546 (1946).
K. Matejka and R. Robinson: J. Am. chem. Soc., p. 1322 (1934).
M. Carmack, L. W. Kissinger and I. Von: J. Am. chem. Soc. 68, 1551 (1946).
W. C. Cooper, A. V. Myatt, T. Hernandez, G. M. Jeffery and G. R. Coatney: Am. J. trop. Med. Hyg. 2, 949 (1953).
K. N. Campbell, R. A. LaForge and B. K. Campbell: J. org. Chem. 14, 346 (1949).
S. M. Talati, M. R. Latham, E. G. Moore, G. W. Hargreaves and C. D. Blanton, Jr.: J. pharm. Sci. 59, 491 (1970).
L. H. Schmidt and C. S. Genther: J. Pharmac. exp. Ther. 107, 61 (1953).
R. V. Shetty and C. De Witt Blanton, Jr.: J. med. Chem. 21, 995 (1978).
R. V. Shetty, W. P. Wetter and C. De Witt Blanton, Jr.: J. med. Chem. 20, 1349 (1977).
P. E. Thompson and L. M. Werbel: Antimalarial agents — Chemistry and Pharmacology, p. 100–118. Ed. G.D. Stevens, Academic Press, New York 1972 ).
F. I. Carroll, B. D. Berrang and C. P. Linn: J. med. Chem. 22, 1363 (1979).
F. I. Carroll, B. D. Berrang, C. P. Linn and C. E. Twine, Jr.: J. med. Chem. 22, 694 (1979).
W. Peters, E. E. Davies and B. L. Robinson: Ann. trop. Med. Parasit. 69, 311 (1975).
L. H. Schmidt: Annu. Rev. Microbiol. 23, 427 (1969).
M. P. LaMontagne, A. Markovac and J. R. Menke: J. med. Chem. 20, 1122 (1977).
K. E. Kinnamon and D. S. Rane: Am. J. trop. Med. Hyg., in preparation (vide ref. 56).
W. P. Wetter and C. De Witt Blanton, Jr.: J. med. Chem. 17, 620 (1974).
W. Peters: Exp. Parasit. 17, 80 (1965).
K. Tanabe, E. H. Chen, B. L. Verma, A. J. Saggiomo and E. A. Nodiff: J. med. Chem. 27, 133 (1978).
E. H. Chen, A. J. Saggiomo, K. Tanabe, B. L. Verma and E. A. Nodiff: J. med. Chem. 20, 1107 (1977).
E. A. Nodiff, K. Tanabe, E. H. Chen and A. J. Saggiomo: J. med. Chem. 25, 1097 (1982).
M. P. LaMontagne, A. Markovac and M. S. Khan: J. med. Chem. 25, 965 (1982).
M. P. LaMontagne, P. Blumbergs and R. E. Strube: J. med. Chem. 25, 1094 (1982).
L. H. Schmidt, R. N. Rossan, R. Fradkin and J. Woods: Bull. Wld Hlth Org. 54, 783 (1966).
F. I. Carroll, J. T. Blackwell, A. Philip and C. E. Twine: J. med. Chem. 19, 1111 (1976).
S. Archer, P. O. Gyimah and S. Silbering: J. med. Chem. 23, 517 (1980).
J. P. Scovill, D. L. Klayman, T. S. Woods and T. R. Sweeney: J. med. Chem. 22, 1164 (1979).
F. C. Lefler, H. S. Lilja and D. J. Holbrook, Jr.: Biochem. Pharmac. 22, 715 (1973).
I. W. Sherman and L. Tanigoshi: Proc. helminth. Soc., Wash., 39, 250 (1972).
F. C. Lefler: Diss. Abstr. Int. (B). 33, 1383 (1972).
R. Roskoski, Jr., and S. R. Jaskanas: Biochem. Pharmac. 21, 391 (1972).
K. A. Conklin and S. C. Chou: Science, N. Y. 170, 1213 (1970).
J. R. Burdickand D. P. Durand: Antimicrob. Ag. Chemother. 6, 460 (1974).
J. G. Olenick and F. E. Hahan: Antimicrob. Ag. Chemother. 1, 259 (1972).
B. Wittels: Biochem. Pharmac. 20, 2099 (1971).
H. Y. Pan, S. C. Chou and K. A. Conklin: Pharmacology 12, 48 (1974).
K. A. Conklin, P. Heu and S. C. Chou: Molec. Pharmac. 9, 304 (1973).
G. Carter and K. Van Dyke: Proc. helminth. Soc., Wash. 39, 244 (1972).
C. H. Lantz and K. Van Dyke: Exp. Parasit. 31, 255 (1972).
