Advertisement

Abstract

Among the ills that have plagued mankind, few have exacted a higher toll than malaria. The advent of insecticides simplified the logistics of malaria control, and following World War II many nations took up this approach in earnest. The goal of global eradication was formally adopted at the eighth World Health Assembly in 1955.

Keywords

Injection Site Antimalarial Drug American Chemical Society Subcutaneous Dose Intramuscular Dose 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. [1]
    WHO Chronicle 21, 373 (1967).Google Scholar
  2. [2]
    Wld Hlth Org. techn. Rep. Ser. 226 (1961).Google Scholar
  3. [3]
    L. J. Bruce-Chwatt, Trans. R. Soc. trop. Med. Hyg. 59, 105 (1965).Google Scholar
  4. [4]
    E. F. Elslager and P. E. Thompson, Ann. Rev. Pharmac. 2, 193 (1962).Google Scholar
  5. [5]
    P. E. Thompson, B. J. Olszewski, E. F. Elslager and D. F. Worth, Am. J. trop. Med. Hyg. 12, 481 (1963).Google Scholar
  6. [6]
    Resolution, Am. J. trop. Med. Hyg. 13, 361 (1964).Google Scholar
  7. [7]
    Wld Hlth Org. techn. Rep. Ser. 296 (1965).Google Scholar
  8. [8]
    F. Y. Wiselogle, A Survey of Antimalarial Drugs, 1941–1945, 2 vols (J. W. Edwards, Ann Arbor, Mich. 1946).Google Scholar
  9. [9]
    K. C. Blanchard, Ann. Rev. Biochem. 16, 587 (1947).Google Scholar
  10. [10]
    F. Schönhöfer, Chemotherapy (Office Tech. Services Rept. PB-85033, Washington 1948).Google Scholar
  11. [11]
    F. L. Rose, J. chem. Soc. 1951, 2770.Google Scholar
  12. [12]
    A. M. Moore, Encyclopedia of Chemical Technology, 1st ed., 8, 660–680 (The Interscience Encyclopedia, Inc., New York 1952).Google Scholar
  13. [13]
    G. R. Coatney, W. C. Cooper, N. B. Eddy and J. Greenberg, Survey of Antimalarial Agents (Public Health Monograph No. 9, U. S. Government Printing Office, Washington 1953).Google Scholar
  14. [14]
    L. G. Goodwin and I. M. Rollo, Biochemistry and Physiology of Protozoa, 2, 227–251 (Ed. S. H. Hutner and A. Lwoff; Academic Press, New York 1955).Google Scholar
  15. [15]
    G. Covell, G. R. Coatney, J. W. Field and J. Singh, Chemotherapy of Malaria (World Health Organization Monograph Series No. 27, World Health Organization, Geneva 1955).Google Scholar
  16. [16]
    A. F. Crowther, J. Pharm. Pharmac. 10, 337 (1958).Google Scholar
  17. [17]
    P. B. Russell, Medicinal Chemistry, 2nd ed., 814–850 (Ed. A. Burger; Interscience, New York 1960).Google Scholar
  18. [18]
    C. A. Alvarado and L. J. Bruce-Chwatt, Scient. Am. 206, 86 (1962).Google Scholar
  19. [19]
    D. G. Davey and J. Hill, Experimental Chemotherapy, 1, 487–601 (Ed. R. J. Schnitzer and F. Hawking; Academic Press, New York 1963).Google Scholar
  20. [20]
    L. J. Bruce-Chwatt, Brit. med. J. 1, 581 (1964).Google Scholar
  21. [21]
    I. M. Rollo, Biochemistry and Physiology of Protozoa, 3, 525–561 (Ed. S. H. Hutner; Academic Press, New York 1964).Google Scholar
  22. [22]
    I. M. Rollo, The Pharmacological Basis of Therapeutics, 2nd ed., 1087–1117 (Ed. L. S. Goodman and A. Gilman; Macmillan, New York 1965).Google Scholar
  23. [23]