D. J. Holbrook, L. P. Wichard, C. R. Morris and L. A. White: Prog, molec. Subcell. Biol. 2, 113 (1971).
K. A. Conklin and S. C. Chou: J. Pharmac. exp. Ther. 180, 158 (1972).
R. C. Field, B. R. Gibson, D. J. Holbrook, Jr., and B. M. Maccall: Br. J. Pharmac. 62, 159 (1978).
L. P. Wichard, M. E. Washington and D.J. Holbrook, Jr.: Biochim. biophys. Acta 287, 52 (1972).
K. A. Conklin, S. C. Chou and P. Heu: Biochem. Pharmac. 20, 1877 (1971).
M. Brunori, E. Fioretti and G. Ritilio: Molec. cell. Biol. 19, 43 (1978).
S.N. Kelman, S. G. Sullivan and A. Stern: Biochem. Pharmac. 30, 81 (1981).
P. J. Sides and B. Wittes: Biochem. Pharmac. 24, 1246 (1975).
T. K. Li and L. J. Magnes: Biochem. Pharmac. 27, 17 (1972).
L. H. Schmidt: A Survey of Antimalarial drugs, p. 106–129. Ed. J. W. Edwards: Ann Arbor, Mich., 1946.
T. J. Kennedy: Fed. Proc. 5, 185 (1946).
C. G. Zubrod, T. J. Kennedy and J. A. Shannon: J. clin. Invest. 27, 114 (1948).
A. S. Alving, B. Craige, Jr., R. Jones, Jr., C. M. Whorton, T. N. Pullman and L. Eichelberger: J. clin. Invest. 27, 25 (1948).
R. W. Berliner, D. P. Earle, Jr., J. V. Taggart, W. J. Welch, C. G. Zubrod, P. Knowlton, J. A. Atchley and J. A. Shannon: J. clin. Invest. 27, 108 (1948).
F. Y. Wiselogle: A Survey of Antimalarial drugs, 1941–1945, 2 vols. Ed. J. W. Edwards: Ann Arbor, Mich., 1946.
K. A. Flecher, D. A. P. Evans, H. M. Gilles, J. Greaves, D. Bunnag and T. Harinasuta: Bull. Wld Hlth Org. 59, 407 (1981).
B. Bhat: Ph. D. Thesis, Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow 1983.
D. J. Holbrook, C. C. Collins and A. M. Clark: J. pharm. Sci. 68, 1239 (1981).
C. C. Smith: J. Pharm, exp. Ther. 116, 67 (1956).
B. Brodie and S. Underfriend: Proc. Soc. exp. Biol. Med. 74, 845 (1950).
J. D. Bety, D. A. P. Evans and P. A. Robinson: Biomed. mass spectrom. 2, 304 (1975).
A. Strother, I. M. Fräser, R. K. Allahyari and B. C. Tilton: Bull. Wld Hlth Org. 59, 413 (1981).
C. D. Hufford, M. A. Clark, I. N. Quinones, J. K. Baker and D. J. McChesney: J. pharm. Sci. 72, 92 (1983).
J. Greenberg, D. J. Taylor and E. S. Josephson: J. infect. Dis. 88, 163 (1951).
W. E. Gutteridge and G. H. Coombs: Biochemistry of Parasitic Protozoa. Macmillan, London 1977.
R. S. Krooth, K. D. Wuu and R. Ma: Science, N. Y. 164, 1073 (1969).
W. E. Gutteridge, D. Dave and W. H. G. Richards: Biochim. biophys. Acta 582, 390 (1979).
C. H. Lantz and K. Vandyke: Fed. Proc. 29, 808 (1970).
C. R. Morris, L. V. Andrew, L. P. Wichard and D. J. Hoolbrook: Molec. Pharmac. 6, 240 (1970).
M. E. Washington, L. A. White and D. J. Holbrook, Jr.: Biochem. Pharmac. 22, 477 (1973).
C. B. Clayman, J. Arnold, R. S. Hockwald, E. J. Yount, Jr., J. H. Edgcomb and A. S. Alving: J. Am. med. Ass. 149, 1563 (1952).
C. G. Zubrod: Fed. Proc. 5, 217 (1946).
F. Sioli: Arch. Schiffsu. Tropenhyg. 30, 319 (1926).
G. J. Brewer, A. R. Tarlov, R. W. Kellermeyer and A. S. Alving: J. Lab. clin. Med. 59, 905 (1962).
R. S. Grewal: Bull.WldHlth Org. 59, 397 (1981).
P. E. Carson, R. Hohl, M. V. Nora, G. W. Parkhurst, T. Ahmad, S. Scanlan and H. Frischer: Bull. Wld Hlth Org. 59, 427 (1981).