    E. F. Elslager, Annual Reports in Medicinal Chemistry, 1965, 136 (Ed. C. K. Cain; Academic Press, New York 1966).Google Scholar
  24. [24]
    R. D. Powell, Clin. Pharmac. Ther. 7, 48 (1966).Google Scholar
  25. [25]
    J. Hill, Experimental Chemotherapy, 4, 448–462 (Ed. F. Hawking; Academic Press, New York 1966).Google Scholar
  26. [26]
    P. E. Thompson, Ann. Rev. Pharmac. 7, 77 (1967).Google Scholar
  27. [27]
    E. F. Elslager, Annual Reports in Medicinal Chemistry, 1966, 131 (Ed. C. K. Cain; Academic Press, New York 1967).Google Scholar
  28. [28]
    L. J. Bruce-Chwatt, Trans. R. Soc. trop. Med. Hyg. 61, 412 (1967).Google Scholar
  29. [29]
    W. Peters, Trop. Dis. Bull. 64, 1145 (1967).Google Scholar
  30. [30]
    W. Peters, Trans. R. Soc. trop. Med. Hyg. 61, 400 (1967).Google Scholar
  31. [31]
    Wld Hlth Org. techn. Rep. Ser. 375 (1967).Google Scholar
  32. [32]
    L. J. Bruce-Chwatt, Bull. Wld Hlth Org. 27, 287 (1962).Google Scholar
  33. [33]
    The author is grateful to Dr. L. J. Bruce-Chwatt and to the World Health Organization, Geneva, Switzerland, for permission to reproduce Fig. 1.Google Scholar
  34. [34]
    L. E. Gaudette and G. R. Coatney, Am. J. trop. Med. Hyg. 10, 321 (1961).Google Scholar
  35. [35]
    J. G. Baget, South African Patent 847/R61, 27 October 1961.Google Scholar
  36. [36]
    E. F. Elslager and P. E. Thompson, Abstracts of Papers, 9th National Medicinal Chemistry Symposium of the American Chemical Society, Minneapolis, Minn., p. 6A (June 1964).Google Scholar
  37. [37]
    J. Schneider, M. Bouvry and J. Le Quellec, Ann. Soc. belge Med. trop. 45, 435 (1965).Google Scholar
  38. [38]
    E. F. Elslager and D. F. Worth, Nature 206, 630 (1965).Google Scholar
  39. [39]
    For a brief review, see E. F. Elslager, Medicinal Chemistry, 2nd ed., 864 (Ed. A. Burger; Interscience, New York 1960).Google Scholar
  40. [40]
    For a brief review, see F. Hawking, Experimental Chemotherapy, 1, 170 (Ed. R. J. Schnitzer and F. Hawking; Academic Press, New York 1963).Google Scholar
  41. [41]
    P. E. Thompson, B. Olszewski and J. A. Waitz, Am. J. trop. Med. Hyg. 14, 343 (1965).Google Scholar
  42. [42]
    P. E. Thompson, Int. J. Lepr. 35, 605 (1967).Google Scholar
  43. [43]
    J. A. Waitz, B. J. Olszewski and P. E. Thompson, Science 141, 723 (1963).Google Scholar
  44. [44]
    L. H. Schmidt, R. N. Rossan and K. F. Fisher, Am. J. trop. Med. Hyg. 12, 494 (1963).Google Scholar
  45. [45]
    P. E. Thompson, J. A. Waitz and B. Olszewski, J. Parasitol. 51, 345 (1965).Google Scholar
  46. [46]
    D. H. Kaump, J. L. Schardein, R. A. Fisken and O. J. Sorenson Jr., Toxic, and appl. Pharmac. 7, 781 (1965).Google Scholar
  47. [47]
    E. R. Buchman, H. Sargent, T. C. Myers and D. R. Howton, J. Am. chem. Soc. 68, 2710 (1946).Google Scholar
  48. [48]
    W. A. Dill, R. A. Fisken, T. F. Reutner, J. K. Weston and A. J. Glazko, Antibiot. Chemother. 7, 99 (1957).Google Scholar
  49. [49]
    T. F. Reutner, R. A. Fisken, W. A. Dill, A. J. Glazko and J. K. Weston, Antibiot. Chemother. 7, 113 (1957).Google Scholar
  50. [50]
    J. H. Burckhalter, F. H. Tendick, E. M. Jones, W. F. Holcomb and A. L. Rawlins, J. Am. chem. Soc. 68, 1894 (1946).Google Scholar
  51. [51]
    E. F. Elslager and P. E. Thompson, unpublished results.Google Scholar
  52. [52]
    D. P. Jacobus, presented before The Division of Medicinal Chemistry at the 153rd National Meeting of The American Chemical Society, Miami Beach, Fla. (April 1967).Google Scholar
  53. [53]
    F. Benazet, Ann. Soc. belge Med. trop. 45, 459 (1965).Google Scholar
  54. [54]
    J. Schneider, M. Bouvry and J. Le Quellec, Abstracts, International Colloquium on P. berghei, Institute of Tropical Medicine ‘Prince Leopold’, Antwerp, Belgium (December 1964).Google Scholar
  55. [55]
    Rhone-Poulenc, French Patents 82,059/1,343,486 (1963); 82,071/1,343,486 (1963); 82,201/1,343,478 (1964); 82,306/1,343,478 (1964); 82,308/1,343,478 (1964); 1,392,458 (1965).Google Scholar
  56. [56]
    Rhone-Poulenc, Erie Patents 461/62 (1963);Google Scholar
  57. [56a]
    Rhone-Poulenc, Erie Patents 620/63 (1963);Google Scholar
  58. [56b]
    Rhone-Poulenc, Erie Patents 591/63 (1963).Google Scholar
  59. [57]
    Rhone-Poulenc, Belgian Patent 618,068 (1962).Google Scholar
  60. [58]
    Rhone-Poulenc, South African Patents 3/62 (1962);Google Scholar
  61. [58a]
    Rhone-Poulenc, South African Patents 2,220/62 (1962);Google Scholar
  62. [58a]
    Rhone-Poulenc, South African Patents 3370/63 (1964);Google Scholar
  63. [58a]
    Rhone-Poulenc, South African Patents 1391/64(1964).Google Scholar
  64. [59]
    J. G. Baget and P. Sarret, U.S. Patent 3,234,129 (1967).Google Scholar
  65. [60]
    C. La Faix, M. Rey, I. Diopmar and A. Nouhouayi, Bull. Soc. Med. Afr. Noire Lang. Fr. 12, 546 (1967);Google Scholar
  66. [60]
    C. La Faix, M. Rey, I. Diopmar and A. Nouhouayi, Trop. Dis. Bull. 65, 1225 (1968).Google Scholar
  67. [61]
    E. F. Elslager, Z. B. Gavrilis, A. A. Phillips and D. F. Worth, J. med. Chem. 12, 357 (1969).Google Scholar
  68. [62]
    E. F. Elslager, A. A. Phillips and D. F. Worth, J. med. Chem. 12, 363 (1969).Google Scholar
  69. [63]
    F. Hawking, Nature 159, 409 (1947).Google Scholar
  70. [64]
    F. Hawking and W. L. M. Perry, Br. J. Pharmac. 3, 320 (1948).Google Scholar
  71. [65]
    H. C. Carrington, A. F. Crowther, D. G. Davey, A. A. Levi and F. L. Rose, Nature 168, 1080 (1951).Google Scholar
  72. [66]
    L. H. Schmidt, T. L. Loo, R. Fradkin and H. B. Hughes, Proc. Soc. exp. Biol. Med. 80, 367 (1952).Google Scholar
  73. [67]
    C. C. Smith, J. Ihrig and R. Menne, Am. J. trop. Med. Hyg. 10, 694 (1961).Google Scholar
  74. [68]
    L. H. Schmidt, Am. J. trop. Med. Hyg. 6, 212 (1957).Google Scholar
  75. [69]
    G. I. Robertson, Trans. R. Soc. trop. Med. Hyg. 51, 488 (1957).Google Scholar
  76. [70]
    D. B. Capps, Z. B. Gavrilis and E. F. Elslager, Abstracts, 149th Meeting of The American Chemical Society, Detroit, Mich., p. 27N. (4–9, April 1965).Google Scholar
  77. [71]
    D. B. Capps, O. D. Bird, E. F. Elslager, Z. B. Gavrilis, J. A. Roush, P. E. Thompson and J. W. Vaitkus, J. Heterocyclic Chem. 5, 355 (1968).Google Scholar