F. L. Ginn, P. Hochstein and B. F.Trump: Science, N. Y. 164, 843 (1969).
A. R. Tarlov, G. J. Brewer, P. E. Carson and A. S. Alving: Arch. int. Med. 109, 209 (1962).
E. Bentler and M. Mitchell: Blood 32, 816 (1969).
A. P. Richardson, H. A. Walker and B. S. Miller: Proc. Soc. exp. Biol. Med. 65, 258 (1947).
G. K. Moe, B. Peralta and M. H. Seevers: J. Pharmac. exp. Ther. 95, 407 (1949).
R. B. Arora and B. R. Madan: Arch. int. Pharmacodyn. Ther. 107, 215 (1956).
E. L. Holland and R. S. McCutcheon: J. pharm. Sci. 51, 791 (1962).
Y. H. Thong, A. Ferrante and B. R. Kelley: Trans. R. Soc. trop. Med. Hyg. 72, 537 (1978).
Y. H. Thong:Trans. R. Soc. trop. Med. Hyg. 73, 474 (1979).
E. R. Seidel, R. L. Mundy and R. S. Teague: Toxic, appl. Pharmac. 45, 258 (1978).
Y. Hayashi: Bull. Fac. Agr., Tottori University 30, 82 (1979).
R. J. Marshall and J. A. O. Ojewoli: Toxic, appl. Pharmac. 46, 759 (1978).
P. E. Carson and H. Frischer: Am. J. Med. 41, 744 (1966).
H. Lehmann and P. A. M. Kynoch: Human haemoglobin variants and their characteristics. Amsterdam, New York, Oxford, North Holland 1976.
L. H. Schmidt: Fed. Proc. 6, 368 (1947).
I. G. Schmidt and L. H. Schmidt: J. Neuropath, exp. Neurol. 7, 368 (1949).
J. C. Sipe, A. V. Nicholas, S. Sidney and F. Cesar: J. Neuropath, exp. Neurol. 32, 446 (1973).
R. J. Dern, E. Beutler and A. S. Alving: J. Lab. clin. Med. 44, 171 (1954).
R. W. Kellermeyer, A. R. Tarlov, S. L. Schrier, P. E. Carson and A. S. Alving: J. Lab. clin. Med. 58, 225 (1961).
A. R. Tarlov, G. J. Brewer, P. E. Carson and A. S. Alving, Arch, intern. Med. 709, 209 (1962).
M. Ziai, G. H. Amirhakami, J. G. Reinhold, M. Tabatabee, M. E. Gettner and J. E. Bowman: Clin. Pediat. 6, 242 (1967).
S. A. Chopra: E. Afr. med. J. 45, 726 (1968).
A. T. Batu, U. H. Pe and T. Than: Trans. R. Soc. trop. Med. Hyg. 64, 785 (1970).
K. P. Abeyaratne and N. L. Halpe: Ceylon Med. J. 27, 134 (1968).
A. Trouet, P. Pirson, R. Steiger, M. Masquelier, R. Baurain and J. Gillet: Bull. Wld Hlth Org. 59, 449 (1981).
G. P. Dutta: Personal communication (Division of Microbiology, Central Drug Research Institute, Lucknow, India).
L. H. Schmidt, S. Alexander, L. Allen and J. Rosco: Antimicrob. Ag. Chemother. 12, 51 (1977).
F. S. Skeleton, P. J. Reitz and K. Folkers: J. med. Chem. 13, 602 (1970).
F. S. Skeleton, R. S. Pardini, J. C. Heidker and K. Folkers: J. Am. chem. Soc. 90, 334 (1968).
L. D. Heaton: Milit. Med. 725, 6 (1963).
W. Peters: Trans. R. Soc. trop. Med. Hyg. 63, 24 (1969).
D. E. Davidson, Jr., A. L. AGer, J. L. Brown, F. E. Chappie, B. E. Whitemire and R. N. Rossan: Bull. Wld Hlth Org. 59, 463 (1981).
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Bhat, B.K., Seth, M., Bhaduri, A.P. (1984). Recent developments in 8-aminoquinoline antimalarials. In: Jucker, E. (eds) Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des recherches pharmaceutiques. Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des recherches pharmaceutiques, vol 28. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7118-1_6
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