  78. [72]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,074,947 (1963).Google Scholar
  79. [73]
    E. F. Elslager and D. F. Worth, U. S. Patent 3,223,705 (1965).Google Scholar
  80. [74]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,248,422 (1966).Google Scholar
  81. [75]
    G. R. Coatney, P. G. Contacos, J. S. Lunn, J. W. Kilpatrick and H. A. Elder, Am. J. trop. Med. Hyg. 12, 504 (1963).Google Scholar
  82. [76]
    G. R. Coatney, P. G. Contacos and J. S. Lunn, Am. J. trop. Med. Hyg. 13, 383 (1964).Google Scholar
  83. [77]
    R. D. Powell, R. L. De Gowin and R. B. Eppes, Am. J. trop. Med. Hyg. 14, 913 (1965).Google Scholar
  84. [78]
    P. G. Contacos, G. R. Coatney, J. S. Lunn and J. W. Kilpatrick, Am. J. trop. Med. Hyg. 13, 386 (1964).Google Scholar
  85. [79]
    P. G. Contacos, G. R. Coatney, J. S. Lunn and W. Chin, Am. J. trop. Med. Hyg. 15, 281 (1966).Google Scholar
  86. [80]
    W. Chin, J. S. Lunn, J. Buxbaum and P. G. Contacos, Am. J. trop. Med. Hyg. 14, 922 (1965).Google Scholar
  87. [81]
    W. Chin, P. G. Contacos, G. R. Coatney, M. H. Jeter and E. Alpert, Am. J. trop. Med. Hyg. 16, 580 (1967).Google Scholar
  88. [82]
    R. D. Powell, G. J. Brewer, R. L. De Gowin and A. S. Alving, Bull. Wld Hlth Org. 31, 379 (1964).Google Scholar
  89. [83]
    A. S. Alving, U.S. Govt. Res. Repts. 38, 72 (1963).Google Scholar
  90. [84]
    J. S. Lunn, W. Chin, P. G. Contacos and G. R. Coatney, Am. J. trop. Med. Hyg. 13, 783 (1964).Google Scholar
  91. [85]
    P. G. Contacos, G. R. Coatney, J. S. Lunn and W. Chin, Am. J. trop. Med. Hyg. 14, 925 (1965).Google Scholar
  92. [86]
    I. A. McGregor, K. Williams, G. H. Walker and A. K. Rahman, Br. Med. J. 1, 695 (1966).Google Scholar
  93. [87]
    R. H. Black, B. B. Dew, W. B. Hennessy, B. McMillan and D. C. Torpy, Med. J. Australian 2, 588 (1966).Google Scholar
  94. [88]
    K. H. Rieckmann, Am. J. trop. Med. Hyg. 15, 833 (1966).Google Scholar
  95. [89]
    D. F. Clyde, Malaria in Tanzania (Oxford University Press, London 1967).Google Scholar
  96. [90]
    M. Payet, P. Pene, R. Michel, M. Sankale, J. C. Bernou and I. Gueye, Bull. Soc. Med. Afr. Noire Lang. Fr. 11, 147 (1966);Google Scholar
  97. [90a]
    M. Payet, P. Pene, R. Michel, M. Sankale, J. C. Bernou and I. Gueye, Trop. Dis. Bull. 64, 145 (1967).Google Scholar
  98. [91]
    R. Michel, P. Pene and K. O. Courtney, Bull. Soc. Path. Exot. 59, 797 (1966);Google Scholar
  99. [91a]
    R. Michel, P. Pene and K. O. Courtney, Trop. Dis. Bull. 65, 101 (1968).Google Scholar
  100. [92]
    R. Michel, P. Pene and K. O. Courtney, Bull. Soc. Med. Afr. Noire Lang. Fr. 11, 463 (1966);Google Scholar
  101. [92]
    R. Michel, P. Pene and K. O. Courtney, Trop. Dis. Bull. 64, 594 (1967).Google Scholar
  102. [93]
    A. B. G. Laing, G. Pringle and F. C. T. Lane, Am. J. trop. Med. Hyg. 15, 838 (1966).Google Scholar
  103. [94]
    K. H. Rieckmann, Trans. R. Soc. trop. Med. Hyg. 61, 189 (1967).Google Scholar
  104. [95]
    D. F. Clyde, Abstracts, Eighth International Congresses on Tropical Medicine and Malaria, Teheran, Iran, 1380 (7–15 September 1968).Google Scholar
  105. [96]
    A. Pena Chavarria, E. Kotcher and C. Lizano, J. Am. med. Ass. 194, 1142 (1965).Google Scholar
  106. [97]
    F. Beltran, F. Biagi and S. Gonzalez, Prensa Med. Mex. 31, 365 (1966).Google Scholar
  107. [98]
    A. Pena Chavarria, E. Kotcher and C. Lizano, Trans. R. Soc trop. Med. Hyg. 62, 550 (1968).Google Scholar
  108. [99]
    B. C. Walton, D. A. Person, M. H. Ellman and R. Bernstein, Am. J. trop. Med. Hyg. 17, 814 (1968).Google Scholar
  109. [99a]
    L. Navarro, Boletín de la Asociación Mexicana De Patologos, A. C. 6, 210 (1968).Google Scholar
  110. [100]
    C. M. Johnson, Am. J. trop. Med. Hyg. 17, 819 (1968).Google Scholar
  111. [101]
    F. Biagi and F. Beltran, Prensa Med. Mex. 32 (1967).Google Scholar
  112. [102]
    E. A. Falco, L. G. Goodwin, G. H. Hitchings, I. M. Rollo and P. B. Russell, Br. J. Pharmac 6, 185 (1951).Google Scholar
  113. [103]
    E. F. Elslager and D. F. Worth, U. S. Patent 3,161,641 (1964).Google Scholar
  114. [104]
    E. F. Elslager and D. F. Worth, U. S. Patent 3,236,849 (1966).Google Scholar
  115. [105]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,244,716 (1966).Google Scholar
  116. [106]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,264,296 (1966).Google Scholar
  117. [107]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,278,536 (1966).Google Scholar
  118. [108]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,313,268 (1967).Google Scholar
  119. [109]
    K. G. Powers, J. Parasitol. Supplement 51, 53 (1965).Google Scholar
  120. [110]
    For a recent review, see L. Doub, Medicinal Chemistry, 5, 350–425 (Ed. W. H. Hartung; John Wiley, New York 1961).Google Scholar
  121. [111]
    L. T. Coggeshall, J. Maier and C. A. Best, J. Am. med. Ass. 117, 1077 (1941).Google Scholar
  122. [112]
    H. M. Archibald and C. M. Ross, J. trop. Med. Hyg. 63, 25 (1960).Google Scholar
  123. [113]
    A. Bishop, Parasitology 53, 10 (1063).Google Scholar
  124. [114]
    A. Bishop, Parasitology 55, 407 (1965).Google Scholar
  125. [115]
    P. E. Thompson, A. Bayles, B. Olszewski and J. A. Waitz, Am. J. trop. Med. Hyg. 14, 198 (1965).Google Scholar
  126. [116]
    S. P. Ramakrishnan, P. C. Basu, H. Singh and N. Singh, Bull. Wld Hlth Org. 27, 213 (1962).Google Scholar
  127. [117]
    E. F. Elslager and D. F. Worth, Abstracts of Papers, 149th Meeting of The American Chemical Society, Detroit, Michigan, p. 28N (4–9 April 1965).Google Scholar
  128. [118]
    P. E. Thompson and E. F. Elslager, U.S. Patent 3,215,600 (1965).Google Scholar
  129. [119]
    D. P. Jacobus, Walter Reed Army Institute of Research, Washington, personal communication (1968).Google Scholar
  130. [120]
    D. M. Aviado, Exp. Parasitol. 20, 88 (1967).Google Scholar
  131. [121]
    A. Ishii, M. Sasa, H. Chinzei, S. Ohshima, H. Tanaka and Y. Inami, Jap. J. exp. Med. 37, 301 (1967).Google Scholar
  132. [122]
    R. H. Black, W. B. Hennessy, B. McMillan, B. B. Dew and J. C. Biggs, Med. J. Australia 2, 808 (1966).Google Scholar
  133. [123]
    W. Chin, G. R. Coatney and H. K. King, Am. J. trop. Med. Hyg. 16, 13 (1967).Google Scholar
  134. [124]
    A. J. Glazko, W. A. Dill, R. G. Montalbo and E. L. Holmes, Am. J. trop. Med. Hyg. 17, 465 (1968).Google Scholar
  135. [125]
    C. C. Shepard, Proc. Soc. exp. Biol. Med. 124, 430 (1967).Google Scholar
  136. [126]
    C. C. Shepard, D. H. McRae and J. A. Habas, Proc. Soc. exp. Biol. Med. 122, 893 (1966).Google Scholar
  137. [127]
    C. C. Shepard, J. G. Tolentino and D. H. McRae, Am. J. trop. Med. Hyg. 17, 192 (1968).Google Scholar
  138. [128]
    C. C. Shepard, Intern. J. Lepr. 35, 616 (1967).Google Scholar
  139. [129]
    E. F. Elslager, A. A. Phillips and D. F. Worth, Abstracts of Papers, 157 th Meeting of the American Chemical Society, Minneapolis, Minn., p. MEDI 32 (13–18 April 1969).Google Scholar
  140. [130]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,325,522 (1967).Google Scholar
  141. [131]
    P. E. Thompson, A. Bayles and J. A. Waitz, manuscript in preparation.Google Scholar
  142. [132]
    D. F. Worth, E. F. Elslager and A. A. Phillips, J. med. Chem. 12, 591 (1969).Google Scholar
  143. [133]
    E. F. Elslager and D. F. Worth, U.S. Patent 3,325,521 (1967).Google Scholar
  144. [134]
    E. F. Elslager, D. B. Capps and D. F. Worth, J. med. Chem. 12, 597 (1969).Google Scholar
  145. [135]
    E. F. Elslager and D. B. Capps, U.S. Patent 3,419,584 (1968).Google Scholar
  146. [136]
    J. Davoll, British Patent 1,045,180 (1966).Google Scholar
  147. [137]
    J. Davoll, British Patent 1,078,887 (1967).Google Scholar
  148. [138]
    P. E. Thompson, A. Bayles and B. Olszewski, Exp. Parasitol., in press.Google Scholar
  149. [139]
    J. Davoll, A. M. Johnson, H. J. Davies, P. E. Thompson, A. Bayles, O. D. Bird, J. Roush and E. F. Elslager, J. med. Chem., in preparation.Google Scholar
  150. [140]
    Parke, Davis and Co., Iran Patent 7430 (1968).Google Scholar
  151. [141]
    P. E. Thompson, A. Bayles, B. Olszewski and L. Boche, Am. J. trop. Med. Hyg., in press.Google Scholar
  152. [142]
    J. Davoll, A. M. Johnson, J. Dickinson, P. E. Thompson, A. Bayles, O. D. Bird, J. Roush and E. F. Elslager, J. Med. Chem., in preparation.Google Scholar
  153. [143]
    E. F. Elslager, E. H. Gold, F. H. Tendick, L. M. Werbel and D. F. Worth, J. Heterocyclic Chem. 1, 6 (1964).Google Scholar
  154. [144]
    E. F. Elslager, R. E. Bowman, F. H. Tendick, D. J. Tivey and D. F. Worth, J. med. Pharm. Chem. 5, 1159 (1962).Google Scholar
  155. [145]
    E. F. Elslager and D. F. Worth, J. med. Chem., in preparation.Google Scholar
  156. [146]
    E. F. Elslager, F. H. Tendick and L. M. Werbel, J. med. Chem. 12, 600 (1969).Google Scholar
  157. [147]
    D. M. Besly and A. A. Goldberg, J. chem. Soc. 1954, 2448.Google Scholar
  158. [148]
    W. Schulemann, F. Schönhöfer and A. Wingler, U.S. Patent 1,872,826 (1932).Google Scholar

Copyright information

© Birkhäuser Verlag Basel 1969

Authors and Affiliations

  1. 1.Department of Chemistry, Medical and Scientific Affairs DivisionParke, Davis & Co.Ann ArborUSA

Personalised recommendations